Anurag Verma - Academia.edu (original) (raw)

Papers by Anurag Verma

Research paper thumbnail of Enhancement of Skin Permeation of Glibenclamide from Ethyl Cellulose- Polyvinyl Pyrollidone based Transdermal Patches Using Olive Oil and Mustard Oil as Penetration Enhancer: In vitro, Ex-vivo and In vivo Evaluation

Drug Delivery Letters, 2015

Research paper thumbnail of Topical Delivery of Drugs for the Effective Treatment of Fungal Infections of Skin

Current Pharmaceutical Design, 2015

The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 mil... more The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 million people across the globe. A wide variety of antifungal drugs has been utilized in the effective management of numerous dermatological infections. Topical treatment of fungal infections has proved to be quite advantageous due to various factors like targeting the site of infection, minimizing systemic side effects, enhanced efficacy of treatment , and improved patient compliance. In spite the fact that these agents are therapeutically active on topical application , these have restricted drug delivery across the skin resulting in insufficient therapeutic index and may exert local as well as systemic side effects. The accomplishment of topical drug delivery needs to pacify two anomalous aspects, first the barrier nature of stratum corneum, and second, deposition of drug within the skin should be ideally achieved with limited percutaneous absorption. Thus, to facilitate the delivery of antifungal drugs and improve the treatment aspects , various novel delivery carriers have been developed. This article attempts to provide an in-depth knowledge of nanoparticulate and vesicular carriers. This article focuses on the different aspects of fungal infections and their effective treatment with antifungal drugs. Efficacy of various carrier systems (nanoparticulate and vesicular carriers) in delivering antifungal drugs topically has also been discussed. Besides, compiling various research reports, this article also includes formulation considerations inclusive of regulatory aspects of ex-cipients used, the mechanisms of penetration, and patents reported.

Research paper thumbnail of Sustained stomach specific delivery of piroxicam from floating emulsion polyelectrolyte complex beads

Journal of Scientific and Industrial Research (JSIR) , 2012

This study presents development of floating emulsion polyelectrolyte complex (PEC) beads based on... more This study presents development of floating emulsion polyelectrolyte complex (PEC) beads based on gellan-chitosan PEC and Gelucire 39/01 and 50/13 without using any chemical crosslinker, and release from developed beads of piroxicam (PRM) in 0.1 M HCl (pH 1.2). Developed beads showed excellent buoyancy, significantly improved encapsulation efficiency and sustained release of PRM compared to floating gellan-chitosan beads bearing PRM. Thus emulsion PEC beads may form a potential stomach site specific drug delivery system for PRM delivery.

Research paper thumbnail of Formulation, optimization and evaluation of enteric coated tablets of Para-amino salicylate sodium

Journal of Scientific and Industrial Research (JSIR), 2012

The objective of present investigation was to develop pharmaceutically elegant, stable, economic ... more The objective of present investigation was to develop pharmaceutically elegant, stable, economic and easy to scale up enteric coated tablet formulation for intestinal delivery of highly gastric irritant and high dose drug, PAS sodium. Various capsule shaped tablet formulations were prepared using wet granulation technique. Formulations showing best flow properties were first subcoated with Opadry white, followed by enteric coating with Acryl-EZE aqueous acrylic enteric system (Eudragit L100-55 with pigment, surfactants and plasicizers). The enteric coated tablets of optimized formulation (s) exhibited best coating characteristics (measured in terms of coating uniformity and % coating process efficiency), remained intact for 120 min in 0.1 M HCl (pH 1.2) and released almost entire drug within 45 min in phosphate buffer (pH 6.8). Further, PAS exhibited excellent stability in phosphate buffer during the entire duration of dissolution. TO : T he prepared enteric coated tablets showed excellent physical and chemical stability, when subjected to accelerated stability studies for three months. Further, when compared to marketed formulation (Pasco Acri), the prepared enteric coated tablets showed excellent similarities with marketed product (with respect to disintegration time, drug release) thereby establishing bioequivalence with marketed product.

Research paper thumbnail of Ceramide palmitic acid complex based Curcumin solid lipid nanoparticles

Journal of Experimental Nanoscience, 2016

Curcumin is an important anti-inflammatory natural compound with low bioavailability which is due... more Curcumin is an important anti-inflammatory natural compound with low bioavailability which is due to poor solubility and absorption. Solid lipid nanoparticles (SLNs) loaded with Curcumin were formulated and evaluated for physical parameters and in vitro/ex vivo permeation. Further the optimised SLN was assessed for pharmacokinetic/pharmacodynamic considerations. SLNs were formulated by emulsion-solvent evaporation technique and evaluated for physical properties and in vitro drug release. Selected SLNs were evaluated for stability and then characterised for pharmacokinetic parameters and anti-inflammatory activity with reference to a commercial formulation. Spherical SLNs were obtained in the size range of 102À156 nm with negative potential. C-SLN category has shown highest entrapment efficiency. The order of drug release was S-SLN > G-SLN > C-SLN. Selected SLN formulation C-SLN-3 has shown good stability under various conditions. C-SLN-3 has demonstrated highest drug permeation through human skin and 171.623 mg drug content permeated in 24 h. It has also shown lowest lag time 0.375 h. Similarly, it has shown maximum value for C max in in vivo determination and increased the bioavailability up to 68.12%. C-SLN-3 provided 90.75% edema inhibition in 6 h. Present study shows that nature of lipids and its physicalÀchemical properties are critical for SLN formulation and can be used for designing better drug delivery systems with optimum transdermal permeation.

Research paper thumbnail of Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity

Artificial Cells, Nanomedicine, and Biotechnology, 2014

of this drug, especially in the case of rheumatic symptoms. The efficacy of transdermal formulati... more of this drug, especially in the case of rheumatic symptoms. The efficacy of transdermal formulations depends greatly on its capacity to facilitate the drug penetration through the skin. In the present study, vesicular formulations were developed, optimized, and evaluated various parameters along with in vitro and skin permeation. Bula and Ghaly (1995) first reported the liposome of ibuprofen and evaluated the effects by varying the ratio of lipid to drug, the filter size, and the stirring period during hydration of the dried lipid layer. Newa et al. (2007) prepared binary solid dispersion of ibuprofen using Poloxamer 188 and evaluated in vitro drug release and in vivo studies after oral administration. Borovac et al. (2006) prepared ibuprofen-loaded polyvinyl alcohol-based hydro-gel beads to alleviate side effects, such as inflammation and pain, following uterine artery embolization for the treatment of leiomyomata. Ntawukulilyayo prepared xanthan gum-n-octenylsuccinate starch matrix tablet containing ibuprofen and evaluated in vitro and in vivo drug release after oral administration (Ntawukulilyayo et al. 1996). Al-Saidan (2004) observed an important phenomenon of transdermal self-permeation enhancement of ibuprofen and reported the permeation enhancer behavior of ibuprofen for itself and for diclofenac sodium. Rasool developed and evaluated chito-san gels of ibuprofen using several penetration enhancers, for example, propylene glycol, polyethylene glycol 400, oleic acid, glycerol, and menthol (Rasool et al. 2010). Shumilov et al. (2010) developed transdermal gel of ibuprofen and evaluated its pharmacokinetics and activity. Stephen et al. (2013) added peripheral vasodilators, tolazoline or papaver-ine, for increasing transdermal permeation of ibuprofen. Nanoliposome, which is submicron bilayer lipid vesicle, is a new technique for encapsulation and drug delivery. Several diverse categories of compounds, that is, drugs, cosmetics , and nutraceuticals, can be incorporated into nanoli-posomes. The applications of nanoliposomes are immense as they are biocompatible, biodegradable, and have size in nanometer range. It includes diagnosis, cancer therapeutics, Abstract Objective: Ibuprofen is an established non-steroidal anti-inflammatory drug commonly used for general inflammation. However, it causes gastrointestinal troubles when administered orally, thereby decreasing patient compliance. Transdermal application of vesicular formulation of Ibuprofen will provide better patient compliance and efficacy. Methods: Six different compositions of lipid constituents have been formulated into nanovesicles using thin-film hydration method and dispersed into gel using Carbopol 934. The formulations were characterized based on physicochemical parameters using photon correlation spectroscopy, transmission electron microscopy, in vitro drug release, ex vivo skin permeation using human skin, and in vivo studies. Results: The formulation, ibuprofen liposomal gel-5 (ILG-5), had nanoliposome of smallest size (159 nm) and polydispersity index (0.331). This formulation showed moderate zeta potential and the highest encapsulation. All the formulations including IG showed a considerable amount of drug release through in vitro synthetic membrane. ILG-5 showed maximum permeation during skin permeation studies. IG showed no permeation in ex vivo settings. ILG-5 has shown the highest C max and AUC during in vivo permeation study. Conclusions: The present work clearly shows the superiority of nanoliposome formulation over non-vesicular formulations and that lipid composition containing 7/3/1 molar ratio of phosphatidylcholine, cholesterol, and dicetyl phosphate is optimum for nanoliposome preparations, in the cases where controlled delivery of drug is needed for a sufficient period of time.

Research paper thumbnail of Ethosomes as Vesicles for Effective Transdermal Delivery: From Bench to Clinical Implementation

Current Clinical Pharmacology, 2016

Background: Drug delivery across the deeper layers of skin to make it systemically available is a... more Background: Drug delivery across the deeper layers of skin to make it systemically available is a considerable challenge in the development of a carrier. Numerous efforts have been put forward to find ways to overcome the formidable barrier of stratum corneum. Various lipid based vesicles viz liposomes, transfersomes, and invasomes have gained prominent deliberations across the globe. More recently, ethosomes have been investigated for their potential for transdermal transdermal delivery of several drugs. Objective: In the present review an attempt has been made to illustrate preclinical and clinical studies depicting enhanced safety and efficacy of drugs delivered via ethosomes. Further, patents on transdermal delivery have been highlighted specifying the effectiveness of ethosomes in the transport of therapeutic actives. Methods: Through the search engine "Scopus" literature on therapeutic categories such as antimicrobials, anti-inflammatory, and drugs acting on CNS has been collected. Results: Preclinical and clinical studies that have been carried out by various researchers affirm the potentiality of ethosomes for delivering wide variety of drugs belonging to different therapeutic categories. In vitro and in vivo permeability analyses delineated the enhancement of permeability. Consequently, enhanced transdermal flux was reported and in vivo confocal laser scanning microscopy depicted the quantity as well as depth of penetrability via ethosomes. Conclusion: From various research reports, it can be concluded that ethosomes are the competent and efficient vesicles to provide better drug transport via transdermal route.

Research paper thumbnail of Feasibility of binary composition in development of nanoethosomal glycolic vesicles of triamcinolone acetonide using Box-behnken design: in vitro and ex vivo characterization View supplementary material

Artificial Cells, Nanomedicine, and Biotechnology, 2016

Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited pen... more Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited penetration into the epidermis. This investigation aimed to explore the role of binary solvents in topical drug delivery of TA by developing nanoethosomal glycolic lipid vesicles by infusion method. Screening of vesicles (TA1-TA17) formulated by Box Behnken design identified the optimized formulation (TA10) that was developed as carbomer gels. The gels were then evaluated for pharmaceutical properties and compared with control and reference ethosomal gel (RG). Higher in vitro permeation was found in gels containing TA10, prepared with or without using penetration enhancer (EGP 83.76 ± 0.72% and EG 82.42 ± 0.89%, respectively). CLSM studies depicted deeper uniform penetration of fluorescent tracer into the epidermis via EG as compared with RG and control gel. Enhanced penetration was due to combinational solvent effect exerted by ethanol and propylene glycol. Histological analysis confirmed the nonirritant potential of the gel. Thus, it can be concluded that nanoethosomal glycolic vesicles proved to be an effective non irritant carrier for improvised penetration of triamcinolone acetonide for potential topical therapeutics.

Research paper thumbnail of Gelucire Based In Situ Gelling Emulsions: A Potential Carrier for Sustained Stomach Specific Delivery of Gastric Irritant Drugs

BioMed Research International, 2013

Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatr... more Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatric patients for the treatment of arthritis and other painful disorders. The major side effects of NSAIDs are related to their effects on the stomach and bowels. The present study concerns assessment of the potential of liquid in situ gelling emulsion formulations (emulgels) as patient compliant stomach specific sustained release carrier for the delivery of highly gastric irritant drug, Piroxicam. Emulgels were prepared, without using any emulgent, by mixing different concentrations of molten Gelucire 39/01 with low viscosity sodium alginate solution prepared in deionized water at 50 ∘ C. CaCO 3 was used as buoyancy imparting as well as crosslinking agent. Emulgels so prepared were homogenous, physically stable, and rapidly formed into buoyant gelled mass when exposed to simulated gastric fluid (SGF, pH 1.2). Drug release studies carried out in SGF revealed significant retardation (í µí±ƒ < 0.05) of Piroxicam release from emulgels compared to conventional in situ gelling formulations prepared without Gelucire 39/01. Pharmacodynamic studies carried out in albino rats revealed significantly increased analgesic/anti-inflammatory response from in situ emulgels compared to conventional in situ gelling formulations. Further, in vivo toxicity studies carried out in albino rats revealed no signs of gastric ulceration upon prolonged dosing.

Research paper thumbnail of Tailored-interpenetrating polymer network beads of k-carrageenan and sodium carboxymethyl cellulose for controlled drug delivery

Journal of Drug Delivery Science and Technology, 2016

Interpenetrating polymer network (IPN) beads of k-Carrageenan and sodium carboxymethyl cellulose ... more Interpenetrating polymer network (IPN) beads of k-Carrageenan and sodium carboxymethyl cellulose (SCMC) containing Ibuprofen were prepared by water-in-water emulsion gelation process using AlCl 3 as a cross-linking agent. The impact of different formulation variables like polymer ratio, gelation time, concentration of crosslinker on physico-chemical parameters and in-vitro drug release were studied. The IPN beads were investigated through Scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analysis. The prepared beads were slightly rough, folded spherical in shape and reflected improved drug encapsulation efficiency. Swelling ability and drug release of beads in alkaline medium was substantial as that of acidic medium. Formulations showed non-Fickian transport mechanism. The results of the study indicate that drug-loaded pH sensitive IPN beads could be used to diminish drug release in an acidic medium and to regulate the drug release in alkaline medium, which would help to minimize the gastric side effects of the model NSAID ibuprofen.

Research paper thumbnail of Small-Angle Neutron Scattering Study of Nonionic Surfactant Micelles and Phase Transitions in w/o Microemulsion

Journal of Dispersion Science and Technology, 2014

The structure of micelles formed by a four component water-in-oil nonionic microemulsion surfac-t... more The structure of micelles formed by a four component water-in-oil nonionic microemulsion surfac-tant polyoxyethene (20) sorbitan monoleate (Tween 80), sorbitan monolaurate (Span 20) at ethyl oleate and deuterated water interface have been probed by small-angle neutron scattering (SANS). The total surfactant concentration in each of the samples studied (Tween 80: Span 20) is fixed at 3:2. The deuterated water content is variable at 5-60% w/w. The experimental SANS data from all the seven samples are fit well by spherical micelles interacting with hard sphere potential. Increased deuterated water leads to spherical to lamellar and rod-like micelle geometry featured in the SANS scattering data. The observed change in micelle geometry supports the characterization of phase transition between the self-assembled micelles of the nonionic microemulsion.

Research paper thumbnail of Preparation and in vitro evaluation of xanthan gum facilitated superabsorbent polymeric microspheres

Carbohydrate Polymers, 2013

Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superab-so... more Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superab-sorbent polymer (SAP) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for sustained release of ciprofloxacin hydrochloride (CIPRO). The microspheres were prepared with various ratios of hydrolyzed SAP to PVA and extent of crosslinking density. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acidic and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results, this study suggest that CIPRO loaded IPN microspheres were suitable for sustained release application.

Research paper thumbnail of Preparation and evaluation of a buflomedil hydrochloride niosomal patch for transdermal delivery

J Liposome Res,, 2014

Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-io... more Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery. Objective: The present research work was aimed to develop niosomal-based transdermal buflomedil hydrochloride patch containing a stable formulation with improved drug permeation. Materials and methods: Niosomes were prepared by solvent evaporation method using 3 2 factorial design. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. Optimized niosomal and liposomal formulation were loaded into a patch system. All the patches were then characterized for drug-excipient interaction study, scanning electron microscopy, pharmacotechnical properties and in vitro permeation studies. Result: F9 formulation having optimum vesicle size (10.09 ± 1.2 mm), highest zeta potential (À85.4 ± 0.56 mV) and maximum percent entrapment efficiency (97.09 ± 0.11%) was selected as optimized formulation. In case of liposomes, formulation F12 was selected. Patches loaded with niosomes showed 95.12 ± 1.19% cumulative amount of drug permeated as compared to liposomal vesicle-loaded patches which showed 82.21 ± 1.24% and control patches 70.10 ± 1.33%. Discussion: Flux, permeation rate and permeability coefficient were found to be higher in case of niosomal patches as compared to liposomal patches and control patches. Surfactant present in niosomes act as a penetration enhancer which contribute in the permeation enhancement of buflomedil hydrochloride from niosomes. Conclusion: Thus, it was concluded that niosomal vesicles represented to be an efficient and stable vesicular carrier for transdermal delivery of buflomedil hydrochloride.

Research paper thumbnail of Physicochemical and Pharmacological Investigation of Topical Ocular w/o Microemulsion of Timolol Maleate for Treatment of Glaucoma

Current Eye Research, 2013

Purpose: Ocular drug delivery system always remained associated with lots of difficulties and fac... more Purpose: Ocular drug delivery system always remained associated with lots of difficulties and faced issues of poor drug absorption and poor bioavailability. Timolol maleate is a nonspecific beta blocker used for reduction of elevated intraocular pressure in glaucoma. Timolol maleate is absorbed systemically and is contraindicated in asthmatic patients. This study is focused to deliver Timolol maleate by a w/o microemulsion to extend the time of reduced intraocular pressure of glaucomatous rabbit's eye measured by using a schoetz tonometer. Methods: The microemulsion is prepared by mixing the oily components with two nonionic surfactants, drug and water, and evaluated for the physicochemical, in vitro and in vivo parameters. Results: The colloidal system demonstrates monodisperse distribution behavior and exhibits a uniform size distribution of finite width. In vitro drug release from microemulsion was found to follow Higuchi's pattern followed by a zero-order drug release by the emulsion. Ex vivo permeation through goat cornea revealed delayed release of Timolol maleate from microemulsion as compared with its aqueous solution. A reduction in intraocular pressure is seen lasting for 12 h compared to aqueous eye drop that lasted for only 5 h. Conclusion: In vivo reduction of intraocular pressure revealed a similar efficacy for once daily dosed 0.3% Timolol maleate in microemulsion formulation compared to 0.5% concentration in both microemulsion as well as aqueous formulation. The possible outcome of dose reduction will reduce the cardiovascular side effects generally reported with Timolol maleate eye drops.

Research paper thumbnail of Low molecular mass chitosan as carrier for a hydrodynamically balanced system for sustained delivery of ciprofloxacin hydrochloride

Acta Pharm., 2012

An important criterion in the selection of polymers as carriers for drug delivery is their metabo... more An important criterion in the selection of polymers as carriers for drug delivery is their metabolic fate in the body or biodegradation. Researchers have strived to engineer or discover polymeric materials. Practically limitless are combinations of these materials to regulate the physical and chemical properties of drug delivery systems, such as their permeability, environmental response, surface functionality, biodegradability, and biore-cognition sites to produce »intelligent» drug delivery systems. Of these, chitosan has re-237 Acta Pharm. 62 (2012) 237-250 Chitosan has become a focus of major interest in recent years due to its excellent biocompatibility, biodegradabi-lity and non-toxicity. Although this material has already been extensively investigated in the design of different types of drug delivery systems, it is still little explored for stomach specific drug delivery systems. The objective of the present investigation was to explore the potential of low molecular mass chitosan (LMCH) as carrier for a hydrodynamically balanced system (HBS) for sustained delivery of water soluble drug ciprofloxacin hydrochlo-ride (CP). Various formulations were prepared by physical blending of drug and polymer(s) in varying ratios followed by encapsulation into hard gelatin capsules. All the formulations remained buoyant in 0.1 mol L-1 HCl (pH 1.2) throughout the experiment. Effect of addition of xanthan gum (XG) or ethyl cellulose (EC) on drug release was also investigated. Zero order drug release was obtained from the formulations containing LMCH alone or in combination with XG, and in one instance also with EC. Our results suggest that LMCH alone or in combination with XG is an excellent material for stomach specific sustained delivery of CP from hydrodynamically balanced single unit capsules.

Research paper thumbnail of Effect of hydrophilic and hydrophobic polymers on permeation of S-amlodipine besylate through intercalated polymeric transdermal matrix: 3(2) designing, optimization and characterization

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2019

Objective: Innovation in material science has made it possible to fabricate a pharmaceutical mate... more Objective: Innovation in material science has made it possible to fabricate a pharmaceutical material of modifiable characteristics and utility, in delivering therapeutics at a sustained/controlled rate. The objective of this study is to design and optimize the controlled release transdermal films of S-Amlodipine besylate by intercalating hydrophilic and hydrophobic polymers. Methods: 3(2) factorial design and response surface methodology was utilized to prepare formulations by intercalating the varied concentration of polymers(A) and penetration enhancer(B) in solvent. The effect of these independent factors on drug release and flux was investigated to substantiate the ex-vivo, stability and histological findings of the study. Results: FTIR, DSC revealed the compatibility of drug with polymers; however, the semicrystallinity in drug was observed under PXRD. SEM micrographs showed homogeneous dispersion and entanglement of drug throughout the matrix. Results from the permeation study suggested the significant effect of factors on the ex vivo permeation of drug. It was observed that drug release was found to be increased with an increase in hydrophilic polymer concentration and PE. The formulations having polymers (EC:PVPK-30) at 7:3 showed maximum drug release with highest flux (102.60 ± 1.12 mg/cm 2 /h) and permeability coefficient (32.78 ± 1.38 cm/h). Significant effect of PE on lipid and protein framework of the skin was also observed which is responsible for increased permeation. The optimized formulation was found to be stable and showed no-sign of localized reactions, indicating safety and compatibility with the skin. Conclusion: Thus, results indicated that the prepared intercalated transdermal matrix can be a promising nonoral carrier to deliver effective amounts of drug.

Research paper thumbnail of Helicobacter pylori: past, current and future treatment strategies with gastroretentive drug delivery systems

Journal of Drug Targeting, 2016

(2016): Helicobacter pylori: past, current and future treatment strategies with gastroretentive d... more (2016): Helicobacter pylori: past, current and future treatment strategies with gastroretentive drug delivery systems, Journal of Drug Targeting,

Research paper thumbnail of Chitosan based in situ forming polyelectrolyte complexes: A potential sustained drug delivery polymeric carrier for high dose drugs

Materials Science and Engineering C, 2017

The present study investigated the feasibility of using combination of Cationic and anionic polym... more The present study investigated the feasibility of using combination of Cationic and anionic polymers as sustained release carrier for the delivery of high dose gastric acid soluble model drug Paracetamol. Various formulations were prepared using wet granulation technique. Briefly a cooled (4 °C) neutral solution of chitosan (CH) was combined with cooled aqueous solution (4 °C) of anionic polymer such as Gum Ghatti (GG) and Xanthan gum (XG). This polyelectrolyte solution was then used to granulate the model drug Paracetamol. The prepared tablets were evaluated for various pharmacopoeial and non pharmacopoeial parameters viz. Thickness, Hardness, Fria-bility, Weight Variation, Content uniformity and Drug Content. The drug release study carried out in 0.1 M HCl revealed in situ Polyelectrolyte complex formation (PEC) between CH and anionic biopolymers. This in situ PEC formation resulted in sustained delivery of high dose gastric fluid soluble drug Paracetamol. Further, effect of incorporation starch and lactose as tablet diluents on release rate was also studied. It was observed that para-cetamol release from lactose granulation was faster than tablets prepared with starch as diluents. From the data generated it was concluded that In situ PEC formation approach has sufficient potential to sustain the release of drugs like paracetamol.

Research paper thumbnail of Chitosan-Hydroxypropyl Methylcellulose Matrices as Carriers for Hydro- dynamically Balanced Capsules of Moxifloxacin HCl

Current Drug Delivery, 2016

Background: In recent years, gastroretentive, hydrodynamically balanced system (HBS) for stomach-... more Background: In recent years, gastroretentive, hydrodynamically balanced system (HBS) for stomach-specific floating sustained drug release has gained a lot of importance in improving absorption of drugs especially those absorbed from stomach and small intestine. Objective: The objective of the current investigation is to evaluate chitosan-hydroxypropyl methylcellulose (HPMC) based on polymeric matrices as a carrier for single-unit capsules based on HBS for stomach-specific floating sustained drug release using moxifloxacin HCl (MX) as a model drug. Method: Various HBS capsules of MX were prepared by physical blending of MX with chitosan (low or medium molecular mass) or HPMC (K4M or K15M) or chitosan-HPMC combinations in varying proportions followed by encapsulation into size 0 capsules made of hard gelatin. The in vitro buoyancy and drug release in 0.1 N HCl (pH 1.2) were evaluated. Results: HBS capsules based on chitosan (low and medium molecular weight and their combination) as polymer matrix failed to float on 0.1 N HCl (pH 1.2). Whereas, formulations containing HPMC (K4M or K15M) or their mixture with chitosan, remained buoyant and released MX over 9 h in the acidic dissolution medium following zero-order kinetics. Conclusion: HPMC (K4M, K15M, blend of K4M and K15M) or their mixture with low/medium molecular mass chitosan may constitute excellent carrier systems for the stomach-specific sustained delivery of MX over a longer period.

Research paper thumbnail of A RP-HPLC method for quantification of diclofenac sodium released from biological macromolecules

International Journal of Biological Macromolecules, 2013

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and so... more Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug, were prepared by single water-in-water (w/w) emulsion gelation process using AlCl 3 as cross-linking agent in a complete aqueous environment. Pharmacokinetic study of these IPN microbeads was then carried out by a simple and feasible high-performance liquid chromatographic method with UV detection which was developed and validated for the quantification of diclofenac sodium in rabbit plasma. The chromatographic separation was carried out in a Hypersil BDS, C18 column (250 mm × 4.6 mm; 5 m). The mobile phase was a mixture of acetonitrile and methanol (70:30, v/v) at a flow rate of 1.0 ml/min. The UV detection was set at 276 nm. The extraction recovery of diclofenac sodium in plasma of three quality control (QC) samples was ranged from 81.52% to 95.29%. The calibration curve was linear in the concentration range of 20-1000 ng/ml with the correlation coefficient (r 2) above 0.9951. The method was specific and sensitive with the limit of quantification of 20 ng/ml. In stability tests, diclofenac sodium in rabbit plasma was stable during storage and assay procedure.

Research paper thumbnail of Enhancement of Skin Permeation of Glibenclamide from Ethyl Cellulose- Polyvinyl Pyrollidone based Transdermal Patches Using Olive Oil and Mustard Oil as Penetration Enhancer: In vitro, Ex-vivo and In vivo Evaluation

Drug Delivery Letters, 2015

Research paper thumbnail of Topical Delivery of Drugs for the Effective Treatment of Fungal Infections of Skin

Current Pharmaceutical Design, 2015

The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 mil... more The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 million people across the globe. A wide variety of antifungal drugs has been utilized in the effective management of numerous dermatological infections. Topical treatment of fungal infections has proved to be quite advantageous due to various factors like targeting the site of infection, minimizing systemic side effects, enhanced efficacy of treatment , and improved patient compliance. In spite the fact that these agents are therapeutically active on topical application , these have restricted drug delivery across the skin resulting in insufficient therapeutic index and may exert local as well as systemic side effects. The accomplishment of topical drug delivery needs to pacify two anomalous aspects, first the barrier nature of stratum corneum, and second, deposition of drug within the skin should be ideally achieved with limited percutaneous absorption. Thus, to facilitate the delivery of antifungal drugs and improve the treatment aspects , various novel delivery carriers have been developed. This article attempts to provide an in-depth knowledge of nanoparticulate and vesicular carriers. This article focuses on the different aspects of fungal infections and their effective treatment with antifungal drugs. Efficacy of various carrier systems (nanoparticulate and vesicular carriers) in delivering antifungal drugs topically has also been discussed. Besides, compiling various research reports, this article also includes formulation considerations inclusive of regulatory aspects of ex-cipients used, the mechanisms of penetration, and patents reported.

Research paper thumbnail of Sustained stomach specific delivery of piroxicam from floating emulsion polyelectrolyte complex beads

Journal of Scientific and Industrial Research (JSIR) , 2012

This study presents development of floating emulsion polyelectrolyte complex (PEC) beads based on... more This study presents development of floating emulsion polyelectrolyte complex (PEC) beads based on gellan-chitosan PEC and Gelucire 39/01 and 50/13 without using any chemical crosslinker, and release from developed beads of piroxicam (PRM) in 0.1 M HCl (pH 1.2). Developed beads showed excellent buoyancy, significantly improved encapsulation efficiency and sustained release of PRM compared to floating gellan-chitosan beads bearing PRM. Thus emulsion PEC beads may form a potential stomach site specific drug delivery system for PRM delivery.

Research paper thumbnail of Formulation, optimization and evaluation of enteric coated tablets of Para-amino salicylate sodium

Journal of Scientific and Industrial Research (JSIR), 2012

The objective of present investigation was to develop pharmaceutically elegant, stable, economic ... more The objective of present investigation was to develop pharmaceutically elegant, stable, economic and easy to scale up enteric coated tablet formulation for intestinal delivery of highly gastric irritant and high dose drug, PAS sodium. Various capsule shaped tablet formulations were prepared using wet granulation technique. Formulations showing best flow properties were first subcoated with Opadry white, followed by enteric coating with Acryl-EZE aqueous acrylic enteric system (Eudragit L100-55 with pigment, surfactants and plasicizers). The enteric coated tablets of optimized formulation (s) exhibited best coating characteristics (measured in terms of coating uniformity and % coating process efficiency), remained intact for 120 min in 0.1 M HCl (pH 1.2) and released almost entire drug within 45 min in phosphate buffer (pH 6.8). Further, PAS exhibited excellent stability in phosphate buffer during the entire duration of dissolution. TO : T he prepared enteric coated tablets showed excellent physical and chemical stability, when subjected to accelerated stability studies for three months. Further, when compared to marketed formulation (Pasco Acri), the prepared enteric coated tablets showed excellent similarities with marketed product (with respect to disintegration time, drug release) thereby establishing bioequivalence with marketed product.

Research paper thumbnail of Ceramide palmitic acid complex based Curcumin solid lipid nanoparticles

Journal of Experimental Nanoscience, 2016

Curcumin is an important anti-inflammatory natural compound with low bioavailability which is due... more Curcumin is an important anti-inflammatory natural compound with low bioavailability which is due to poor solubility and absorption. Solid lipid nanoparticles (SLNs) loaded with Curcumin were formulated and evaluated for physical parameters and in vitro/ex vivo permeation. Further the optimised SLN was assessed for pharmacokinetic/pharmacodynamic considerations. SLNs were formulated by emulsion-solvent evaporation technique and evaluated for physical properties and in vitro drug release. Selected SLNs were evaluated for stability and then characterised for pharmacokinetic parameters and anti-inflammatory activity with reference to a commercial formulation. Spherical SLNs were obtained in the size range of 102À156 nm with negative potential. C-SLN category has shown highest entrapment efficiency. The order of drug release was S-SLN > G-SLN > C-SLN. Selected SLN formulation C-SLN-3 has shown good stability under various conditions. C-SLN-3 has demonstrated highest drug permeation through human skin and 171.623 mg drug content permeated in 24 h. It has also shown lowest lag time 0.375 h. Similarly, it has shown maximum value for C max in in vivo determination and increased the bioavailability up to 68.12%. C-SLN-3 provided 90.75% edema inhibition in 6 h. Present study shows that nature of lipids and its physicalÀchemical properties are critical for SLN formulation and can be used for designing better drug delivery systems with optimum transdermal permeation.

Research paper thumbnail of Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity

Artificial Cells, Nanomedicine, and Biotechnology, 2014

of this drug, especially in the case of rheumatic symptoms. The efficacy of transdermal formulati... more of this drug, especially in the case of rheumatic symptoms. The efficacy of transdermal formulations depends greatly on its capacity to facilitate the drug penetration through the skin. In the present study, vesicular formulations were developed, optimized, and evaluated various parameters along with in vitro and skin permeation. Bula and Ghaly (1995) first reported the liposome of ibuprofen and evaluated the effects by varying the ratio of lipid to drug, the filter size, and the stirring period during hydration of the dried lipid layer. Newa et al. (2007) prepared binary solid dispersion of ibuprofen using Poloxamer 188 and evaluated in vitro drug release and in vivo studies after oral administration. Borovac et al. (2006) prepared ibuprofen-loaded polyvinyl alcohol-based hydro-gel beads to alleviate side effects, such as inflammation and pain, following uterine artery embolization for the treatment of leiomyomata. Ntawukulilyayo prepared xanthan gum-n-octenylsuccinate starch matrix tablet containing ibuprofen and evaluated in vitro and in vivo drug release after oral administration (Ntawukulilyayo et al. 1996). Al-Saidan (2004) observed an important phenomenon of transdermal self-permeation enhancement of ibuprofen and reported the permeation enhancer behavior of ibuprofen for itself and for diclofenac sodium. Rasool developed and evaluated chito-san gels of ibuprofen using several penetration enhancers, for example, propylene glycol, polyethylene glycol 400, oleic acid, glycerol, and menthol (Rasool et al. 2010). Shumilov et al. (2010) developed transdermal gel of ibuprofen and evaluated its pharmacokinetics and activity. Stephen et al. (2013) added peripheral vasodilators, tolazoline or papaver-ine, for increasing transdermal permeation of ibuprofen. Nanoliposome, which is submicron bilayer lipid vesicle, is a new technique for encapsulation and drug delivery. Several diverse categories of compounds, that is, drugs, cosmetics , and nutraceuticals, can be incorporated into nanoli-posomes. The applications of nanoliposomes are immense as they are biocompatible, biodegradable, and have size in nanometer range. It includes diagnosis, cancer therapeutics, Abstract Objective: Ibuprofen is an established non-steroidal anti-inflammatory drug commonly used for general inflammation. However, it causes gastrointestinal troubles when administered orally, thereby decreasing patient compliance. Transdermal application of vesicular formulation of Ibuprofen will provide better patient compliance and efficacy. Methods: Six different compositions of lipid constituents have been formulated into nanovesicles using thin-film hydration method and dispersed into gel using Carbopol 934. The formulations were characterized based on physicochemical parameters using photon correlation spectroscopy, transmission electron microscopy, in vitro drug release, ex vivo skin permeation using human skin, and in vivo studies. Results: The formulation, ibuprofen liposomal gel-5 (ILG-5), had nanoliposome of smallest size (159 nm) and polydispersity index (0.331). This formulation showed moderate zeta potential and the highest encapsulation. All the formulations including IG showed a considerable amount of drug release through in vitro synthetic membrane. ILG-5 showed maximum permeation during skin permeation studies. IG showed no permeation in ex vivo settings. ILG-5 has shown the highest C max and AUC during in vivo permeation study. Conclusions: The present work clearly shows the superiority of nanoliposome formulation over non-vesicular formulations and that lipid composition containing 7/3/1 molar ratio of phosphatidylcholine, cholesterol, and dicetyl phosphate is optimum for nanoliposome preparations, in the cases where controlled delivery of drug is needed for a sufficient period of time.

Research paper thumbnail of Ethosomes as Vesicles for Effective Transdermal Delivery: From Bench to Clinical Implementation

Current Clinical Pharmacology, 2016

Background: Drug delivery across the deeper layers of skin to make it systemically available is a... more Background: Drug delivery across the deeper layers of skin to make it systemically available is a considerable challenge in the development of a carrier. Numerous efforts have been put forward to find ways to overcome the formidable barrier of stratum corneum. Various lipid based vesicles viz liposomes, transfersomes, and invasomes have gained prominent deliberations across the globe. More recently, ethosomes have been investigated for their potential for transdermal transdermal delivery of several drugs. Objective: In the present review an attempt has been made to illustrate preclinical and clinical studies depicting enhanced safety and efficacy of drugs delivered via ethosomes. Further, patents on transdermal delivery have been highlighted specifying the effectiveness of ethosomes in the transport of therapeutic actives. Methods: Through the search engine "Scopus" literature on therapeutic categories such as antimicrobials, anti-inflammatory, and drugs acting on CNS has been collected. Results: Preclinical and clinical studies that have been carried out by various researchers affirm the potentiality of ethosomes for delivering wide variety of drugs belonging to different therapeutic categories. In vitro and in vivo permeability analyses delineated the enhancement of permeability. Consequently, enhanced transdermal flux was reported and in vivo confocal laser scanning microscopy depicted the quantity as well as depth of penetrability via ethosomes. Conclusion: From various research reports, it can be concluded that ethosomes are the competent and efficient vesicles to provide better drug transport via transdermal route.

Research paper thumbnail of Feasibility of binary composition in development of nanoethosomal glycolic vesicles of triamcinolone acetonide using Box-behnken design: in vitro and ex vivo characterization View supplementary material

Artificial Cells, Nanomedicine, and Biotechnology, 2016

Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited pen... more Triamcinolone acetonide (TA) employed for the treatment of atopic dermatitis exhibits limited penetration into the epidermis. This investigation aimed to explore the role of binary solvents in topical drug delivery of TA by developing nanoethosomal glycolic lipid vesicles by infusion method. Screening of vesicles (TA1-TA17) formulated by Box Behnken design identified the optimized formulation (TA10) that was developed as carbomer gels. The gels were then evaluated for pharmaceutical properties and compared with control and reference ethosomal gel (RG). Higher in vitro permeation was found in gels containing TA10, prepared with or without using penetration enhancer (EGP 83.76 ± 0.72% and EG 82.42 ± 0.89%, respectively). CLSM studies depicted deeper uniform penetration of fluorescent tracer into the epidermis via EG as compared with RG and control gel. Enhanced penetration was due to combinational solvent effect exerted by ethanol and propylene glycol. Histological analysis confirmed the nonirritant potential of the gel. Thus, it can be concluded that nanoethosomal glycolic vesicles proved to be an effective non irritant carrier for improvised penetration of triamcinolone acetonide for potential topical therapeutics.

Research paper thumbnail of Gelucire Based In Situ Gelling Emulsions: A Potential Carrier for Sustained Stomach Specific Delivery of Gastric Irritant Drugs

BioMed Research International, 2013

Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatr... more Non steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed medications to the geriatric patients for the treatment of arthritis and other painful disorders. The major side effects of NSAIDs are related to their effects on the stomach and bowels. The present study concerns assessment of the potential of liquid in situ gelling emulsion formulations (emulgels) as patient compliant stomach specific sustained release carrier for the delivery of highly gastric irritant drug, Piroxicam. Emulgels were prepared, without using any emulgent, by mixing different concentrations of molten Gelucire 39/01 with low viscosity sodium alginate solution prepared in deionized water at 50 ∘ C. CaCO 3 was used as buoyancy imparting as well as crosslinking agent. Emulgels so prepared were homogenous, physically stable, and rapidly formed into buoyant gelled mass when exposed to simulated gastric fluid (SGF, pH 1.2). Drug release studies carried out in SGF revealed significant retardation (í µí±ƒ < 0.05) of Piroxicam release from emulgels compared to conventional in situ gelling formulations prepared without Gelucire 39/01. Pharmacodynamic studies carried out in albino rats revealed significantly increased analgesic/anti-inflammatory response from in situ emulgels compared to conventional in situ gelling formulations. Further, in vivo toxicity studies carried out in albino rats revealed no signs of gastric ulceration upon prolonged dosing.

Research paper thumbnail of Tailored-interpenetrating polymer network beads of k-carrageenan and sodium carboxymethyl cellulose for controlled drug delivery

Journal of Drug Delivery Science and Technology, 2016

Interpenetrating polymer network (IPN) beads of k-Carrageenan and sodium carboxymethyl cellulose ... more Interpenetrating polymer network (IPN) beads of k-Carrageenan and sodium carboxymethyl cellulose (SCMC) containing Ibuprofen were prepared by water-in-water emulsion gelation process using AlCl 3 as a cross-linking agent. The impact of different formulation variables like polymer ratio, gelation time, concentration of crosslinker on physico-chemical parameters and in-vitro drug release were studied. The IPN beads were investigated through Scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analysis. The prepared beads were slightly rough, folded spherical in shape and reflected improved drug encapsulation efficiency. Swelling ability and drug release of beads in alkaline medium was substantial as that of acidic medium. Formulations showed non-Fickian transport mechanism. The results of the study indicate that drug-loaded pH sensitive IPN beads could be used to diminish drug release in an acidic medium and to regulate the drug release in alkaline medium, which would help to minimize the gastric side effects of the model NSAID ibuprofen.

Research paper thumbnail of Small-Angle Neutron Scattering Study of Nonionic Surfactant Micelles and Phase Transitions in w/o Microemulsion

Journal of Dispersion Science and Technology, 2014

The structure of micelles formed by a four component water-in-oil nonionic microemulsion surfac-t... more The structure of micelles formed by a four component water-in-oil nonionic microemulsion surfac-tant polyoxyethene (20) sorbitan monoleate (Tween 80), sorbitan monolaurate (Span 20) at ethyl oleate and deuterated water interface have been probed by small-angle neutron scattering (SANS). The total surfactant concentration in each of the samples studied (Tween 80: Span 20) is fixed at 3:2. The deuterated water content is variable at 5-60% w/w. The experimental SANS data from all the seven samples are fit well by spherical micelles interacting with hard sphere potential. Increased deuterated water leads to spherical to lamellar and rod-like micelle geometry featured in the SANS scattering data. The observed change in micelle geometry supports the characterization of phase transition between the self-assembled micelles of the nonionic microemulsion.

Research paper thumbnail of Preparation and in vitro evaluation of xanthan gum facilitated superabsorbent polymeric microspheres

Carbohydrate Polymers, 2013

Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superab-so... more Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superab-sorbent polymer (SAP) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for sustained release of ciprofloxacin hydrochloride (CIPRO). The microspheres were prepared with various ratios of hydrolyzed SAP to PVA and extent of crosslinking density. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acidic and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results, this study suggest that CIPRO loaded IPN microspheres were suitable for sustained release application.

Research paper thumbnail of Preparation and evaluation of a buflomedil hydrochloride niosomal patch for transdermal delivery

J Liposome Res,, 2014

Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-io... more Context: Niosomes are the non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants. These are the promising vehicles for effective transdermal drug delivery. Objective: The present research work was aimed to develop niosomal-based transdermal buflomedil hydrochloride patch containing a stable formulation with improved drug permeation. Materials and methods: Niosomes were prepared by solvent evaporation method using 3 2 factorial design. All the formulations were evaluated for vesicle size, zeta potential and percent entrapment efficiency. Optimized niosomal and liposomal formulation were loaded into a patch system. All the patches were then characterized for drug-excipient interaction study, scanning electron microscopy, pharmacotechnical properties and in vitro permeation studies. Result: F9 formulation having optimum vesicle size (10.09 ± 1.2 mm), highest zeta potential (À85.4 ± 0.56 mV) and maximum percent entrapment efficiency (97.09 ± 0.11%) was selected as optimized formulation. In case of liposomes, formulation F12 was selected. Patches loaded with niosomes showed 95.12 ± 1.19% cumulative amount of drug permeated as compared to liposomal vesicle-loaded patches which showed 82.21 ± 1.24% and control patches 70.10 ± 1.33%. Discussion: Flux, permeation rate and permeability coefficient were found to be higher in case of niosomal patches as compared to liposomal patches and control patches. Surfactant present in niosomes act as a penetration enhancer which contribute in the permeation enhancement of buflomedil hydrochloride from niosomes. Conclusion: Thus, it was concluded that niosomal vesicles represented to be an efficient and stable vesicular carrier for transdermal delivery of buflomedil hydrochloride.

Research paper thumbnail of Physicochemical and Pharmacological Investigation of Topical Ocular w/o Microemulsion of Timolol Maleate for Treatment of Glaucoma

Current Eye Research, 2013

Purpose: Ocular drug delivery system always remained associated with lots of difficulties and fac... more Purpose: Ocular drug delivery system always remained associated with lots of difficulties and faced issues of poor drug absorption and poor bioavailability. Timolol maleate is a nonspecific beta blocker used for reduction of elevated intraocular pressure in glaucoma. Timolol maleate is absorbed systemically and is contraindicated in asthmatic patients. This study is focused to deliver Timolol maleate by a w/o microemulsion to extend the time of reduced intraocular pressure of glaucomatous rabbit's eye measured by using a schoetz tonometer. Methods: The microemulsion is prepared by mixing the oily components with two nonionic surfactants, drug and water, and evaluated for the physicochemical, in vitro and in vivo parameters. Results: The colloidal system demonstrates monodisperse distribution behavior and exhibits a uniform size distribution of finite width. In vitro drug release from microemulsion was found to follow Higuchi's pattern followed by a zero-order drug release by the emulsion. Ex vivo permeation through goat cornea revealed delayed release of Timolol maleate from microemulsion as compared with its aqueous solution. A reduction in intraocular pressure is seen lasting for 12 h compared to aqueous eye drop that lasted for only 5 h. Conclusion: In vivo reduction of intraocular pressure revealed a similar efficacy for once daily dosed 0.3% Timolol maleate in microemulsion formulation compared to 0.5% concentration in both microemulsion as well as aqueous formulation. The possible outcome of dose reduction will reduce the cardiovascular side effects generally reported with Timolol maleate eye drops.

Research paper thumbnail of Low molecular mass chitosan as carrier for a hydrodynamically balanced system for sustained delivery of ciprofloxacin hydrochloride

Acta Pharm., 2012

An important criterion in the selection of polymers as carriers for drug delivery is their metabo... more An important criterion in the selection of polymers as carriers for drug delivery is their metabolic fate in the body or biodegradation. Researchers have strived to engineer or discover polymeric materials. Practically limitless are combinations of these materials to regulate the physical and chemical properties of drug delivery systems, such as their permeability, environmental response, surface functionality, biodegradability, and biore-cognition sites to produce »intelligent» drug delivery systems. Of these, chitosan has re-237 Acta Pharm. 62 (2012) 237-250 Chitosan has become a focus of major interest in recent years due to its excellent biocompatibility, biodegradabi-lity and non-toxicity. Although this material has already been extensively investigated in the design of different types of drug delivery systems, it is still little explored for stomach specific drug delivery systems. The objective of the present investigation was to explore the potential of low molecular mass chitosan (LMCH) as carrier for a hydrodynamically balanced system (HBS) for sustained delivery of water soluble drug ciprofloxacin hydrochlo-ride (CP). Various formulations were prepared by physical blending of drug and polymer(s) in varying ratios followed by encapsulation into hard gelatin capsules. All the formulations remained buoyant in 0.1 mol L-1 HCl (pH 1.2) throughout the experiment. Effect of addition of xanthan gum (XG) or ethyl cellulose (EC) on drug release was also investigated. Zero order drug release was obtained from the formulations containing LMCH alone or in combination with XG, and in one instance also with EC. Our results suggest that LMCH alone or in combination with XG is an excellent material for stomach specific sustained delivery of CP from hydrodynamically balanced single unit capsules.

Research paper thumbnail of Effect of hydrophilic and hydrophobic polymers on permeation of S-amlodipine besylate through intercalated polymeric transdermal matrix: 3(2) designing, optimization and characterization

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2019

Objective: Innovation in material science has made it possible to fabricate a pharmaceutical mate... more Objective: Innovation in material science has made it possible to fabricate a pharmaceutical material of modifiable characteristics and utility, in delivering therapeutics at a sustained/controlled rate. The objective of this study is to design and optimize the controlled release transdermal films of S-Amlodipine besylate by intercalating hydrophilic and hydrophobic polymers. Methods: 3(2) factorial design and response surface methodology was utilized to prepare formulations by intercalating the varied concentration of polymers(A) and penetration enhancer(B) in solvent. The effect of these independent factors on drug release and flux was investigated to substantiate the ex-vivo, stability and histological findings of the study. Results: FTIR, DSC revealed the compatibility of drug with polymers; however, the semicrystallinity in drug was observed under PXRD. SEM micrographs showed homogeneous dispersion and entanglement of drug throughout the matrix. Results from the permeation study suggested the significant effect of factors on the ex vivo permeation of drug. It was observed that drug release was found to be increased with an increase in hydrophilic polymer concentration and PE. The formulations having polymers (EC:PVPK-30) at 7:3 showed maximum drug release with highest flux (102.60 ± 1.12 mg/cm 2 /h) and permeability coefficient (32.78 ± 1.38 cm/h). Significant effect of PE on lipid and protein framework of the skin was also observed which is responsible for increased permeation. The optimized formulation was found to be stable and showed no-sign of localized reactions, indicating safety and compatibility with the skin. Conclusion: Thus, results indicated that the prepared intercalated transdermal matrix can be a promising nonoral carrier to deliver effective amounts of drug.

Research paper thumbnail of Helicobacter pylori: past, current and future treatment strategies with gastroretentive drug delivery systems

Journal of Drug Targeting, 2016

(2016): Helicobacter pylori: past, current and future treatment strategies with gastroretentive d... more (2016): Helicobacter pylori: past, current and future treatment strategies with gastroretentive drug delivery systems, Journal of Drug Targeting,

Research paper thumbnail of Chitosan based in situ forming polyelectrolyte complexes: A potential sustained drug delivery polymeric carrier for high dose drugs

Materials Science and Engineering C, 2017

The present study investigated the feasibility of using combination of Cationic and anionic polym... more The present study investigated the feasibility of using combination of Cationic and anionic polymers as sustained release carrier for the delivery of high dose gastric acid soluble model drug Paracetamol. Various formulations were prepared using wet granulation technique. Briefly a cooled (4 °C) neutral solution of chitosan (CH) was combined with cooled aqueous solution (4 °C) of anionic polymer such as Gum Ghatti (GG) and Xanthan gum (XG). This polyelectrolyte solution was then used to granulate the model drug Paracetamol. The prepared tablets were evaluated for various pharmacopoeial and non pharmacopoeial parameters viz. Thickness, Hardness, Fria-bility, Weight Variation, Content uniformity and Drug Content. The drug release study carried out in 0.1 M HCl revealed in situ Polyelectrolyte complex formation (PEC) between CH and anionic biopolymers. This in situ PEC formation resulted in sustained delivery of high dose gastric fluid soluble drug Paracetamol. Further, effect of incorporation starch and lactose as tablet diluents on release rate was also studied. It was observed that para-cetamol release from lactose granulation was faster than tablets prepared with starch as diluents. From the data generated it was concluded that In situ PEC formation approach has sufficient potential to sustain the release of drugs like paracetamol.

Research paper thumbnail of Chitosan-Hydroxypropyl Methylcellulose Matrices as Carriers for Hydro- dynamically Balanced Capsules of Moxifloxacin HCl

Current Drug Delivery, 2016

Background: In recent years, gastroretentive, hydrodynamically balanced system (HBS) for stomach-... more Background: In recent years, gastroretentive, hydrodynamically balanced system (HBS) for stomach-specific floating sustained drug release has gained a lot of importance in improving absorption of drugs especially those absorbed from stomach and small intestine. Objective: The objective of the current investigation is to evaluate chitosan-hydroxypropyl methylcellulose (HPMC) based on polymeric matrices as a carrier for single-unit capsules based on HBS for stomach-specific floating sustained drug release using moxifloxacin HCl (MX) as a model drug. Method: Various HBS capsules of MX were prepared by physical blending of MX with chitosan (low or medium molecular mass) or HPMC (K4M or K15M) or chitosan-HPMC combinations in varying proportions followed by encapsulation into size 0 capsules made of hard gelatin. The in vitro buoyancy and drug release in 0.1 N HCl (pH 1.2) were evaluated. Results: HBS capsules based on chitosan (low and medium molecular weight and their combination) as polymer matrix failed to float on 0.1 N HCl (pH 1.2). Whereas, formulations containing HPMC (K4M or K15M) or their mixture with chitosan, remained buoyant and released MX over 9 h in the acidic dissolution medium following zero-order kinetics. Conclusion: HPMC (K4M, K15M, blend of K4M and K15M) or their mixture with low/medium molecular mass chitosan may constitute excellent carrier systems for the stomach-specific sustained delivery of MX over a longer period.

Research paper thumbnail of A RP-HPLC method for quantification of diclofenac sodium released from biological macromolecules

International Journal of Biological Macromolecules, 2013

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and so... more Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug, were prepared by single water-in-water (w/w) emulsion gelation process using AlCl 3 as cross-linking agent in a complete aqueous environment. Pharmacokinetic study of these IPN microbeads was then carried out by a simple and feasible high-performance liquid chromatographic method with UV detection which was developed and validated for the quantification of diclofenac sodium in rabbit plasma. The chromatographic separation was carried out in a Hypersil BDS, C18 column (250 mm × 4.6 mm; 5 m). The mobile phase was a mixture of acetonitrile and methanol (70:30, v/v) at a flow rate of 1.0 ml/min. The UV detection was set at 276 nm. The extraction recovery of diclofenac sodium in plasma of three quality control (QC) samples was ranged from 81.52% to 95.29%. The calibration curve was linear in the concentration range of 20-1000 ng/ml with the correlation coefficient (r 2) above 0.9951. The method was specific and sensitive with the limit of quantification of 20 ng/ml. In stability tests, diclofenac sodium in rabbit plasma was stable during storage and assay procedure.