Rajashree Hirlekar - Academia.edu (original) (raw)

Papers by Rajashree Hirlekar

International Journal of Pharmaceutical Sciences and Nanotechnology(IJPSN)

Purpose: The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of cur... more Purpose: The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of curcumin (CUR) and piperine (PIP) loaded nanostructured lipid carriers (NLCs). Methods: CUR and PIP-loaded NLCs (CP NLCs) were prepared by modified hot-melt emulsification using precirol ATO5 (PRE) as solid lipid, labrafac lipophile WL1349 (LAF) as liquid lipid, and a combination of tween 80 (T80) with gelucire 50/13 (G50/13) as surfactants. The NLCs system was subjected to physical stability, particle size, zeta potential, thermal behaviour, crystallinity study and in-vitro drug release. Further, an evaporative drying technique converted the NLC system into stable DANs by adsorbing onto mannitol (Pearlitol 200SD). The DANs were characterized for redispersion properties, particle size, flow properties and in-vitro drug release. The stability studies were carried out for 30 days. Results: The optimized CP NLCs were of imperfect type and had a mean particle size of 248.5 ± 12.8 nm (size dis...

Skin aging is influenced by many factors including ultraviolet radiation, excess alcohol consumpt... more Skin aging is influenced by many factors including ultraviolet radiation, excess alcohol consumption, tobacco abuse, and environmental pollution. Age-related skin changes are the result of genetically programmed changes (intrinsic factors) and environmental wear-and-tear on the skin (extrinsic factors). This article also provides information about wrinkles development and the approaches to stimulate collagen formation. This article provides overview on different anti-aging technologies like Intense Pulsed Light System, Liposomal Encapsulation Technology, Nanosomes, Intelligent Nanoparticles Drop Anti-aging Cargo, etc. This article also provides overview on different ant aging products of Salvona and Olay.

International Journal of Applied Pharmaceutics, Sep 8, 2018

Objective: The present study was aimed to develop a simple, sensitive and precise high performanc... more Objective: The present study was aimed to develop a simple, sensitive and precise high performance liquid chromatographic (HPLC) method for the simultaneous estimation of curcumin and piperine and to implement the developed method for the estimation of curcumin and piperine in the nanoparticulate formulation. Methods: Method development was performed using various solvent, buffer-solvent ratios, at different flow rates for adequate separation of both drugs. The developed method was validated in accordance with the international conference on harmonization (ICH) guidelines. The developed method was implemented to estimate the amount of curcumin and piperine in the nanoparticulate formulation. Results: Chromatographical conditions were optimized, and the best chromatographical conditions with adequate resolution for curcumin and piperine was achieved using enable C18G reverse phase column, using a mobile phase combination of acetonitrile and phosphate buffer (pH 3)in a ratio of 70:30 v/v at a flow rate of 1.0 ml/min. The detection was monitored at a wavelength of 360 nm. The retention time of curcumin and piperine was found to be 7.2 min and 8.5 min respectively. Conclusion: The developed analytical method is simple, precise, and reproducible and thus can be used for simultaneous estimation of curcumin and piperine in pharmaceutical formulations.

Archives of Pharmacal Research, Mar 1, 2010

Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-... more Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-benzamide, a non-selective alpha, beta-adrenoceptor antagonist is used in the treatment of hypertension. It shows variable bioavailability ranging from 10-80% which may be attributed to its minimum solubility in pH range 6 to 10, the pH conditions prevailing at the major site of absorption i.e. small intestine. Also due to its half life of 3 to 6 hrs it is administered twice daily. In the present work non-effervescent sustained release gastroretentive floating tablets of labetalol hydrochloride have been developed using various grades of HPMC and Poloxamer M127 as wetting agent. The tablets were evaluated for in vitro drug release, floating time, floating lag time, swelling studies etc. The tablets formulated with HPMC K4M CR and HPMC K15M CR along with Poloxamer showed negligible floating lag time with a total floating time over 12 hrs with complete release. Formulation was optimized using Stat-Ease Design Expert 7.1 software. Optimized batch was evaluated for the effect of change of osmolarity and pH on drug release, floating and swelling behaviour.

Current Drug Therapy, Nov 1, 2011

International Journal of Pharmacy and Pharmaceutical Sciences, Dec 1, 2016

Objective: The present study was aimed to develop a rapid, accurate, linear, sensitive and stabil... more Objective: The present study was aimed to develop a rapid, accurate, linear, sensitive and stability-indicating high performance liquid chromatographic method for determination of curcumin and to implement the developed method for the estimation of curcumin in the nanoparticulate formulation. Methods: Method development was performed using various solvent, buffer-solvent ratios, at different flow rates for better resolution and to decrease the run time. The developed method was validated in accordance with the international conference on harmonization (ICH) guidelines. The developed method was implemented to estimate the amount of curcumin in the curcumin-nanoparticulate formulation. Results: The optimum chromatographic conditions with adequate resolution for curcumin (16.10 min) was achieved when the separation was carried using C18 Conclusion: The developed analytical method is simple, precise, and reproducible and thus can be used for stability-indicating analysis of curcumin in pharmaceutical formulations. column at ambient temperature with an isocratic elution mode of mobile phase composed of a degassed mixture of phosphate buffer pH 3 and acetonitrile (50:50 v/v) at 1.0 ml/min flow rate with a total run time of 20 min. The developed method was validated for system suitability, accuracy, precision, limit of detection (LOD), limit of quantitation (LOQ), linearity and range. The LOD and LOQ were found to be 0.018 and 0.056 μg/ml respectively, which indicates that the method was sensitive, and can detect and quantify at lower levels of curcumin. Linearity range was from 5-15 μg/ml for curcumin with regression coefficient 0.997 indicates that at this concentration range curcumin was highly linear. Percent assay of curcumin was found to be 98.7% and curcumin recovered was found to be 0.78 mg which are estimated by using the developed method.

Journal of Inclusion Phenomena and Macrocyclic Chemistry, Aug 25, 2009

... Ren et al. have filed a patent for the V. Mohit Á G. Harshal Á D. Neha Á K. Vilasrao Á H. Raj... more ... Ren et al. have filed a patent for the V. Mohit Á G. Harshal Á D. Neha Á K. Vilasrao Á H. Rajashree (&) Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, CBD Belapur, Sector-8, Navi Mumbai 400614, India e-mail: rshirlekar@rediffmail.com 123 ...

Carvedilol is an antihypertensive drug used in the treatment of congestive heart failure, cardiac... more Carvedilol is an antihypertensive drug used in the treatment of congestive heart failure, cardiac arrhythmias and angina pectoris. It exhibits poor bioavailability of 25-30% which is attributed to its poor solubility and high first pass metabolism. The present work was aimed at overcoming these two limitations. Drug-Methyl-β-cyclodextrin complex was prepared by kneading method and characterized by Fourier Transformation Infrared spectroscopy, Differential Scanning Calorimetry and powder X-Ray Diffractometry studies. Dissolution rate of complex was compared with plain drug and physical mixture. The complex was incorporated into buccal tablet. The buccal tablets were evaluated for drug release, mucoadhesive strength and ex-vivo permeability. Characterization of binary system revealed the formation of inclusion complex of drug with Methyl-β-cyclodextrin. The complex showed complete release as compared to 32.8% and 42.7% from plain drug and physical mixture respectively in 60min. Tablets containing complex showed complete release at the end of 180min compared to 40.23% from tablets containing plain drug. The buccal tablets containing complex had good mucoadhesive strength. The amount of drug permeated from these tablets across the porcine buccal mucosa at the end of 5h was 6.2mg as compared to 2.51mg from tablets containing plain drug. Thus it can be concluded that buccal tablet containing complexed CAR would have improvement in bioavailability.

Even though oral route is the most preferred one, certain conditions necessitate the use of paren... more Even though oral route is the most preferred one, certain conditions necessitate the use of parenteral dosage form. But this route being invasive, is considered as non-patient compliant. Thus, there came a need for a more patient compliant system which led to the development of needleless injection technology. This review intends to throw light on the basic mechanisms by which this technology works, its applications and thereby also discusses the scope it has for the delivery of many new upcoming drugs.

Current Drug Delivery, Dec 1, 2010

ABSTRACT Atherosclerosis is the primary cause of coronary heart disease, which is characterized b... more ABSTRACT Atherosclerosis is the primary cause of coronary heart disease, which is characterized by a narrowing (stenosis) of the arteries that supply blood to tissues of the heart. Over the past decade, the use of &amp;quot;Bare metallic stents&amp;quot; during Percutaneous Transluminal Coronary Angioplasty (PTCA) has become a common practice for treating the coronary arterial stenosis. However, the restenosis is common problem in patients receiving stents. Recently, Drug-Eluting Stents (DES) with synthetic polymer coatings which act as drug reservoirs and elute drugs over a period of several weeks or months have emerged to tackle restenosis. The polymer coatings on these stents contain various drugs like immunosuppressive drugs, anti-neoplastic drugs, anti-inflammatory drugs, migration inhibitor drugs and enhanced healing drugs that inhibit thrombus formation, inflammation or cellular proliferation which in turn prevent restenosis. Different methods like dip coating, dip spin coating, ultrasonic spray coating and ink-jet coating help to coat stent uniformly. Drug from the stent can be released by diffusion, dissolution or ion exchange mechanism. There are some disadvantages of the polymer coated stents and hence they are being superseded by completely bioabsorbable stents. Such stents are heading for clinical trials and may hit the market soon. This review gives a glimpse over DES and the future prospects of DES.

Current Drug Therapy, 2018

Brain targeting has always been challenging due to the presence of various physiological barriers... more Brain targeting has always been challenging due to the presence of various physiological barriers resulting in low bioavailability via the oral and parenteral route. Altering the integrity of these barriers so as to permit the drugs to enter into the brain could severely damage the Central Nervous System by also allowing the entrance of toxic substances, bacteria and viruses into the brain. This problem can be tackled by delivering drugs via the intranasal route which bypasses the blood brain barrier and reaches different parts of the brain primarily via the olfactory and trigeminal neural pathways. This route offers several advantages over the oral and parenteral route and has shown potential for targeting drugs to the brain for treating various central nervous system disorders such as Psychosis, Parkinson's and Alzheimer's disease. In spite of several advantages, the intranasal route faces many challenges. Hence, a complete understanding of every aspect related to nose to brain delivery is of utmost importance. This article reviews the mechanism of nose to brain drug transport, challenges and approaches for nose to brain drug delivery, a few specialized olfactory delivery devices and some applications of this novel route of brain targeting.

Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2009

In this work, we illustrate the usefulness of cyclodextrins, namely, methyl-β-cyclodextrin (MβCD)... more In this work, we illustrate the usefulness of cyclodextrins, namely, methyl-β-cyclodextrin (MβCD), an amorphous, methylated derivative of the natural β-cyclodextrin, as a tool to form an inclusion complex with Valsartan (VAL), a poorly water soluble drug. The phase solubility study showed AL type of curve with slope less than one indicating the formation of complexes in 1:1 molar ratio of

Journal of Inclusion Phenomena and Macrocyclic Chemistry, Nov 20, 2010

Abstract The aim of this study was to investigate the effect of hydroxypropyl-b-cyclodextrin (HPb... more Abstract The aim of this study was to investigate the effect of hydroxypropyl-b-cyclodextrin (HPbCD) on the solubility and dissolution rate of Cefdinir (CEF). The methods that were employed to prepare CEFHPbCD complexes were Kneading (KN), Co-evaporation (CE), Spray ...

Current Drug Delivery, 2008

Background: The present work focuses on the development of ultra-small solid lipid nanoparticles ... more Background: The present work focuses on the development of ultra-small solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) encapsulating cyclosporine and calcipotriol, further incorporated into gel, increasing their penetration through the skin. Research Design and Methods: Developed SLN and NLC were characterized regarding particle size, zeta potential, %entrapment efficiency and dispersed into carbopol 934P-NF gel. Gel was further characterized for rheological behavior and spreadability. Ex vivo dermatokinetic by tape stripping method, in vitro efficacy on HaCaT cell lines and in vivo efficacy on imiquimod induced psoriatic model in mice were evaluated. Results: Ultra-small (size<100nm) particles were formed with high entrapment efficiency and spherical morphology. Ex vivo dermatokinetic studies revealed deeper and confined drug penetration of lipid formulation gel in epidermal layers as compared to free drug. In vitro study on HaCaT cell lines depicted higher uptake and high efficacy owing to decrease in cell viability for NLC. The anti-psoriatic efficacy in BALB/c mice (evaluated on basis of cytokine levels and skin morphology) highlighted potential of drug-loaded NLC significantly higher as compared to drug loaded SLN and marketed formulation Betagel. Conclusions: The study demonstrated that NLC gel had higher efficacy in psoriatic management and hold promise for further exploration.

Journal of Applied Pharmaceutical Science

The purpose of the research was to develop ultraviolet (UV) spectroscopic methods to simultaneous... more The purpose of the research was to develop ultraviolet (UV) spectroscopic methods to simultaneously estimate curcumin (CUR) and piperine (PIP). This method involves interpreting simultaneous equations using UV visible spectrophotometer with 1 cm matched quartz cells and methanol as a solvent based on measuring absorbance at two wavelengths of 423 and 342 nm. The method developed obeyed the law of Beer-Lambert in the concentration range of 1-7 μg/ml, with the correlation coefficient for CUR and PIP at their respective maximum wavelengths being 0.9990 and 0.9988, respectively. At an iso-absorptive point, CUR and PIP in the concentration range of 1-7 μg/ml showed a correlation coefficient of 0.9995 and 0.9988, respectively. Various validation parameters, such as precision (intraday and interday studies), limit of detection, and limit of quantitation, have been tested and found to be within the limit. The results of the method have been statistically validated. For the simultaneous estimation of CUR and PIP, a novel, simple, sensitive, fast, accurate, and economical spectrophotometric method has been developed. The method can be used to estimate the amount of CUR and PIP in a nanoparticulate system containing CUR and PIP.

International Journal of Current Pharmaceutical Research, 2022

Objective: The present study was aimed at preparing stable lyophilized curcumin loaded nanostruct... more Objective: The present study was aimed at preparing stable lyophilized curcumin loaded nanostructured lipid carriers (NLCs). The optimized lyophilized curcumin loaded NLCs were characterized and evaluated for various quality control parameters. Methods: The optimized curcumin loaded NLCs were prepared by modified hot emulsification using precirol ATO 5 (PRE), capmul MCM C8 EP (CAP) as solid and liquid lipids, respectively. The combination of tween 80 (T80) and solutol HS 15 (SHS) were used as an emulsifier. The NLCs dispersion was lyophilized into powder form to improve the thermodynamic stability of the formulation. The lyophilized curcumin loaded NLCs were evaluated for particle size, size distribution, zeta potential, entrapment efficiency (EE), drug loading, assay, in vitro drug release, crystallinity and surface morphology studies. Results: The optimized lyophilized curcumin loaded NLCs have a mean particle size of 286.2±11.5 nm with a size distribution of 0.288±0.011, a zeta p...

Polymers are an important formulation consideration for Gastroretentive Drug Delivery System (GRD... more Polymers are an important formulation consideration for Gastroretentive Drug Delivery System (GRDDS) as the polymers play an important role in allowing the dosage form to remain in gastrointestinal tract for a longer time thus enabling the required quantity of drug to be released and absorbed into the body. The objective of this study was to compare swelling, water uptake [1] and water holding capacity of commonly used grades of Hypromellose (Hydroxypropylmethyl cellulose) for their potential application as polymer for GRDDS. The study found that K100M grade of Hypromellose provided the best results which could facilitate its use as polymer in GRDDS.

Journal of Drug Delivery and Therapeutics, 2019

Objective: The aim of this study was to develop the diallyl disulphide (DADS) liposomal dispersio... more Objective: The aim of this study was to develop the diallyl disulphide (DADS) liposomal dispersion and further the dispersion was to formulate into gel. Methods: The DADS liposomal system was developed using thin film hydration method. 32 factorial design was employed to study the effect of various factors to obtain the optimized liposomal system. Further, it was converted to gel using suitable gelling agent. The optimized liposomal system and gel formulations were evaluated for various parameters. The optimized gel was evaluated for its in-vitro antifungal efficacy. The stability studies for gel were carried as per International conference on harmonisation (ICH) guidelines. Results: The optimized liposomal system was having vesicle size of 208.6nm, % entrapment was 91.7±1.16% and loading was 11.12±0.23%. % drug permeation was 61.10±0.85%. The zeta potential showed moderate stability. The optimized DADS liposomal gel showed satisfactory results. Ex-vivo permeation studies showed tha...