Shagufta Khan - Academia.edu (original) (raw)

Papers by Shagufta Khan

BioMed Research International

The goal of this study was to use polymeric konjac glucomannan (KGM), Kollidon VA 64 (KVA64), and... more The goal of this study was to use polymeric konjac glucomannan (KGM), Kollidon VA 64 (KVA64), and glutaraldehyde to ameliorate stomach specific floating microspheres (SSFM) using domperidone (DoN) to increase in vivo bioavailability and emerging health pathologies. The SSFM were made using the emulsion cross-linking process, and the polymer was chosen based on its ability to get cross-linked. The thermodynamic parameters were used to determine the AL classes of phase solubility curves using ideal complexes produced with KVA64. The optimal interaction constants at 25 and 37°C were found to be 116.14 and 128.05 M-1, respectively. The prepared SSFM had an average particle size (PS) of 163.71 ± 2.26 mm and a drug content of 96.66 ± 0.32 %. It can be determined from in vitro drug release experiments that drug release is good in terms of regulated drug release after 12 h ( 92.62 ± 2.43 %). The SSFMs were approximately sphere-shaped and had smooth surfaces, according to the morphological ...

Turkish Journal of Pharmaceutical Sciences, Jan 21, 2020

INTRODUCTION: In the current investigation a novel sterculia foetida and pullulan based semiinter... more INTRODUCTION: In the current investigation a novel sterculia foetida and pullulan based semiinterpenetrating polymer network gastroretentive microsphere formulation was prepared by emulsion crosslinking method and optimized by central composite design. METHODS: The effect of amount of glutraldehyde, sterculia foetida and pullulan on percent drug entrapment efficiency (% EE), percent mucoadhesion at 12h and percent in vitro drug release at 12h (% Q12h) were optimized. The microspheres were also characterized by SEM, FTIR and DSC. RESULTS: The formulation containing 4%v/v Glutraldehyde, 8.28%w/v pullulan and 2.14% w/v sterculia foetida had 88.75± 1.18% EF, gave 80.43± 1.2% drug release in 12 h and 81.73± 1.50% mucoadhesion at 12 h was considered optimum and was used for in-vivo radiographic study. DISCUSSION AND CONCLUSION: From the study it was concluded that semiinterpenetrating polymer network microspheres loaded with amoxicillin trihydrate were successfully prepared using Sterculia foetida and pullulan gum. The prolong retention of microspheres in the stomach with sustained drug release could effectively act against the H-Pyroli reservoir in the stomach and improve the therapeutic effectiveness of amoxicillin trihydrate against H-Pyroli.

Artificial Cells, Nanomedicine, and Biotechnology, 2017

Incompetence of antiretrovirals (ARV) in complete eradication of HIV from the CNS is the biggest ... more Incompetence of antiretrovirals (ARV) in complete eradication of HIV from the CNS is the biggest issue in neuro-AIDS treatment. The ineffectiveness is largely due to the poor penetration of ARV. Hence, the present study is attempted to enhance the CNS uptake of efavirenz (EFV) by designing intranasal EFV nanoparticles (EFV-NPs). EFV-NPs were fabricated using chitosan-g-HPbCD by ionic gelation method and optimized using quadratic response surface methodology (RSM) employing two-factor, five-level circumscribed central composite design. NPs containing drug: polymer ratio (1.25:0.79) were spherical with 198 ± 4.4 nm size, 23.28 ± 1.5% drug loading and 38 ± 1.43% entrapment efficiency. NPs showed sustained drug release (99.03 ± 0.30% in 8 h) and followed Fickian diffusion mechanism. It gave 4.76 times greater permeability than plain drug solution through porcine nasal mucosa. Enhanced CNS bioavailability (12.40-fold that of i.v solution) of EFV, high drug-targeting percentage (99.24%) and drug-targeting index (141.3) post-intranasal administration of NPs was observed. These results are corroborated by gamma scintigraphy images, which revealed high CNS uptake. NPs appeared histocompatible with porcine nasal mucosa and non-toxic to L929 cell line. Thus, CS-g-HPbCD served as a potential carrier in developing intranasal mucoadhesive EFV-NPs for the CNS targeting.

Indian Journal of Pharmaceutical Sciences, May 1, 2005

Recent scientific and patent literature shows increased interest in academics and industrial rese... more Recent scientific and patent literature shows increased interest in academics and industrial research groups regarding the novel dosage forms that can be retained in the stomach for a prolonged and predictable period of time. One of the most feasible approaches for achieving a prolonged and predictable dug delivery profiles in the gastrointestinal tract is to control the gastric residence time, using gastroretentive dosage forms that will provide us with new and important therapeutic options. From the formulation and technological point of view, the floating drug delivery system is considerably easy and logical approach. An attempt has been made in this review article to introduce the readers to the current technological developments in floating drug delivery system.

The aim of the present research was to study the effects of weak cation exchange resins, polacril... more The aim of the present research was to study the effects of weak cation exchange resins, polacrilex with exchangeable H + and polacrillin potassium and strong cation exchange resin sodium polystyrene sulfonate on water uptake behavior of ranitidine hydrochloride. Drug resin complexes (DRC) were prepared and evaluated for the percentage of moisture gain when placed in a humidity chamber at 40E2 °C and 75E5% RH for 17 h as compared to drug and free resins under the same condition. Equilibrium moisture content (EMC) under different humidity conditions and the rate and extent of moisture uptake in the presence (15 watt florescence light) and absence of light under 40E2 °C and 75E5% RH were also calculated for DRCs, drug and unloaded resins. DRC 264 (containing polacrilex with H +) gained minimum weight (10.22%) maintaining free flowing characteristics whereas other resinates showed higher weight gain and formation of sticky mass while ranitidine HCl turned liquid with gain of 28.11% wei...

PDA journal of pharmaceutical science and technology / PDA

This investigation examined the effect of a ranitidine hydrocholoride (RHCl)-ion exchange resin c... more This investigation examined the effect of a ranitidine hydrocholoride (RHCl)-ion exchange resin complexation on the drug's moisture uptake behavior. Drug resin complexes (DRCs) were prepared using the batch method with (i) two weak cation exchange resins, Polacrilex with exchangeable H+ and Polacrillin potassium; and (ii) a strong cation exchange resin;Sodium polystyrene sulfonate. RHCl, simple resins, and DRCs were subjected to storage stability under 40 +/- 2 degrees C and 75 +/- 5% relative humidity (RH) for 16 h, and the resulting percent increase in weight was calculated. DRCs gained less moisture than the simple drug and free resins. Out of the three complexes tested, DRC containing Polacrilex resin showed the most promising effect in protecting RHCl against moisture uptake with an increase in weight of 10.22 +/- 17% (free RHCl gained 28.11%) and was thereby selected for tablet formulation. Tablets were prepared using simple RHCl with Starch 1500 (F1); low moisture-grade S...

Die Pharmazie, 2008

Oral administration is unsuitable for drugs prone to extensive first-pass metabolism, like buspir... more Oral administration is unsuitable for drugs prone to extensive first-pass metabolism, like buspirone. Thus, in the present study an attempt has been made to develop a mucoadhesive intranasal formulation improving permeation characteristics of buspirone HCl. Nasal formulations containing different concentrations of chitosan HCl and hydroxypropyl-beta-cyclodextrins (HP-beta-CD) were prepared and compared with control buspirone HCl solution regarding permeability, in vitro duration of mucoadhesion, in vivo nasal clearance in rats and in vitro cytotoxicity on cell culture. Nearly two fold increase in buspirone permeation was observed with 1% chitosan HCl and a 3.5 fold increase with 1% chitosan HCI and 5% HP-beta-CD. Nasal clearance studies showed retention of 50% radioactivity up to about 3.5 h for formulation F7 containing 1% chitosan HCI compared to 1.5 h for control buspirone solution (F1). Results conclusively demonstrated enhancement in permeation with no cytotoxicity. Thus formul...

Journal of Pharmaceutical Investigation, 2014

Natural polysaccharides are widely used for development of colon-specific drug delivery systems. ... more Natural polysaccharides are widely used for development of colon-specific drug delivery systems. The present study was carried out to develop multi-particulate calcium pectinate (Ca-pectinate) formulations for colon-targeted delivery of lornoxicam. The formulations were developed using a combination of polycarbophil and low-methoxy amidated pectin. The beads were prepared using an ionotropic gelation technique. The effects of the polycarbophil and low-methoxy amidated pectin concentrations on the beads characteristics, encapsulation efficiency, swelling study and drug release performance were investigated. The optimized formulation was evaluated for its morphological characteristics. The in vitro drug release of the optimized formulation over a period of 12 h was 96.78 ± 1.35 %. The concentration of the polycarbophil was a decisive factor in sustaining drug release in the colon. The study revealed that optimized Ca-pectinate beads prepared with polycarbophil can efficiently encapsulate lornoxicam. It also showed that these beads can potentially be used for colon-specific delivery of lornoxicam.

Journal of Materials Science: Materials in Medicine, 2013

The objective of this study was to develop submicron carriers of two drugs that are practically i... more The objective of this study was to develop submicron carriers of two drugs that are practically insoluble in water, i.e. meloxicam and aceclofenac, to improve their dissolution behavior. The phase solubility of the drugs was studied using different concentrations of sparingly methylated β-cyclodextrin, Kleptose(®) Crysmeβ (Crysmeb), in the presence and absence of 0.2 % w/v water-soluble chitosan. Drug-loaded submicron particles (SMPs) were prepared using chitosan chlorhydrate and Crysmeb by the ionotropic gelation method. The SMPs were characterized in terms of powder X-ray diffraction, Fourier transforms infrared spectroscopy, size determination, process yield, drug loading, encapsulation efficiency, surface morphology and in vitro release. The drug loading in the SMPs was enhanced in the presence of Crysmeb. The in vitro drug release was found to be enhanced with SMPs prepared using higher concentrations of Crysmeb. These results indicate that SMPs formed from chitosan chlorhydrate and Crysmeb are promising submicron carriers for enhancing the dissolution of meloxicam and aceclofenac.

Journal of Drug Targeting, 2010

Journal of drug …, 2010

Mucoadhesive temperature-mediated in situ gel formulations using chitosan and hydroxyl propyl met... more Mucoadhesive temperature-mediated in situ gel formulations using chitosan and hydroxyl propyl methyl cellulose were used to enhance intranasal (i.n.) delivery of the dopamine D2 agonist ropinirole to the brain. Formulations were tested for gelation time, thermosensitivity, mucoadhesion, in vitro release and permeation, in vitro cytotoxicity, nasal clearance, in vivo bioavailability and brain uptake. In vivo bioavailability and brain uptake of ropinirole were assessed in albino rats following intranasal administration of 99mTc-ropinirole in situ gel, intranasal ropinirole solution and intravenous (i.v.) ropinirole solution. Radiolabeled ropinirole uptake was calculated as a fraction of administered dose. The absolute bioavailabilty of ropinirole from the temperature-mediated in situ gelling nasal formulation was 82%. The AUC (0-480 min) in brain after nasal administration of ropinirole in situ gel was 8.5 times (869 +/- 250% x min/g versus 102 +/- 20% x min/g) that obtained following i.v. administration, this value was also considerably higher (869 +/- 250% x min/g versus 281 +/- 52% x min/g) than that achieved with intranasal ropinirole solution. High brain direct drug transport percentage (DTP; 90.36%) and drug targeting index (DTI) &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;gt; 1 confirms direct nose to brain transport of the intranasal in situ gel formulation of ropinirole.

AAPS PharmSciTech, 2007

The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to for... more The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to formulate a rapiddisintegrating tablet (RDT) of the taste-masked drug. Taste masking was done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios by the precipitation method. Drug-polymer complexes (DPCs) were tested for drug content, in vitro taste in simulated salivary fluid (SSF) of pH 6.2, and molecular property. Complex that did not release drug in SSF was considered taste-masked and selected for formulation RDTs. The complex with drug-polymer ratio of 8:2 did not show drug release in SSF; therefore, it was selected. The properties of tablets such as tensile strength, wetting time, water absorption ratio, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch F4 containing spray-dried mannitol and microcrystalline cellulose in the ratio 1:1 and 7% wt/wt Polyplasdone XL-10 showed faster disintegration, within 12.5 seconds, than the marketed tablet (112 seconds). Good correlation between in vitro disintegration behavior and in the oral cavity was recognized. Taste evaluation of RDT in human volunteers revealed considerable taste masking with the degree of bitterness below threshold value (0.5) ultimately reaching to 0 within 15 minutes, whereas ondansetron HCl was rated intensely bitter with a score of 3 for 10 minutes. Tablets of batch F4 also revealed rapid drug release (t 90 , 60 seconds) in SGF compared with marketed formulation (t 90 , 240 seconds; P G .01). Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets in the oral cavity.

Journal of Pharmacy and …, 2009

Objectives The purpose of this study was to find out whether nasal application of buspirone could... more Objectives The purpose of this study was to find out whether nasal application of buspirone could increase its bioavailability and directly transport the drug from nose to brain. Methods A nasal formulation (Bus-chitosan) was prepared by dissolving 15.5 mg buspirone hydrochloride, 1% w/v chitosan hydrochloride and 5% w/v hydroxypropyl b-cyclodextrin (HP-b-CD) in 5 ml of 0.5% sodium chloride solution. The formulation was nasally administered to rats and the plasma and brain concentration compared with that for buspirone hydrochloride solution after intravenous and intranasal (Bus-plain) administration. The brain drug uptake was also confirmed by gamma scintigraphic study. Key findings The nasal Bus-chitosan formulation improved the absolute bioavailability to 61% and the plasma concentration peaked at 30 min whereas the peak for nasal Bus-plain formulation was 60 min. The AUC 0-480 in brain after nasal administration of Bus-chitosan formulation was 2.5 times that obtained by intravenous administration (711 252 ng/g vs 282 110 ng/g); this was also considerably higher than that obtained with the intranasal Bus-plain formulation (354 80 ng/g). The high percentage of direct drug transport to the brain (75.77%) and high drug targeting index (>1) confirmed the direct nose to brain transport of buspirone following nasal administration of Bus-chitosan formulation. Conclusions These results conclusively demonstrate increased access of buspirone to the blood and brain from intranasal solution formulated with chitosan and HP-b-CD.