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Dhankar V.,Spectrum Institute of Pharmaceutical science and Research | Garg G.,Meerut Institute of Engineering and Technology | Awasthi R.,Laureate Institute of Pharmacy
Polimery w medycynie | Year: 2014

Mucoadhesion enables localization of drugs to a defined region of the gastrointestinal tract through attractive interactions between polymers composing the drug delivery devices and the mucin layer of the intestinal epithelium. Thus, this approach can be used for enhancement of the oral bioavailability of the drug. The current communication deals with the development of ranitidine hydrochloride-loaded chitosan-based mucoadhesive microspheres. Microspheres were prepared by water-in-oil emulsion technique, using glutaraldehyde as a cross-linking agent. The effect of independent variables like stirring speed and polymer-to-drug ratio on dependent variables, i.e. percentage mucoadhesion, percentage drug loading, particle size and swelling index, was examined using a 3(2); factorial design. The microspheres were discrete, spherical, free-flowing and also showed high percentage drug entrapment efficiency (43-70%). An in vitro mucoadhesion test showed that the microspheres adhered strongly to the mucous layer for an extended period of time. The RC 4 batch exhibited a high percentage of drug encapsulation (70%) and mucoadhesion (75%). The drug release was sustained for more than 12 h. The drug release kinetics were found to follow Peppas' kinetics for all the formulations and the drug release was diffusion controlled. The preliminary results of this study suggest that the developed microspheres containing ranitidine hydrochloride could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.


Monga V.,Rajendra Institute of Technology and science | Goyal K.,Laureate Institute of Pharmacy | Steindel M.,Federal University of Santa Catarina | Rajani D.P.,Microcare Laboratory | Rajani S.D.,Microcare Laboratory
Medicinal Chemistry Research | Year: 2014

A series of chalcones (1-8) were prepared by Claisen-Schmidt condensation of 3-nitroacetophenone with various aldehydes. These chalcones on cyclization with hydrazine hydrate in the presence of glacial acetic acid, hydrazine hydrate in absolute ethanol and ethyl acetoacetate in the presence of barium hydroxide gave corresponding N-acetyl pyrazolines (9-16 ), N-unsubstituted pyrazolines (17-19) and cyclohexenone derivatives (20-22). All the synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity by using broth microdilution method, and many compounds showed promising activity against various tested bacteria and fungi. Among various tested compounds, 16 and 19 exhibited strongest activities against Streptococcus pyogenes and Pseudomonas aeruginosa; both have MIC value of 25 μg/mL, which is fourfold greater than the standard drug. Many compounds showed good activity against Candida albican. Analogs 11, 12, 15-17 and 19 displayed two- to fivefold greater activity against C. albican as compared to the standard drug. Results of antitubercular evaluation revealed that compounds 4 and 19 displayed strong antimycobacterial activity against H 37Rv having MIC of 25 and 62.5 lg/mL, respectively. All analogs were found to be inactive against Leishmania braziliensis except analogs 4 and 5 which exhibited strong leishmanicidal activity against Leishmania promastigotes with IC50 values of 9.3 and 8.9 μg/mL, respectively. © Springer Science+Business Media 2013.


PubMed | Amity University, University of Newcastle, Laureate Institute of Pharmacy and University of Sao Paulo
Type: Journal Article | Journal: Drug delivery and translational research | Year: 2016

The present study aimed to develop matrix-type transdermal drug delivery system (TDDS) of metoprolol tartrate using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA). The transdermal films were evaluated for physical parameters, Fourier transform infrared spectroscopy analysis (FTIR), differential scanning calorimetry (DSC), in vitro drug release, in vitro skin permeability, skin irritation test and stability studies. The films were found to be tough, non-sticky, easily moldable and possess good tensile strength. As the concentration of PVA was increased, the tensile strength of the films was also increased. Results of FTIR spectroscopy and DSC revealed the absence of any drug-polymer interactions. In vitro release of metoprolol followed zero-order kinetics and the mechanism of release was found to be diffusion rate controlled. In vitro release studies of metoprolol using Keshary-Chein (vertical diffusion cell) indicated 65.5% drug was released in 24h. In vitro skin permeation of metoprolol transdermal films showed 58.13% of the drug was released after 24h. In vitro skin permeation of metoprolol followed zero-order kinetics in selected formulations. The mechanism of release was found to be diffusion rate controlled. In a 22-day skin irritation test, tested formulation of transdermal films did not exhibit any allergic reactions, inflammation, or contact dermatitis. The transdermal films showed good stability in the 180-day stability study. It can be concluded that the TDDS of MPT can help in bypassing the first-pass effect and will provide patient improved compliance, without sacrificing the therapeutic advantages of the drugs.


Kumar S.,Laureate Institute of Pharmacy | Awasthi R.,Laureate Institute of Pharmacy
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry | Year: 2015

The aim of this study was to develop and characterize montelukast sodium loaded niosomal drug carrier systems. The vesicles were prepared by film hydration technique using different surfactants. The optimized formulation was selected on the basis of results obtained from drug entrapment, morphology and in vitro drug release studies, and further evaluated for possible drug-excipient interaction, thermal behavior and drug physical state, before and after formulation using Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction analysis methods, respectively. The morphological characterization of vesicles was done using Transmission electron microscopy. Energy-dispersive X-ray spectroscopy system was used for elemental and dimensional analysis of developed vesicles. The vesicle surface charge was determined using zeta potential measurements. The results suggested that the optimized formulation had small size (103±6.01 nm) and high drug entrapment (72.20±2.10%). No chemical interaction was observed between the drug and excipients. The study revealed that Span 60 is a good nonionic surfactant for vesicle formulation. After 3 months storage at 2-8°C, the optimized formulation preserved stability in terms of formulation colour, drug amount and percent drug release. After 3 months, flocculation occured and hard cake was not formed on the settlement of vesicles. The preliminary results of this study suggest that the designed vesicles could enhance drug entrapment, reduce the initial burst release of drug and modulate the drug release. © 2015 Bentham Science Publishers.


Srivastav P.,Laureate Institute of Pharmacy
Current drug delivery | Year: 2014

The purpose of this study was to prepare and characterize levocetirizine hydrochloride loaded liposome of by film hydration technique followed by sonication. Sorbitol was added to facilitate the hydration of dried liposome into vesicles or to prepare rehydration system. The liposomes were characterized for size, shape, entrapment efficiency, in vitro drug release and stability. The morphology of liposomes was characterized through a phase-contrast microscope and transmission electron microscope. The percent entrapment efficiency and particle size varied between 55.6 ± 0.21 to 81.2 ± 0.52 and 15.73 ± 0.99 to 24.52 ± 0.97 μm, respectively. The drug release increased at higher concentration of phospholipids. On the other hand, the drug release was decreased at higher concentration of cholesterol. The preliminary results of this study suggest that the developed multi-lamellar vesicles containing levocetirizine hydrochloride could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.


Sharma N.,Jawaharlal Nehru University | Sharma N.,Crossing tech | Kulkarni G.T.,Laureate Institute of Pharmacy | Sharma A.,Crossing tech
Tropical Journal of Pharmaceutical Research | Year: 2013

Purpose: To develop a safe mucoadhesive gel for nasal drug delivery using okra polysaccharide. Methods: Rizatriptan benzoate nasal gel was developed using natural polysaccharide obtained from the Abelmoschus esculentus. The gel formulation was characterized for pH, viscosity, mucoadhesion, and in vitro permeation. Permeation parameters obtained include drug flux (j), permeation coefficient (kP) and lag time (tL). The effect of sodium thioglycollate and sodium taurocholate on permeation of the gel formulations was evaluated using excised goat nasal mucosa. Results: Okra gel formulation showed good properties in terms of pH, viscosity and mucoadhesion. The drug was able to permeate through the goat nasal mucosa within 255 min. The test okra nasal gel, with and without enhancer, showed superior permeation properties to gels prepared with synthetic polymers - hydroxylpropyl methylcellulose (HPMC) and sodium carboxymethyl cellulose (NaCMC). For example, drug flux (j) of okra nasal gel formulation and gel formulations made with HPMC and NaCMC was 134.8, 120.9 and 84.8, respectively. Conclusion: Okra mucilage is a promising natural and safe gel former that can be developed to serve as an alternative to currently used synthetic gel formers for nasal drug delivery. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved.


Agrawal S.,Crossing tech | Kulkarni G.T.,Laureate Institute of Pharmacy | Sharma V.N.,Crossing tech
Advances in Natural and Applied Sciences | Year: 2010

In this study, antioxidant activity of methanol extract of Acacia nilotica (AN) and Berberis chitria (BC) were evaluated using different in vitro methods. ABTS, DPPH, Nitric oxide, hydroxyl radical and hydrogen peroxide scavenging activities were used as standard methods of evaluation of antioxidant properties. Total phenolic content of the selected extracts was estimated by Folin-Ciocalteu method and correlated with antioxidant properties of the extracts. Butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), and Ascorbic acid (ASC) were used as the reference antioxidant compounds. Both the extracts were found to possess significant antioxidant property. Among the two, Acacia nioltica had higher antioxidant property than Berberis chitria. The antioxidant property was directly related to the total phenolic content of the extract, which was found to be 9.88 and 2.73 μg/ml, respectively for AN and BC. From the above studies it can be suggested that Acacia nilotica could be used as an antioxidant, probably for the treatment of diseases related to free radicals, such as, cancer, diabetes, etc. Further studies are needed on the isolation and identification of antioxidant compounds in AN to prove its worth as antioxidant drug. © 2010, American Eurasian Network for Scientific Information.


Kumar M.,Laureate Institute of Pharmacy | Awasthi R.,Laureate Institute of Pharmacy
Polimery w medycynie | Year: 2015

BACKGROUND: Crohn’s disease and ulcerative colitis are the main autoimmune inflammatory bowel diseases. Metronidazole is the most commonly used drug for the treatment of Crohn’s disease. However, the pharmacokinetic profile of this drug indicates that the largest amount of the drug is absorbed from the upper part of the intestines and very little concentration of the drugs reaches the colon.Objectives: The aim of this investigation was to formulate metronidazole loaded microspheres for the efficient therapy of inflammatory bowel diseases.Material and Methods: Microspheres were prepared using the emulsification-solvent evaporation method. The effect of Eudragit S100 concentration and the ratio of liquid paraffin (light: heavy) on percentage yield, particle size, morphology, drug encapsulation and in vitro drug release was examined. Drug-polymer interaction was investigated using Fourier Transformed Infrared Spectroscopy (FTIR).RESULTS: The results showed that the particle had good flow properties, encapsulation efficiency (56.11 ・} 1.51–81.02 ・} 2.14%)and cumulative drug release (64.14 ・} 0.83–79.69 ・} 2.45%) in a phosphate buffer (pH 6.8) after 10 h of the dissolution study.An increased particle size was observed with an increasing polymer concentration. It was observed that the Eudragit had a positive effect on the drug encapsulation and negative effect on drug release. Aggregation of drug-polymer droplets was observed at a lower level of magnesium stearate during microsphere preparation. The results of FTIR spectroscopy revealed the absence of any drug-polymer interactions. However, slight peak shifting and suppression in peak height was observed.This might be due to the minor ionic interactions. The microspheres were discrete, spherical and free-flowing. The spherical shape of the microspheres was confirmed from SEM photomicrographs. The developed microspheres showed a controlled drug release and were found to follow Higuchi’s model. The release mechanism of metronidazole from the microspheres was Fickian diffusion without swelling.CONCLUSIONS: The results suggest that the developed microspheres could enhance drug entrapment, and inflect the drug release.


PubMed | Laureate Institute of Pharmacy and Ram Eesh Institute of Vocational and Training Education
Type: Journal Article | Journal: Drug delivery and translational research | Year: 2016

The purpose of this investigation was to prepare and characterize acyclovir loaded floating microspheres by emulsification solvent evaporation method. Piperine was added to investigate its effect on acyclovir bioavailability. The microspheres were characterized for size, shape, entrapment efficiency, in vitro drug release, and in vivo pharmacokinetic parameters. The morphological characterization of microspheres was done using a scanning electron microscope. The microspheres were spherical and had particle size in the range of 400 to 525m. The percent drug entrapment efficiency varied between 56.121.32% to 87.325.28%. The drug release was decreased at higher polymer concentrations. Nearly two times higher AUC0-24 value of acyclovir-loaded piperine containing microspheres (15614.136953.13nghml(-1)) was observed as compared to the drug solution (7552.333219.09nghml(-1)). Under the accelerated storage conditions, the best selected formulation was found to be stable for 90days. The preliminary results of this study suggest that the developed microspheres containing acyclovir could enhance drug entrapment efficiency, reduce initial burst release, and prolong the drug release with enhanced bioavailability.


Awasthi R.,Jawaharlal Nehru University | Awasthi R.,Laureate Institute of Pharmacy | Kulkarni G.T.,Laureate Institute of Pharmacy
Drug Development and Industrial Pharmacy | Year: 2014

Aim: The current communication deals with the development of hollow floating beads of gliclazide. The primary effect of this drug is to potentiate glucose-stimulated insulin release from pancreatic islet-β-cells by induction of a decrease in potassium efflux from these cells. Because of the poor aqueous solubility, its absorption is limited. Thus, an attempt was made to improve its release profile. Methods: The hollow drug-loaded alginate beads in combination with low methoxyl pectin and hydroxypropylmethylcellulose (HPMC) were prepared by a simple ionotropic gelation method. The beads were evaluated for particle size and morphology using optical microscopy and scanning electron microscopy (SEM), respectively. Mucoadhesion test was done using goat stomach mucosal membrane. Release characteristics of the gliclazide-loaded hollow beads were studied in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 5.8). Results: The developed beads were spherical in shape with hollow internal structure and had a particle size in the range of 0.730 ± 0.05 to 0.890 ± 0.03 mm. The incorporation efficiency of alginate-pectin beads was higher than alginate-HPMC beads. The Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction analysis showed stable character of drug in the drug-loaded hollow beads and revealed the absence of any drug-polymer interactions. The beads remained buoyant for more than 12 h. The drug release from beads followed Fickian diffusion with swelling. Conclusion: The preliminary results of this study suggest that the developed beads containing gliclazide could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release. © 2014 Informa Healthcare USA, Inc.

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