Sustained Release Delivery of Repaglinide by Biodegradable Microspheres (original) (raw)
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Journal of Applied Polymer Science, 2010
The objective of the present work was to study the release behavior of plain and blend microspheres (MS) of PLGA and Pluronic F68/127. In this study, a novel blend MS of poly(D,L‐lactic‐co‐glycolic acid) (PLGA) and Pluronic F68/127 (PLF68/127) were prepared by the emulsion–solvent evaporation method. Repaglinide, an antidiabetic drug with a very short half‐life, was successfully encapsulated into the blend MS. Various formulations were prepared by varying the ratio of PLGA and PLF68/127. Drug encapsulation up to 91% was achieved as measured by UV spectroscopy. Scanning electron microscopy showed that MS have smooth surfaces even after incorporation of PLF68/127. Particle size, as measured by using laser light scattering technique, gave an average size ranging from 12 to 47 μm. Differential scanning calorimetry (DSC) was performed to understand the crystalline nature of the drug after encapsulation into MS. DSC revealed the crystalline dispersion in the polymer matrix. In vitro relea...
DESIGN AND CHARACTERIZATION OF POLYMERIC MICROSPHERES FOR ORAL ADMINISTRATION
An appropriately designed sustained or controlled release drug delivery system can be a major advance towards solving the problem associated with the existing drug delivery system. Microspheres as a novel drug delivery system for oral administration are having the feasibility of carrying the drug. These are the monolithic spheres or therapeutic agent distributed throughout the matrix as a molecular dispersion of particles. Rational behind the drug encapsulation into microspheres is preparation of suitable formulation with longer duration of action for control release thereby sustaining the role of release of core material by rupture of polymeric wall. This will also reduce the dosing frequency and helps to improve the patient compliance. The aim of present work was to produce and characterize Repaglinide (Rg) polymeric microspheres by solvent evaporation method, in an attempt to obtain a delivery system adequate for the treatment of diabetes. Batches were prepared with different ratios of drug and polymer. Polymeric microspheres of Repaglinide were successfully prepared using Eudragit RSPO as polymer by emulsion solvent evaporation method. The prepared microspheres were evaluated for percentage yield, particle size, and drug entrapment efficiency, scanning electron microscopy, micromeritic studies and in vitro drug release study. From all the evaluation parameters the batch which is considered to be optimized batch, the final formulation i.e. tablet were prepared from the microspheres prepared in that optimized batch.
International Journal of Research and Development in Pharmacy & Life Sciences
Objectives: To rationalize the use of surfactants by preparing Repaglinide Microspheres using two types of Surfactants, Tween 80 and Span 80 and study their effects on different characteristics of the microspheres. Methods: The microspheres were produced by emulsion solvent evaporation method, using the Eudragit RS100, Ethylcellulose, Tween 80 and Span80. Results and discussion: The microspheres were free flowing in nature. The surfactant concentration was found to be greatly affected the microspheres size distribution and dissolution. Scanning Electron Microscopy was done to study the surface morphology of the microspheres. Results have indicated that the incorporation of hydrophilic surfactant (Tween 80) gave larger microspheres, where as incorporation of the hydrophobic surfactant (Span 80) gave smaller microspheres and hydrophilic surfactant containing microspheres had higher drug release rate compared to hydrophobic surfactant containing microspheres. Conclusion: Microspheres containing repaglinide was prepared successfully by using an emulsion solvent evaporation technique.
During the study repaglinide encapsulated floating microspheres were formulated and characterized for enhancing residence time of drug in git and thereby increasing its bioavailability. Floating microspheres of Eudragit RL100 loaded with repaglinide were prepared by solvent evaporation technique. During process optimization various parameters were studied such as: concentration of polymer and concentration of emulsifier. Selected optimized formulation was studied for scanning electron microscope (SEM), entrapment, floating behaviour, drug release and kinetics. In-vivo floating ability (X-ray) study and in-vivo antidiabetic activity were performed on alloxan induced diabetic rats. Microspheres prepared with different concentrations of polymer were spherical shaped with smooth surface. Size of microspheres was in the range of 109.3-241.0 um. Good entrapment and buoyancy were observed for more than 12 hr. X-ray image showed that optimized formulation remained buoyant for more than 10 hr. Optimized formulation treated group shows significant (p < 0.01) reduction in blood glucose level as compared to pure drug treated group. Repaglinide loaded floating microspheres expected to give new choice for safe, economical and increased bioavailable formulation for effective management of diabetes mellitus.
Saudi Pharmaceutical Journal, 2015
During the study repaglinide encapsulated floating microspheres were formulated and characterized for enhancing residence time of drug in git and thereby increasing its bioavailability. Floating microspheres of ethylcellulose (EC) and hydroxypropyl methyl cellulose (HPMC) (5 and 100 cps) were prepared by emulsion solvent diffusion technique. During process optimization various parameters were studied such as: drug: polymer ratio, polymer ratio, concentration of emulsifier and stirring speed. Selected optimized formulations were studied for SEM, entrapment, floating behavior, drug release and kinetics. In-vivo floating ability (X-ray) study and in-vivo antidiabetic activity were performed on alloxan induced diabetic rats. Microspheres prepared with different viscosity grade HPMC were spherical shaped with smooth surface. Size of microspheres was in the range of 181.1-248 lm. Good entrapment and buoyancy were observed for 12 h. X-ray image showed that optimized formulation remained buoyant for more than 6 h. Optimized formulation treated group shows significant (p < 0.01) reduction in blood glucose level as compared to pure drug treated group. Repaglinide loaded floating microspheres expected to give new choice for safe, economical and increased bioavailable formulation for effective management of NIDDM.
2015
Irin Dewan *1, , Swarnali Islam Khandaker 2 and Md. Sohel Rana 1 Department of Pharmacy , Jahangirnagar University, Savar, Dhaka, Bangladesh Pharmaceutical Technology Research Laboratory , Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka-1209, Bangladesh ABSTRACT: Glibenclamide is an oral anti-hyperglycemic agent designed intended for the management of non-insulin-dependent diabetes mellitus (NIDDM). In certain conditions conventional drug release pattern is not suitable similar to Diabetes mellitus, cardiovascular diseases and many more diseases, this present study has taken a challenge to formulate controlled release microspheres by using different polymers. An effort has been given to prepare controlled release microspheres along with Ethyl cellulose, Eudragit RS/RL100 and Methocel K15, 100M by using non-aqueous emulsion solvent evaporation method. UV-Spectrophotometric was applied to assay the drug content and in vitro dissolution studies according to USP pad...
Journal of drug delivery, 2015
The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and er...
2016
Copyright © 2015 Irin Dewan et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The present study has been performed tomicroencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug.The attempt of this studywas to formulate and evaluate theVildagliptin loadedmicrospheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, andMethocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5 % and 68.5 % from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies hav...
Journal of Applied Polymer Science, 2007
In this study, hollow microspheres of cellulose acetate butyrate (CAB) and poly(ethylene oxide) (PEO) were prepared by emulsion-solvent evaporation method. Repaglinide was successfully encapsulated into floating microspheres. Various formulations were prepared by varying the ratio of CAB and PEO, drug loading and concentration of poly(vinyl alcohol) (PVA) solution. Encapsulation of the drug up to 95% was achieved. The microspheres tend to float over the simulated gastric media for more than 10 h. The micromeritic properties of microspheres reveal the excellent flow and good packing properties. The % buoyancy of microspheres was found to be up to 87. SEM showed that microspheres have many pores on their surfaces. Particle size ranges from 159 to 601 mm.
Formulation and Development of Novel Gastroretentive Microballoons of Repaglinide
Journal of Advanced Scientific Research, 2021
The present study involves preparation and evaluation of Microballoons of Repaglinide which is having poor solubility in water and low oral bioavailability. Repaglinide, an oral hypoglycemic agent, is rapidly absorbed and eliminated from the body after oral administration. The peak plasma level occurs within an hour of oral administration with elimination half life of 1 hr. The objective of the present work is to prepare floating microballoons of Repaglinide for delivering the drug in controlled manner which will help to reduce dosing frequency and maintain the plasma concentration of drug for longer time without fluctuations. This will be helpful in having better control over clinical maintenance of the type 2 diabetic condition. The Microballoons were prepared by solvent evaporation emulsification technique using Sodium Alginate as coating agent and Calcium Chloride as cross-linking agent. The formation of spherical and hollow Microballoons was confirmed by SEM studies ranging fro...