Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug.

Irin Dewan,Md Sohel Rana,Swarnali Islam

doi:10.1155/2015/496807

Irin Dewan, Md Sohel Rana + Show 1 more

Open Access

https://doi.org/10.1155/2015/496807

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Abstract

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 erosion as the correlation coefficient (R 2) best fitted with Korsmeyer model and release exponent (n) was 0.45–0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

Highlights

Vildagliptin is a potent, selective, and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor, which prevents inactivation of incretion hormones by inhibiting DPP-4
It has been shown to be an effective and safe option for better glycemic control in a wide range of T2DM patients and has demonstrated HbA1C lowering potential when given as monotherapy or in combination with other OADs, without weight gain and minimal hypoglycemia [1]
Meglitinides, and insulin are associated with weight gain and hypoglycemia; thiazolidinediones (TZDs) cause weight gain and possibly peripheral edema

Summary

Introduction

Vildagliptin is a potent, selective, and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor, which prevents inactivation of incretion hormones by inhibiting DPP-4. Meglitinides, and insulin are associated with weight gain and hypoglycemia; thiazolidinediones (TZDs) cause weight gain and possibly peripheral edema. Its biological half-life is 1 to 3 hrs as a consequence; it requires repeated administration to keep plasma concentration. This causes bother to the patient and leads to fluctuations in plasma drug concentration so that it might reduce the therapeutic effect. Advanced controlled release forms enhance patient compliance by reducing frequency of dosing. Development of Vildagliptin sustained release dosage forms is desirable to achieve a more effective therapy avoiding the large fluctuations in drug concentration and reduction in adverse effects and to reduce the need of several administrations

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