Abstract

FORMULATION, OPTIMIZATION AND EVALUATION OF CONTROLLED RELEASE MICROSPHERES OF LOSARTAN POTASSIUM

Geeta*, Charan Singh, Tarun Virmani, Jyoti Gupta, Reshu Virmani

Abstract

Objective: The aim of this study was to prepare losartan potassium loaded albumin microspheres. Methods: w/o emulsion thermal crosslinking method with different drug-to-polymer ratios {(1:1), (1:2), (1:3)}, using a 22-gauge hypodermic syringe into an external phase. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X1) and stirring speed (X2), on dependent variables, encapsulation efficiency, particle size, and % drug release. Result: Nine F1, F2, F3, F4, F6, F7, F8 and F9, formulations prepared, F7 i.e., 1:3 (drug–polymer) ratio was selected as the optimized formulation based on particle size, encapsulation efficiency, and the release behavior. The microsphere formulations were able to sustain the release of drug in vitro more than 8 hrs Dissolution data obtained from in-vitro release studies fitted on zero order, first order, Higuchi, and Peppas model. The DRS spectrum revealed that the presence of excipient did not show any shift in the spectrum. The microspheres stored under variable storage condition were found to be stable both physically and chemically.

Keywords: In vitro release, microspheres, encapsulation efficacy, losartan potassium, albumin.