Design, formulation and evaluation of abacavir microspheres

Abstract

The objective of present study was to encapsulate the anti-retroviral drug in various polymers in order to provide

the sustained release and to minimize or reduce the dose dependent side effects as well as to improve the patient

compliance. Abacavir sulphate microspheres were prepared by w/o emulsification solvent evaporation method

using different polymers viz. sodium alginate and gelatin. The prepared microspheres were characterized for

drug entrapment efficiency, muco-adhesion test, particle size analysis, surface morphology and in-vitro drug

release study. The in-vitro release studies were performed using pH 1.2 Hcl and pH 7.4 phosphate buffer and

drug release is evaluated. Morphology of microspheres was characterized by using Scanning Electron

Microscopy (SEM). The prepared microspheres were small, discrete, free flowing and spherical in shape. The

mean diameter of microspheres was between 21.00±1.96 to32.43±2.19μm for different formulations. The drug

loaded microspheres showed 40-65% and 45-50% of entrapment for sodium alginate and gelatin microspheres

respectively. Fourier Transform- Infra Red (FT-IR) was performed to evaluate interaction between drug and

polymer. The prepared microspheres exhibited prolonged drug release (10h) as the concentration of sodium

alginate increased, the muco-adhesion is also increased as the sodium alginate concentration increases and the

drug release rate was decreased at higher concentration of gelatin.