Preparation, Characterization and <i>In Vitro </i>Release Study of Microcapsule Simvastatin Using Biodegradable Polymeric Blend of Poly(L-Lactic Acid) and Poly(ɛ-Caprolactone) with Double Emulsifier

Abstract

Simvastatin is a cholesterol-lowering agent that inhibits the microsomal activity of 3-hydroxy-3-methylglutaril-CoA-reductase (HMG-CoA reductase), enzyme that contributes in biosynthesis cholesterol. Simvastatin has short half-life elimination about 2 hours and low solubility, this condition makes its bioavailability to be quite small. Simvastatin has adverse effect such as myopathy and rhabdomyolysis because of higher dose consumption of simvastatin. Controlled drug delivery system is needed to reduce the adverse effect. One of method that is used in drug delivery system is encapsulation using biodegradable polymer such as poly(L-lactic acid) and poly(ɛ-caprolactone). PLLA and PCL was blended with fix composition PLLA : PCL 60 : 40 (%w/w) by solvent evaporation technique using Tween 80 and Span 80 as emulsifier. Based on the optimization, the best encapsulation efficiency microcapsules were obtained at concentration of Tween 80 0.025% (v/v), Span 80 1% (v/v) with stirring speed at 900 rpm for 1 hour. The encapsulation efficiency was 83.67%. The best microcapsules were dissolved in dissolution media to get drug release profile. The percentage of drug release at pH 1.2 was 0.86% for 3 hours and in the phosphate buffer solution pH 7.4 for 12.22% for 52 hours.