PREPARATION AND STUDY OF EFAVIRENZ MICROEMULSION DRUG DELIVERY SYSTEM FOR ENHANCEMENT OF BIOAVAILABILITY

Hemal Tandel*, Pratiksh Patel, Parva Jani

ABSTRACT

The purpose of study was to develop a microemulsion drug delivery system to enhance the bioavailability of Efavirenz(EFV). The microemulsion was prepared using efavirenz(drug), Capryol 90(oil), Tween 20 and Cremophor EL(surfactant) and Transcutol HP (co-surfactant) and water. The optimized formula for microemulsion was determined using phase diagrams which were constructed prior to the formulation. The physical evaluation like globule size, zeta potential, pH, conductance, drug content, stability etc. were performed along with in vitro and ex vivo studies. The pharmacokinetics studies were
also performed on male albino rat. The optimized formulation of efavirenz microemulsion had globule size and zeta potential of was found to be 15.8±0.71nm and -12.6±0.23mv respectively. The optimized formulation showed higher drug release in in vitro and ex vivo studies as compared to pure drug suspension. Efavirenz microemusion shows 1.88 folds increase in peak plasma concentration in comparison to pure drug suspension and AUC was found to increase 2.15 fold in comparison to pure drug suspension. The size reduction by microemulsion would improve the bioavailability of the drug in vivo after oral administration.

Keywords: Microemulsion, Efavirenz, Pharmacokinetic, Bioavailability.