Abstract

DEVELOPMENT AND IN VITRO EVALUATION OF NANOSTRUCTURED LIPID CARRIERS (NLCs) OF GLICLAZIDE

Aindrilla S. Duttagupta*, Kisan R. Jadhav and Vilasrao J. Kadam

ABSTRACT

Gliclazide is a potential second generation oral hypoglycemic agent, which belongs to BCS class II drugs having low solubility and high permeability. It has log P value of 2.6, pKa of 5.8, molecular weight of 323.42, and has poor and variable oral bioavailability. The GI absorption rate of gliclazide is very slow and requires 2 to 8 hrs to reach peak serum levels. Therefore keeping these in mind, an attempt was made to prepare NLCs of Gliclazide which will provide controlled release, along with a concomitant improvement in solubility and dissolution profile of drug. Gliclazide loaded NLCs were produced by high shear homogenization coupled with ultrasonication technique using Precirol ATO 5 as solid lipid, Capryol 90 as liquid lipid, Tween 20 as surfactant and Transcutol HP as a cosurfactant. The NLCs were characterized for entrapment efficiency, particle size and in vitro drug release. The optimized batch was subjected to freeze drying using trehalose as cryoprotectant and the freeze dried powder was filled into hard gelatin capsule of suitable size. In vitro release studies of NLC capsules showed that Gliclazide exhibited an initial burst release followed by a sustained release of 88.46% compared to the marketed S.R. tablet which showed a slow and sustained release of 86.34% at the end of 24 hours.

Keywords: Nanostructured lipid carrier, Gliclazide, Sustained release.