Abstract

FORMULATION DEVELOPMENT AND EVALUATION OF SOLID LIPID NANOPARTICLES OF BUPRENORPHINE

Suryakalyanam Vikas*, S. Poonguzhali, Manohar Babu S.

Abstract

Buprenorphine is a poorly water soluble drug as it is a BCS Class II drug and the oral bioavailability is very less due to the extensive first pass effect. So there is a need to develop a formulation that can improve the oral bioavailability. In this work, efforts were made to prepare stable solid lipid nanoparticles for enhancement of oral bioavailability of Buprenorphine. Drug solubility studies were performed with various lipids to test the solubility and the glyceryl monostearate was the lipid in which the drug is more soluble. SLNs were prepared by the hot homogenization method. For the optimization of the surfactant the three more formulations were prepared. Characterization of SLNs was done by measuring particle size, Poly dispersity index and zeta potential by zeta sizer. The Entrapment efficiency of the SLNs was found to be in the range of 80 to 95% In- vitro drug release studies were performed for all these SLNs for 24 hrs in pH 6.8 phosphate buffer. In these studies the cumulative percentage drug release from all these formulations showed prolonged release. The formulation (F2) was found to be promising prolonged release. This formulation (F2) released 77.3 % of drug in 24 hours. The release kinetics of the optimized formulation is first order and from the higuchi plot the release is by diffusion process and from the korsemeyers plot the diffusion process is non-fickian diffusion.

Keywords: Buprenorphine, Solid Lipid Nanoparticles, Bioavailability, Glyceryl monostearate, Solubility studies.