Abstract

FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLE LOADED DOLUTEGRAVIR SODIUM

M. Sujitha*, K. S. Mohamed Rafeek, A. R. Mohammed Aseef, E. Naresh, D. Ragul and T. Raja

ABSTRACT

Nanoparticle as an innovative formulation of dolutegravir sodium with improved therapeutic efficacy and bioavailability. Dolutegravir sodium (DTG) is an antiretroviral drug and most widely used in treatment of integrase inhibitor. Dolutegravir sodium is a poorly soluble antiretroviral drug that belongs to BCS class II approved by the FDA for treatment of HIV infections; However, DTG has several shortcomings, including low solubility in water, low oral bioavailability, hepatotoxicity, and instability in an acidic environment. And this indicates the need for the development of Dolutegravir sodium loaded Solid Lipid Nanoparticle for the improvement of oral bioavailability of Dolutegravir. The objective of this research is to formulate and evaluate solid lipid nanoparticles containing dolutegravir sodium by various concentration of phospholipid and surfactant using hot homogenization. Totally four batches of SLN were formulated by hot homogenization technique and evaluates for FTIR,drug content, entrapment efficiency, in-vitro drug release studies, particle size, zeta potential, polydispersity index, scanning electron microscopic. Formulation (F1) showed the highest entrapment efficiency and invitro drug release. In this research a drug entrapment efficiency as high as 98.02% and invitro drug release as high as 98.20% has been achieved. It was found that as the concentration of glycerol dibehenate and tween 80 increased, the entrapment efficiency and drug release also increased. The present study revealed that the hot homogenization technique can be used as an effective tool for the preparation of solid lipid nanoparticle of dolutegravir sodium.

Keywords: Dolutegravir sodium, solid lipid nanoparticle, tween 80, glycerol dibehenate, entrapment efficiency, in-vitro drug release studies.