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BioMed Research International
Volume 2014, Article ID 363404, 9 pages
http://dx.doi.org/10.1155/2014/363404
Research Article

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles: In Vitro Drug Release and Pharmacokinetics Studies

1Department of Pharmaceutics, I.T.S. Paramedical College (Pharmacy), Muradnagar, Ghaziabad 201206, India
2Department of Pharmacognosy & Phytochemistry, Jamia Hamdard, New Delhi 110062, India

Received 24 February 2014; Revised 6 April 2014; Accepted 10 April 2014; Published 21 May 2014

Academic Editor: Mehrdad Hamidi

Copyright © 2014 Praveen Kumar Gaur et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C 2°C and % relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration ( ) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).