International Journal of Pharmaceutical Investigation, 2014, 4, 3, 142-148.
DOI:10.4103/2230-973X.138348
Published: August 2014
Type: Original Article
Authors:
Josephine Leno Jenita
Department of Pharmaceutics, Dayananda Sagar College of Pharmacy, Bangalore, Karnataka, India.
Vijaya Chocalingam
Department of Pharmaceutics, Ultra College of Pharmacy, Madurai, Tamil Nadu, India.
Barnabas Wilson
Department of Pharmaceutics, Dayananda Sagar College of Pharmacy, Bangalore, Karnataka, India.
ABSTRACT
Purpose of the study: The antiretroviral therapy (ART) has dramatically improved human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) treatment, prevention and also has been found to increase the lifespan of HIV/AIDS patients by providing durable control of the HIV replication in patients. Efavirenz is a non-nucleoside reverse transcriptase inhibitor of HIV-1. The purpose of this study is to formulate efavirenz-loaded bovine serum albumin nanoparticles to improve efavirenz delivery into various organs. Materials and Methods: Nanoparticles were prepared by desolvation technique and coated with polysorbate 80. Ethanol, glutaraldehyde, and mannitol were used as desolvating, cross-linking agent and cryoprotectant, respectively. Drug to polymer ratio was chosen at five levels from 1:2, 1:3, 1:4, 1:5, and 1:6 (by weight). The formulated nanoparticles were characterized for Fourier Transform Infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) studies, entrapment efficiency, particle size, surface charge, surface morphology, in vitro drug release, release kinetics, stability studies, and biodistribution studies. Results and Major Conclusion: The particle size of the prepared formulations was found below 250nm with narrow size distribution, spherical in shape and showed good entrapment efficiency (45.62–72.49%). The in vitro drug release indicated biphasic release and its data were fitted to release kinetics models and release pattern was Fickian diffusion controlled release profile. The prepared nanoparticles increased efavirenz delivery into various organs by several fold in comparison with the free drug.
Keywords: Albumin nanoparticles, Animal testing, Desolvation technique, Efavirenz (NNRTIs), Polysorbate 80 .