Mon, 18 Dec 2017

Preparation, Characterization and Surface Modification of Nevirapine Nanoparticles

Bhagyashree R. Dalvi1, Rupesh U. Shelke1, Ejaz A. Siddiqui2, Asad S. Syed2, Mariam S. Degani1, Padma V. Devarajan1*

1. Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N.P. Marg, Matunga (E), Mumbai, Maharashtra, India

2. Biochemical Sciences Division, CSIR-National Chemical Laboratory, Pune, India.


ABSTRACT

HIV/AIDS is an intracellular infection of the macrophages and play an important role in dissemination of the infection across the body. Nevirapine although remains a drug of choice for the treatment; the life threatening hepatotoxicity limits its clinical application. Present study reports preparation, characterization and surface modification of nevirapine nanoparticles. The anti-HIV potential of gold nanoparticles prompted us to prepare nevirapine loaded gold nanoparticles using a biodegradable in house polymer polyethylene sebacate. Core shell nevirapine nanoparticles comprising gold in the core and nevirapine loaded polyethylene sebacate as shell (average particle size ~ 250nm) were successfully prepared using double emulsion solvent evaporation method followed by surface modification with macrophage mannose receptor targeting ligand Concanavalin A by simple incubation. Concanavalin A was selected as a targeting ligand as the molecular docking studies of Concanavalin A with excipients suggested possible interactions. Concanavalin A anchoring was confirmed by spectrofluoremetrically, FTIR and zeta potential analysis. UV analysis of nevirapine nanoparticles revealed shell formation and NVP loading. SEM-EDAX analysis indicated presence of Au in the spherical nanoparticles while TEM confirmed formation of core shell nanoparticles with smooth surface. DSC and XRD analysis demonstrated amorphization of NVP in nanoparticles. Residual solvent analysis complied ICH standards. Nanoparticles with and without CON exhibited sustained release till 24 h in phosphate buffer pH 7.4 and good stability for 1 year as per ICH guidelines.

Keywords: HIV/AIDS, macrophages, nevirapine, gold nanoparticles, concanavalin A, spectrofluoremetry.


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