Jornal de Nanomedicina e Nanotecnologia

Abstrato

Preparation and Characterization and Biodistribution Studies of Lomustine Loaded PLGA Nanoparticles by Interfacial Deposition Method.

Archana Mehrotra and Jayanta Kumar Pandit

The incorporation of lomustine, a hydrophobic anticancer drug into PLGA nanoparticles by interfacial deposition method was optimized. Based on the optimal parameters, it was found that lomustine-PLGA nanoparticles with acceptable properties could be obtained. Optimization of formulation variables to control the size and drug entrapment efficiency of the prepared nanoparticles seems to be based on the same scientific principles as drug-loaded nanoparticles prepared by nanoprecipitation, solvent evaporation method. The process was the most important factor to control the particle size, while both the drug-polymer interaction and the partition of drug in organic and aqueous phases were the crucial factors to govern the drug entrapment efficiency. PLGA concentration at lower level (100 mg), 1:5 organic phase: aqueous ratio, 1%w/v PVA concentration, 3%w/v pluronic F68 achieved smaller particle size. Additionally, L:G ratio of PLGA 75:25, lower volume of organic solvent (1:10 organic phase: aqueous phase), higher initial drug content (10 mg) enhanced the drug entrapment efficiency and maintained lomustine concentration in blood for an extended time period, elevated lomustine concentration in lungs and slowed the elimination of lomustine. The biodistribution profiles of prepared nanoparticles in albino mice showed higher plasma drug concentration for longer period of time, elevated drug concentration in lungs and slow elimination from kidney. No toxic effects of prepared nanoparticles were observed in histopathological examination of lungs and kidney. The systematic investigation reported here promises the development of PLGA nanoparticles loaded with lomustine when tested in Lung Cancer cell line L132 and toxicological/ histopathological studies in albino mice.