title: Colloidal formulations of etoposide based on poly(butyl cyanoacrylate) nanoparticles: preparation, physicochemical properties and cytotoxicity.
abstract: This article describes the preparation, physicochemical characterization and cytotoxicity assessment of novel colloidal formulations of etoposide based on poly(butyl cyanoacrylate) nanoparticles. Nanoparticles were prepared by controlled emulsion polymerization of butyl cyanoacrylate in aqueous medium using two different non-ionic colloidal stabilizers (pluronic F68 and polysorbate 80). The nanoparticles were spherical in shape, with average size ranging from 110-150 nm (empty nanoparticles) to 170-260 nm (drug-loaded nanoparticles), monomodal size distributions, and negative zeta-potentials at pH 7.4. Drug loading efficiency was around 63-68%. More than 80% of the drug was released from the formulations within 6-7h of dialysis experiments. Pluronic-coated nanoparticles possessed lower magnitude of the ζ-potentials (around -4 mV) in comparison with the polysorbate-coated ones (around -12 mV). All tested etoposide formulations induced apoptosis in adenocarcinoma human epithelial (A549) cells, as evident from condensation of chromatin and fragmentation of nuclei. It was found that etoposide formulated with poly(butyl cyanoacrylate) nanoparticles and polysorbate 80 exhibited the highest cytotoxicity toward adenocarcinoma cells.
authors.affiliation: Sofia University St. Kliment Ohridski, Faculty of Chemistry and Pharmacy, Sofia, Bulgaria. g.g.yordanov@gmail.com
authors.forename: Georgi
authors.initials: G
authors.lastname: Yordanov
authors.forename: Ralica
authors.initials: R
authors.lastname: Skrobanska
authors.forename: Alexander
authors.initials: A
authors.lastname: Evangelatov
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001562:Benzimidazoles; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D003102:Colloids / Q000737:chemistry*; D004396:Coloring Agents; D004659:Enbucrilate / Q000737:chemistry*; D005047:Etoposide / Q000737:chemistry* / Q000494:pharmacology*; D005456:Fluorescent Dyes; D006801:Humans; D007202:Indicators and Reagents; D008027:Light; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012542:Scattering, Radiation; D013778:Tetrazolium Salts; D013844:Thiazoles
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001562:Benzimidazoles; D003102:Colloids; D004396:Coloring Agents; D005456:Fluorescent Dyes; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D005047:Etoposide; C022616:thiazolyl blue; D004659:Enbucrilate; C017807:bisbenzimide ethoxide trihydrochloride