PLGA nanoparticles loaded with etoposide and quercetin dihydrate individually: in vitro cell line study to ensure advantage of combination therapy

摘要

PLGA nanoparticles, separately loaded with etoposide (ETN) and quercetin dihydrate (QDN), were prepared by adapting the solvent diffusion (nanoprecipitation) technique. The effect of formulation variables such as amount of polymer, theoretical drug loading, surfactant concentration, and aqueous and organic phase volumes on particle size and entrapment efficiency, were systematically studied. The optimal formulations obtained were of submicron size (153.4 ± 4.2 nm for ETN and 148.6 ± 1.6 nm for QDN) and with low polydispersity indices (0.058 ± 0.02 for ETN and 0.088 ± 0.03 for QDN). The entrapment efficiencies were found as 63.88 ± 1.5 % and 41.36 ± 3.4 % for ETN and QDN, respectively. The characterization of ETN and QDN was done by measuring the zeta potential, TEM, and DSC analysis. The comparison was made in respect of in vitro cytotoxicity assay using cancer cell line A549 (human lung adenocarcinoma epithelial cell line). The results revealed significant increase in cytotoxicity in nanoparticle formulations than their respective free drug. The comparison was also made with respect to cytotoxic activity of individual drug and combination of drugs in the form of free drugs as well as nanoparticles. The combination treatment in the form of nanoparticles is found to produce best results among the treatments used in cytotoxicity studies.