Effect of Stabilizer Concentration on Parameters of Poly(D,L-lactide-co-glycolide) Nanoparticles Produced by Nanoprecipitation

Abstract

Effect of a poly(vinyl alcohol) (PVA) stabilizer concentration on the parameters of nanoparticles prepared by nanoprecipitation of biodegradable poly(D,L-lactide-co-glycolide) (PLGA) copolymers has been studied. It has been revealed that, at a constant concentration of the organic phase (5 mg/mL), the hydrodynamic diameter of PLGA particles does not depend on stabilizer concentration in an aqueous phase (2.5–15 mg/mL) and is ~130–140 nm, while the polydispersity index and the absolute value of the electrokinetic potential of the particles decrease with an increase in the PVA concentration. It has been shown that the PVA concentration has almost no effect on the content of a hydrophobic model drug, docetaxel, loaded into the PLGA particles, as well as on its in vitro cytotoxic activity against mice colorectal carcinoma cells and human embryo lung fibroblasts of the CT26 and WI-38 lines, respectively. At the same time, the ability of drug-loaded PLGA particles to lyophilization and subsequent redispersion in water depend on the stabilizer concentration: the higher the PVA concentration in the system the easier the redispersion of the particles to their initial sizes.