Doxorubicin-Loaded (PEG)3-PLA Nanopolymersomes: Effect of Solvents and Process Parameters on Formulation Development and In Vitro Study

This study is focused on the preparation of doxorubicin-loaded nanopolymersomes (PolyDoxSome) and assessment of the effects of various solvents and process variables on the size and drug loading during preparation of formulation. PolyDoxSome was prepared by nanoprecipitation method using amphiphilic (PEG)3-PLA copolymer, and the formation of polymersomes was assessed by dynamic light scattering and optical and transmission electron microscopy and evaluated for in vitro release profile and in vitro cytotoxicity. A systematic investigation indicated that solvent composition, order of addition, aqueous phase, copolymer concentration, and external energy input have significant influence on size and dispersity of PolyDoxSome. Under optimized conditions, PolyDoxSome had a size range of 130−180 nm with PDI < 0.2, a zeta potential ∼−8 mV, and a drug loading at ∼11% w/w with an encapsulation efficiency at ∼53% w/w. In vitro release profile of PolyDoxSome at 37 °C demonstrated that doxorubicin release was pH depend...