A simple method to achieve high doxorubicin loading in biodegradable polymersomes

Charles Sanson (1) , Christophe Schatz (1, 2) , Jean-François Le Meins (1, 2) , Alain Soum (1) , Julie Thevenot (1) , Elisabeth Garanger (1, 2) , Sébastien Lecommandoux (1, 2)

1 LCPO - Laboratoire de Chimie des Polymères Organiques
2 Team 3 LCPO : Polymer Self-Assembly & Life Sciences

Doxorubicin (Dox), an anthracycline anticancer drug, was successfully incorporated into block copolymer vesicles of poly(trimethylene carbonate)-b-poly(L-glutamic acid) (PTMC-b-PGA) by a solvent-displacement (nanoprecipitation) method. pH conditions were shown to have a strong influence on loading capacity and release profiles. Substantial drug loading (47% w/w) was achieved at pH 10.5. After pH neutralization, aqueous dispersions of drug-loaded vesicles were found stable for a prolonged period of time (at least 6 months) without vesicle disruption or drug precipitation. Dox-loaded vesicles exhibited in vitro pH and temperature-dependent drug release profiles: release kinetics fastened in acid conditions or by increasing temperature. These features strongly support the interest of developing PTMC-b-PGA polymersomes as carriers for the controlled delivery of Dox

Mots clés: Block copolymer; Vesicle; Polymersome; Doxorubicin; Drug delivery; Controlled release

Domaines: Polymères

Charles Sanson, Christophe Schatz, Jean-François Le Meins, Alain Soum, Julie Thevenot, et al.. A simple method to achieve high doxorubicin loading in biodegradable polymersomes. Journal of Controlled Release, 2010, 147 (3), pp.428-435. ⟨10.1016/j.jconrel.2010.07.123⟩. ⟨hal-00652812⟩