In vitro and In vivo Evaluation of Docetaxel Loaded Biodegradable Polymersomes

Kamal Kumar Upadhyay (1) , Anant N. Bhatt (2) , Emilio Castro (1) , Anil K. Mishra (3) , Krishna Chuttani (3) , Bilikere S. Dwarakanath (2) , Christophe Schatz (1, 4) , Jean-François Le Meins (1, 4) , Ambikanandan Misra (5) , Sébastien Lecommandoux (1, 4)

1 LCPO - Laboratoire de Chimie des Polymères Organiques
2 DRDO, INMAS - Div Radiat Biosci
3 DRDO, INMAS - Div Cyclotron & Radiopharmaceut Sci
4 Team 3 LCPO : Polymer Self-Assembly & Life Sciences
5 Pharm Dept, Fac Technol & Eng, Univ Baroda

Formulation of docetaxel (DOC), a hydrophobic anticancer drug, was successfully achieved in poly(gamma-benzyl L-glutamate)-block-hyaluronan polymersomes using a simple and reproducible nanoprecipitation method. The prepared DOC loaded polymersomes (PolyDOC) was stable either in solution or in a lyophilized form, and showed controlled release behaviour over several days. PolyDOC showed high in vitro toxicity after 24h in MCF-7 and U87 cells compared to free DOC. Biodistribution data demonstrated that (99m)Tc labelled PolyDOC t(1/2) and MRT significantly increased compared to a DOC solution (DS). In addition, PolyDOC uptake in Ehrlich Ascites Tumor (EAT) tumor bearing mice was larger at each time point compared to DS, making such a polymer vesicle formulation an efficient drug nanocarrier for improved DOC cancer therapy.

Mots clés: biodegradable; biodistribution; docetaxel; drug delivery systems; hyaluronan; polymersome; tumor uptake

Domaines: Polymères

Kamal Kumar Upadhyay, Anant N. Bhatt, Emilio Castro, Anil K. Mishra, Krishna Chuttani, et al.. In vitro and In vivo Evaluation of Docetaxel Loaded Biodegradable Polymersomes. Macromolecular Bioscience, 2010, 10 (5), pp.503-512. ⟨10.1002/mabi.200900415⟩. ⟨hal-00652855⟩