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Updated: Apr 6, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
An efficient injectable formulation with block copolymer micelles for hydrophobic antitumor candidate-pyridazinone
XiuXiu Jin1,2, YaLi Wang1, LiWei Tan1
1State Key Laboratory of Biotherapy & Cancer Center, West China Hospital, Sichuan University, & Collaborative Innovation Center for Biotherapy. Chengdu, China.
Aim:
To make delivery improvements via delivery systems for 6-(4-morpholino-3-(trifluoromethyl)phenyl)pyridazin-3(2H)-one (DZO) - a model compound of hydrophobic antitumor candidate pyridazinone derivatives.
Materials & Methods:
Methoxy poly(ethylene glycol)-poly(D,L-lactide) (MPEG-PDLLA) micelle was employed as a vector, and DZO was encapsulated in. The DZO-loaded micelles were characterized in detail and its cytotoxicity, maximum tolerated dose (MTD) and pharmacokinetic experiments were done. In vivo anticancer activity was studied through a subcutaneous 4T1 tumor model.
Results:
Compared with free DZO, the DZO-loaded micelles possessed a sustained release property, an improved MTD, better pharmacokinetic parameters and an enhanced antitumor activity for subcutaneous 4T1 model in vivo.
Conclusion:
An effective injectable delivery system for DZO was developed successfully.
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