A Novel Paclitaxel-Loaded Polymeric Micelle System with Favorable Biocompatibility and Superior Antitumor Activity

Polymeric micelles are promising vehicles for paclitaxel delivery. Further improvement in the stability of the micelle formulation is desirable. Monomethoxy poly(ethylene glycol)-block-poly(D,L-lactide)-9-fluorenylmethoxycarbonyl-L-phenylalanine (mPEG-PDLLA-Phe(Fmoc)) was synthesized through a class...

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Bibliographic Details
Published in:Anticancer research 2018-01, Vol.38 (1), p.219
Main Authors: Deng, Caiyun, Xu, Chang, Zhang, Xiaomin, Yao, J U, Zhang, Yingxin, Yu, B O, Lee, Robert J, Jiang, Chengjun
Format: Article
Language:English
Subjects:
Anticancer properties
Antitumor activity
Biocompatibility
Chemical synthesis
Drug delivery
Drug delivery systems
Esterification
Hemolysis
Hydrophobicity
Micelles
MPEG encoders
Paclitaxel
Pharmacokinetics
Pharmacology
Phenylalanine
Physicochemical properties
Polyethylene glycol
Safety
Self-assembly
Toxicity
Toxicity testing
Video compression
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Summary:Polymeric micelles are promising vehicles for paclitaxel delivery. Further improvement in the stability of the micelle formulation is desirable. Monomethoxy poly(ethylene glycol)-block-poly(D,L-lactide)-9-fluorenylmethoxycarbonyl-L-phenylalanine (mPEG-PDLLA-Phe(Fmoc)) was synthesized through a classical esterification reaction. Paclitaxel-loaded mPEG-PDLLA-Phe(Fmoc) micelles (PTX-PheMs) were prepared by the self-assembly method. Composition, structure and physicochemical properties were characterized. Pharmacokinetics were evaluated in rats. Therapeutic effect was evaluated in tumor-bearing mice. Safety profile was assessed by a hemolysis assay and an acute-toxicity study. The average size of PTX-PheMs was about 45 nm. The hemolysis and acute-toxicity tests confirmed its biocompatibility and safety. The pharmacokinetics and therapeutic effect experiments demonstrated its long circulation property and superior antitumor effect. mPEG-PDLLA-Phe(Fmoc) micelle is a biocompatible and effective drug delivery system for hydrophobic drugs such as PTX.
ISSN:0250-7005
1791-7530
DOI:10.21873/anticanres.12211