PT  - JOURNAL ARTICLE
AU  - CAIYUN DENG
AU  - CHANG XU
AU  - XIAOMIN ZHANG
AU  - JU YAO
AU  - YINGXIN ZHANG
AU  - BO YU
AU  - ROBERT J. LEE
AU  - CHENGJUN JIANG
TI  - A Novel Paclitaxel-Loaded Polymeric Micelle System with Favorable Biocompatibility and Superior Antitumor Activity
DP  - 2018 Jan 01
TA  - Anticancer Research
PG  - 219--225
VI  - 38
IP  - 1
4099  - http://ar.iiarjournals.org/content/38/1/219.short
4100  - http://ar.iiarjournals.org/content/38/1/219.full
SO  - Anticancer Res2018 Jan 01; 38
AB  - Background/Aim: Polymeric micelles are promising vehicles for paclitaxel delivery. Further improvement in the stability of the micelle formulation is desirable. Materials and Methods: 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. Results: 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. Conclusion: mPEG-PDLLA-Phe(Fmoc) micelle is a biocompatible and effective drug delivery system for hydrophobic drugs such as PTX.