RT Journal Article
SR Electronic
T1 A Novel Paclitaxel-Loaded Polymeric Micelle System with Favorable Biocompatibility and Superior Antitumor Activity
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 219
OP 225
VO 38
IS 1
A1 CAIYUN DENG
A1 CHANG XU
A1 XIAOMIN ZHANG
A1 JU YAO
A1 YINGXIN ZHANG
A1 BO YU
A1 ROBERT J. LEE
A1 CHENGJUN JIANG
YR 2018
UL http://ar.iiarjournals.org/content/38/1/219.abstract
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.