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Docetaxel‐Loaded Nanoparticles of Dendritic Amphiphilic Block Copolymer H40‐PLA‐ b ‐TPGS for Cancer Treatment
Author(s) -
Zeng Xiaowei,
Tao Wei,
Wang Zhongyuan,
Zhang Xudong,
Zhu Huijun,
Wu Yanping,
Gao Yongfeng,
Liu Kewei,
Jiang Yuyang,
Huang Laiqiang,
Mei Lin,
Feng SiShen
Publication year - 2015
Publication title -
particle and particle systems characterization
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.877
H-Index - 56
eISSN - 1521-4117
pISSN - 0934-0866
DOI - 10.1002/ppsc.201400048
Subject(s) - polyethylene glycol , copolymer , amphiphile , in vivo , nanoparticle , chemistry , particle size , peg ratio , drug carrier , docetaxel , drug delivery , materials science , nuclear chemistry , nanotechnology , polymer , organic chemistry , cancer , medicine , microbiology and biotechnology , finance , economics , biology
A dendritic amphiphilic block copolymer H40‐poly( d,l ‐lactide)‐block‐d‐α‐tocopheryl polyethylene glycol 1000 succinate (H40‐PLA‐ b ‐TPGS) is synthesized, which is then employed to develop a system of nanoparticles (NPs) loaded with docetaxel (DTX) as a model drug for cancer treatment due to its higher drug‐loading content and drug encapsulation efficiency, smaller particle size, faster drug release, and higher cellular uptake in comparison to the linear PLA polymer NPs and PLA‐ b ‐TPGS copolymer NPs. The drug‐loaded NPs are prepared by a modified nanoprecipitation method and characterized in terms of size and size distribution, surface morphology, drug release profile, and physical state of DTX. Cellular uptake of coumarin 6‐loaded NPs by MCF‐7 cancer cells is determined by flow cytometry and confocal laser scanning microscopy. The antitumor efficacy of the drug‐loaded NPs is investigated in vitro by MTT assay and in vivo by xenograft tumor model. The 72 h IC50 of the drug formulated in the PLA, PLA‐ b ‐TPGS, and H40‐PLA‐ b ‐TPGS NPs is found to be, 1.5 ± 0.3, 0.9 ± 0.1, and 0.15 ± 0.06 μg mL −1 , which are 7.3, 12.2, and 73.3‐fold effective than 11.0 ± 1.2 μg mL −1 for Taxotere, respectively. Such advantages are further confirmed by the measurement of the tumor size and weight.