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- Title
Docetaxel-Loaded Nanoparticles of Dendritic Amphiphilic Block Copolymer H40-PLA- b-TPGS for Cancer Treatment.
- Authors
Zeng, Xiaowei; Tao, Wei; Wang, Zhongyuan; Zhang, Xudong; Zhu, Huijun; Wu, Yanping; Gao, Yongfeng; Liu, Kewei; Jiang, Yuyang; Huang, Laiqiang; Mei, Lin; Feng, Si‐Shen
- Abstract
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.
- Subjects
DOCETAXEL; NANOPARTICLES; AMPHIPHILES; SURFACE morphology; POLYETHYLENE glycol; COPOLYMERS; PARTICLE size distribution; ANTINEOPLASTIC agents
- Publication
Particle & Particle Systems Characterization, 2015, Vol 32, Issue 1, p112
- ISSN
0934-0866
- Publication type
Article
- DOI
10.1002/ppsc.201400048