Long circulating self-assembled nanoparticles from cholesterol-containing brush-like block copolymers for improved drug delivery to tumors.

作者: Thanh-Huyen Tran , Chi Thanh Nguyen , Laura Gonzalez-Fajardo , Derek Hargrove , Donghui Song

DOI: 10.1021/BM5013822

关键词:

摘要: Amphiphilic brush-like block copolymers composed of polynorbonene-cholesterol/poly(ethylene glycol) (P(NBCh9-b-NBPEG)) self-assembled to form a long circulating nanostructure capable encapsulating the anticancer drug doxorubicin (DOX) with high loading (22.1% w/w). The release DOX from DOX-loaded P(NBCh9-b-NBPEG) nanoparticles (DOX-NPs) was steady at less than 2% per day in PBS. DOX-NPs were effectively internalized by human cervical cancer cells (HeLa) and showed dose-dependent cytotoxicity, whereas blank noncytotoxic. demonstrated superior vivo circulation time relative that free DOX. Tissue distribution imaging studies preferentially accumulated tumor tissue markedly reduced accumulation heart other vital organs. greatly improved survival significantly inhibited growth tumor-bearing SCID mice compared for untreated DOX-treated groups. results indicated may be useful carrier improving delivery hydrophobic drugs.

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