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Rod-Shaped Micelles Based on PHF-g-(PCL-PEG) with pH-Triggered Doxorubicin Release and Enhanced Cellular Uptake

Wu, Yanqian, Xiao, Yi, Huang, Yushu, Xu, Yanyun, You, Donglei, Lu, Wei, Yu, Jiahui
Biomacromolecules 2019 v.20 no.3 pp. 1167-1177
biodegradability, composite polymers, cytotoxicity, doxorubicin, endocytosis, flow cytometry, in vitro studies, kinetics, micelles, models, pH, polyethylene glycol
A biodegradable brush-type copolymer PHF-g-(PCL-PEG) based on a cleavable polyacetal backbone and biodegradable side chain modified with polyethylene glycol (PEG) was synthesized in this paper. This particular structure was directional to facilitate the formation of spherical or rod-shaped micelles. Flow cytometry showed that rod-shaped micelles displayed enhanced cellular uptake compared to spherical micelles. Rod-shaped micelles were selected to investigate their drug delivery abilities in detail. In vitro experiments verified the pH-triggered drug release of DOX-loaded micelles, and the release rate of doxorubicin (DOX) was 77% at pH 5.0 and 26% at pH 7.4. In drug-release kinetic analysis, a double-exponential model achieved the best fit. The copolymer appeared to be almost nontoxic, while the DOX-loaded micelles showed equivalent cytotoxicity compared to DOX at high concentration. The endocytosis of DOX-loaded micelles was two times that of DOX. Our findings suggest that the pH-sensitive brush type copolymer could be a possible carrier in drug delivery.