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The poor stability of micellar drug delivery system in vivo due to large volume dilution often leads to?premature drug release with low therapeutic efficacy. In this study, shell cross-linked micelles of?graftlike block copolymer bearing biodegradable 3-caprolactone branches (PMAA-b-PFM) were?prepared to be used as a novel carrier for paclitaxel (PTX). PTX was successfully encapsulated into the?hydrophobic cores of the cross-linked micelles using the dialysis method. The resultant PTX-loaded?cross-linked micelles were about 99 nm in diameter with spherical shape and high encapsulation
efficiency. The PTX-loaded cross-linked micelles had smaller sizes and better stability as compared to?the non-cross-linked controls. Fluorescence microscopy and flow cytometry studies showed that PTXloaded?cross-linked micelles had excellent cellular uptake ability by bone marrow derived macrophages?and human glioma U87 cells. Cellular uptake of cross-linked micelles was found to be higher than noncross-?linked controls due to smaller size. In vitro cytotoxicity studies also revealed that the PTX-loaded?cross-linked micelles exhibit high anti-cancer activity to U87 cells. These results suggested that crosslinked?PMAA-b-PFM micelles could be a potential vehicle for delivering hydrophobic?chemotherapeutic drugs to tumors.

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作者

Youhua Tao,Ren Liu,Mingqing Chen,Cheng Yang and Xiaoya Liu

期刊

Journal of Materials Chemistry

年份