文献：Tumor-targeting and redox-sensitive micelles based on hyaluronic acid conjugate for delivery of paclitaxel

作者：Jiyang Liu, Na Liang, […], and Shaoping Sun 

文献链接：https://journals.sagepub.com/doi/abs/10.1177/0885328220905256

The clinical application of paclitaxel is limited due to its low solubility and severe side effects. A tumor-targeting and redox-sensitive paclitaxel-loaded micellar system could exhibit high drug solubility, excellent antitumor activity and low toxicity to normal tissues. An mPEG and hexadecanol-modified hyaluronic acid with disulfide bridges in the molecules (mPEG-S-S-HA-C16) was designed and synthesized. Using mPEG-S-S-HA-C16 as the carrier, the paclitaxel-loaded micelles were fabricated, and their physicochemical properties were studied deeply. Moreover, the antitumor evaluation of the paclitaxel-loaded micelles was conducted in vitro and in vivo. For the optimized paclitaxel-loaded mPEG-S-S-HA-C16 micelles, the average size and zeta potential were 168.6 nm and −38.2 mV, respectively. In vitro drug release study demonstrated the redox-sensitivity of the micelles that the encapsulated paclitaxel could be released rapidly in the presence of glutathione. MTT assay confirmed the low toxicity of the polymeric material itself and the excellent cytotoxicity of paclitaxel-loaded mPEG-S-S-HA-C16 micelles against MCF-7 cells. Moreover, the in vivo antitumor evaluation demonstrated the superior antitumor efficacy of the paclitaxel-loaded micelles. These results suggested that the paclitaxel-loaded mPEG-S-S-HA-C16 micelles held great promise for targeted delivery of paclitaxel.

负载紫杉醇的肿瘤靶向和氧化还原敏感胶束系统可以表现出高药物溶解度、优异的肿瘤活性和对正常组织的低毒性。

设计并合成了一种分子中带有二硫键的mPEG和十六醇修饰的透明质酸（mPEG-S-S-HA-C16）。以mPEG-S-S-HA-C16为载体，制备了紫杉醇胶束，并对其理化性质进行了深入研究。 

对于优化的紫杉醇负载mPEG-S-S-HA-C16胶束，平均粒径和ζ电位为168.6 nm和-38.2 mV。体外药物释放研究证明了胶束的氧化还原敏感性，即包封的紫杉醇在谷胱甘肽存在下可以快速释放。

MTT法证实了聚合物材料本身的低毒性和紫杉醇负载mPEG-S-S-HA-C16胶束对MCF-7细胞的优异细胞毒性。

这些结果表明，负载紫杉醇的mPEG-S-S-HA-C16胶束在紫杉醇的靶向递送方面具有很大的前景。

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