Synthetic Glycopolypeptide Micelle for Targeted Drug Delivery to Hepatic Carcinoma

Synthetic Glycopolypeptide Micelle for Targeted Drug Delivery to Hepatic Carcinoma
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用于肝癌靶向药物递送的合成糖多肽胶束

DOI:
10.3390/polym10060611
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发表时间:
2018-06
期刊:
影响因子:
5
通讯作者:
Xu Weiguo
Xu Weiguo
中科院分区:
工程技术3区
文献类型:
--
作者:
Li Pengqiang;Han Ji;ong;Li Di;Chen Jinjin;Wang Wei;Xu Weiguo

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将化疗药物靶向递送至肿瘤病灶是肿瘤治疗的一大挑战。到目前为止,人们已经探索了各种聚合物纳米粒子,以通过被动或主动靶向过程来提高这些治疗药物的靶向性。在聚合物纳米颗粒的设计和构建中,糖多肽因其优异的靶向能力和生物相容性而显示出巨大的潜力。为了增强阿霉素(DOX)的抗肿瘤作用,合成了α-乳糖(Lac)修饰的糖多肽胶束(GPM)用于肝癌的靶向治疗。负载DOX的GPM(即GPM/DOX)可以显着靶向人肝癌(HepG2)细胞并进一步抑制其体外增殖。此外,与游离DOX相比,GPM/DOX在肿瘤组织中表现出更高的药物积累和更强的体内抗肿瘤作用。上述结果表明,该药物递送系统为肝癌的靶向治疗提供了一个有前景的平台。
The targeted delivery of chemotherapy drugs to tumor lesions is a major challenge for the treatment of tumors. Up until now, various polymeric nanoparticles have been explored to improve the targetability of these therapeutic drugs through passive or active targeting processes. In the design and construction of polymer nanoparticles, glycopolypeptide has shown great potential owing to its excellent targeting ability and biocompatibility. In order to enhance the antitumor effect of doxorubicin (DOX), a glycopolypeptide-based micelle (GPM) modified by α-lactose (Lac) was synthesized for targeted treatment of hepatoma. The DOX-loaded GPM (i.e., GPM/DOX) could significantly target human hepatoma (HepG2) cells and further inhibit their proliferation in vitro. Additionally, GPM/DOX exhibited a much higher drug accumulation in tumor tissue and a stronger antitumor effect in vivo than free DOX. The above results revealed that this drug delivery system provides a promising platform for the targeting therapy of hepatic cancer.
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