Folate-conjugated and pH-responsive polymeric micelles for target-cell-specific anticancer drug delivery
Folate-conjugated and pH-responsive polymeric micelles for target-cell-specific anticancer drug delivery
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用于靶细胞特异性抗癌药物递送的叶酸缀合和 pH 响应聚合物胶束
DOI：
10.1016/j.actbio.2017.07.018
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发表时间：
2017-09-15
影响因子：
9.7
通讯作者：
Zhang, Zheng-Yun
中科院分区：
文献类型：
--
作者：
Guan, Jiao;Zhou, Zun-Qiang;Zhang, Zheng-Yun
在这项研究中，我们开发了一种用于抗癌药物递送的叶酸 (FA) 缀合和 pH 响应主动靶向胶束系统。在该体系中，FA附着在聚乳酸-聚L-赖氨酸(PLA-PLL)亲水链段的末端，并且PLL被柠檬酸基团修饰。 FA受体介导的主动靶向以及由于负电荷反转而导致胶束与细胞膜之间的静电相互作用被结合在一种胶束抗癌药物递送系统中，以增强胶束的肿瘤靶向和细胞内化。体外和体内抗癌研究表明，负载阿霉素、FA 缀合和 pH 响应的聚合物胶束具有增强且有效的抗癌功效。意义说明带负电的纳米载体可延长抗癌药物的血液循环。但很难内化。因此，带负电至正电的胶束表面可以提高肿瘤细胞的选择性并增加摄取机会。 意义声明：在这项研究中，我们开发了一种叶酸 (FA) 偶联且 pH 响应的主动靶向胶束系统，用于抗癌药物递送。 FA受体介导的主动靶向以及由于负电荷反转而导致胶束与细胞膜之间的静电相互作用被结合在一种胶束抗癌药物递送系统中，以增强胶束的肿瘤靶向和细胞内化。体外和体内抗癌研究表明，负载阿霉素、FA 结合且 pH 响应的聚合物胶束具有增强且有效的抗癌功效。 (C) 2017 年由 Elsevier Ltd 代表 Acta Materialia Inc. 发布。
In this study, we developed a folate (FA)-conjugated and pH-responsive active targeting micellar system for anti-cancer drug delivery. In this system, FA was attached to the terminal of the hydrophilic segment of poly(lactic acid)-poly(L-lysine) (PLA-PLL), and PLL was modified by a citric acid group. The FA receptor-mediated active targeting and electrostatic interaction between micelles and cell membrane due to a negative-to-positive charge reversal was combined in one micellar anti-cancer drug delivery system to enhance the tumour targeting and cellular internalisation of micelles. In vitro and in vivo anticancer studies demonstrated that the doxorubicin-loaded, FA-conjugated and pH-responsive polymeric micelles possess an enhanced and effective cancer efficiency.Statement of significanceNegatively charged nano-carriers prolonged anti-cancer drugs' blood circulation. However it is difficult to be internalised. Therefore, a negative-to-positive charged micelle surface could improve selectivity for tumour cells and increase uptake chance.Statement of significance: In this study, we developed a folate (FA)-conjugated and pH-responsive active targeting micellar system for anti-cancer drug delivery. The FA receptor-mediated active targeting and electrostatic interaction between micelles and cell membrane due to a negative-to-positive charge reversal was combined in one micellar anti-cancer drug delivery system to enhance the tumour targeting and cellular internalisation of micelles. In vitro and in vivo anti-cancer studies demonstrated that the doxorubicin-loaded, FA-conjugated and pH-responsive polymeric micelles possess an enhanced and effective cancer efficiency. (C) 2017 Published by Elsevier Ltd on behalf of Acta Materialia Inc.