Intracellular K+-Responsive Block Copolymer Micelles for Targeted Drug Delivery of Curcumin
作者全名："Jiang, Mingyue; Chen, Le; Chen, Bo; Yu, Qinghua; Zhang, Xianming; Jing, Weihong; Ma, Limei; Deng, Tao; Yang, Zhangyou; Yu, Chao"
作者地址："[Jiang, Mingyue; Chen, Le; Chen, Bo; Yu, Qinghua; Zhang, Xianming; Jing, Weihong; Ma, Limei; Deng, Tao; Yang, Zhangyou; Yu, Chao] Chongqing Med Univ, Coll Pharm, Chongqing Key Lab Pharmaceut Metab Res, Chongqing, Peoples R China; [Jiang, Mingyue; Yu, Qinghua; Zhang, Xianming; Jing, Weihong; Deng, Tao; Yang, Zhangyou; Yu, Chao] Chongqing Med Univ, Coll Pharm, Res Ctr Pharmaceut Preparat & Nanomed, Chongqing, Peoples R China; [Chen, Le; Ma, Limei; Yu, Chao] Chongqing Med Univ, Coll Pharm, Chongqing Pharmacodynam Evaluat Engn Technol Res C, Chongqing, Peoples R China"
通信作者："Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing Key Lab Pharmaceut Metab Res, Chongqing, Peoples R China.; Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Res Ctr Pharmaceut Preparat & Nanomed, Chongqing, Peoples R China.; Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Chongqing Pharmacodynam Evaluat Engn Technol Res C, Chongqing, Peoples R China."
来源：FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
ESI学科分类：Multidisciplinary
WOS号：WOS:000826974800001
JCR分区：Q1
影响因子：5.7
年份：2022
卷号：10
期号：
开始页：
结束页：
文献类型：Article
关键词：curcumin; polymer micelles; K+ -triggered drug release; responsive host-guest system; anticancer
摘要："Curcumin (CUR) is a natural bioactive compound that has attracted attention as a ""golden molecule"" due to its therapeutic properties against several types of tumors. Nonetheless, the antitumor application of CUR is hampered due to its extremely low aqueous solubility and chemical instability. Herein, a novel type of CUR-loaded polymeric micelles with intracellular K+-responsive controlled-release properties is designed and developed. The polymeric micelles are self-assembled by poly (N-isopropylacrylamide-co-acryloylamidobenzo-15-crown-5-co-N, N-dimethylacrylamide)-b-DSPE (PNDB-b-DSPE) block copolymers, and CUR. CUR is successfully loaded into the micelles with a CUR loading content of 6.26 wt%. The proposed CUR-PNDB-DSPE polymeric micelles exhibit a significant CUR release in simulated intracellular fluid due to the formation of 2 : 1 ''sandwich'' host-guest complexes of 15-crown-5 and K+, which lead to the hydrophilic outer shell of micelles to collapse and the drug to rapidly migrate out of the micelles. In vitro, the B16F10 cell experiment indicates that CUR-PNDB-DSPE micelles exhibit a high cellular uptake and excellent intracellular drug release in response to the intracellular K+ concentration. Moreover, CUR-PNDB-DSPE micelles show high cytotoxicity to B16F10 cells compared to free CUR and CUR-PEG-DSPE micelles. The polymeric micelles with intracellular K+-responsive controlled release properties proposed in this study provide a new strategy for designing novel targeted drug delivery systems for CUR delivery for cancer treatment."
基金机构：Natural Science Foundation of Chongqing [cstc2021jcyj-msxmX0246]; Special Postdoctoral Foundation of Chongqing [2010010005416933]; Postdoctoral Foundation of Chongqing Medical University [YXY2019BSH1]
基金资助正文："Funding The authors gratefully acknowledge support from the Natural Science Foundation of Chongqing (cstc2021jcyj-msxmX0246), the Special Postdoctoral Foundation of Chongqing (2010010005416933), and the Postdoctoral Foundation of Chongqing Medical University (YXY2019BSH1)."
