文献类型：期刊文献

英文题名：Synthesis of a Pillar[5]arene-Based Polyrotaxane for Enhancing the Drug Loading Capacity of PCL-Based Supramolecular Amphiphile as an Excellent Drug Delivery Platform

作者：He, Jianping[1];Chen, Jianzhuang[1];Lin, Shaoliang[1];Niu, Dechao[1];Hao, Jina[1];Jia, Xiaobo[1];Li, Nan[1];Gu, Jinlou[1];Li, Yongsheng[1];Shi, Jianlin[1,2]

机构：[1]East China Univ Sci & Technol, Sch Mat Sci & Engn, Key Lab Ultrafine Mat, Lab Low Dimens Mat Chem,Minist Educ, Shanghai 200237, Peoples R China;[2]Chinese Acad Sci, Shanghai Inst Ceram, State Lab High Performance Ceram & Superfine Micr, Shanghai 200050, Peoples R China

年份：2018

卷号：19

期号：7

起止页码：2923

外文期刊名：BIOMACROMOLECULES

收录：;EI(收录号：20182205256947);WOS:【SCI-EXPANDED(收录号:WOS:000438470800056)】；

基金：This work was financially supported by the National Natural Science Foundation of China for Innovative Research Groups (No. 51621002); the National Key Research and Development Program of China (Grant No. 2016YFA0203700); NSFC (Grant Nos. 51572083, 51461165202, and 51472085); Program of Shanghai Academic/Technology Research Leader (18XD1401400); Basic Research Program of Shanghai (17JC1404702); the Shanghai Rising-Star Program (16QA1401300); the 111 Project (B14018); and The Fundamental Research Funds for Central Universities (222201718002). All animal experiments were performed in compliance with the Guidelines for the Care and Use of Research Animals established by the East China University of Science and Technology Animal Studies Committee.

语种：英文

外文关键词：Targeted drug delivery - Aromatic hydrocarbons - Crystallinity - Drug interactions - Controlled drug delivery

摘要：A pillar[5]arene-based nonionic polyrotaxane (PR) with star-poly(e-caprolactone) (S-PCL) as the axle, pillar[5]arene (DEPS) as the wheel and adamantane as the end-capped group is designed and synthesized. The resulting PR is subsequently assembled with beta-cyclodextrin end-capped pH-stimulated poly(acrylic acid) (CD-PAA) via a host-guest interaction to form the supramolecular pseudoblock polymer PR-PAA. This supramolecular pseudoblock polymer could self-assemble in aqueous solution to produce PR-PAA-based supramolecular vesicular nanoparticles (PR-SVNPs), which present significantly enhanced drug loading capacity (DLC, 45.6%) of DOX, much higher than those of superamphiphiles (PCL-PAA, 17.1%). Such a high DLC of PR-SVNPs can be most probably attributed to the greatly decreased crystallinity of PCL in PR Moreover, the loaded drugs could be selectively released in an acidic microenvironment-responsive manner. Compared to free DOX, the DOX-loaded PR-SVNPs (DOX@PR-SVNPs) shows much enhanced cellular uptake and cytotoxicity against the SMMC-7721. More importantly, thanks to the enhanced permeability and retention (EPR) effect, DOX@PR-SVNPs exhibits appealing features such as extremely low toxicity, highly efficient intratumoral accumulation and substantial antitumor efficacy in vivo.