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,Biomacromolecules

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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
Biomacromolecules ( IF 5.5 ) Pub Date : 2018-05-22 00:00:00 , DOI: 10.1021/acs.biomac.8b00488
Jianping He ₁ , Jianzhuang Chen ₁ , Shaoliang Lin ₁ , Dechao Niu ₁ , Jina Hao ₁ , Xiaobo Jia ₁ , Nan Li ₁ , Jinlou Gu ₁ , Yongsheng Li ₁ , Jianlin Shi _{1,

2}

Affiliation

A pillar[5]arene-based nonionic polyrotaxane (PR) with star-poly(ε-caprolactone) (S-PCL) as the axle, pillar[5]arene (DEP5) as the wheel and adamantane as the end-capped group is designed and synthesized. The resulting PR is subsequently assembled with β-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 ([email protected]) shows much enhanced cellular uptake and cytotoxicity against the SMMC-7721. More importantly, thanks to the enhanced permeability and retention (EPR) effect, [email protected] exhibits appealing features such as extremely low toxicity, highly efficient intratumoral accumulation and substantial antitumor efficacy in vivo.

中文翻译：

支柱[5]芳烃基聚轮烷的合成，以增强基于PCL的超分子两亲物的药物载量，作为优良的药物递送平台

具有星型聚（ε-己内酯）的基于柱[5]芳烃的非离子聚轮烷（PR ）（S设计并合成了以[PCL]为轴，以[5]芳烃（DEP5）为车轮和以金刚烷为末端封端的基团。随后，通过主体-客体相互作用，将生成的PR与β-环糊精末端封端的pH刺激的聚丙烯酸（CD-PAA）组装在一起，形成超分子假嵌段聚合物PR-PAA。这种超分子假嵌段聚合物可以在水溶液中自组装以产生基于PR-PAA的超分子水泡纳米颗粒（PR-SVNP），其呈现出显着提高的DOX载药量（DLC，45.6％），远高于超两亲物（ PCL-PAA，17.1％）。PR-SVNPs如此高的DLC最有可能归因于PR中PCL的结晶度大大降低。而且，可以以酸性微环境响应性方式选择性地释放负载的药物。与免费DOX相比，装载DOX的PR-SVNP（[电子邮件保护]）显示出对SMMC-7721的细胞摄取和细胞毒性大大增强。更重要的是，由于增强的渗透性和保留（EPR）效果，[电子邮件保护]表现出吸引人的功能，例如极低的毒性，高效的肿瘤内累积和体内显着的抗肿瘤功效。

更新日期：2018-05-22

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