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用于疏水性药物递送的自组装pH响应性超分子水凝胶

Self-assembled pH-responsive supramolecular hydrogel for hydrophobic drug delivery.

作者信息

Wang Lin, Shi Xuefeng, Zhang Jian, Zhu Yuejun, Wang Jinben

机构信息

CAS Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences Beijing 100190 P. R. China

University of Chinese Academy of Sciences Beijing 100049 P. R. China.

出版信息

RSC Adv. 2018 Sep 10;8(55):31581-31587. doi: 10.1039/c8ra06064a. eCollection 2018 Sep 5.

Abstract

In this study, a novel supramolecular hydrogel system, abbreviated as AGC/NTS, prepared by molecular self-assembly of cationic gemini surfactant 1,3-bis(,-dimethyl--cetylammonium)-2-propylacrylatedibromide (AGC) and anionic aromatic compound trisodium 1,3,6-naphthalenetrisulfonate (NTS), was used to encapsulate hydrophobic model drug curcumin (Cur), constructing a pH-responsive drug delivery system. Cur was effectively encapsulated into the hydrophobic domains of AGC/NTS through hydrophobic interaction, which was confirmed by H NMR measurement. The effects of Cur on the mechanical strength, phase transition behaviour and morphology of AGC/NTS were characterized by rheology and cryogenic scanning electron microscopy (cryo-SEM) methods. The pH-responsive release of Cur from AGC/NTS was obtained and the release amount of Cur ascended with pH value decreasing from 7.4 to 3.0. The hydrodynamic sizes of the released Cur-aggregates determined by dynamic light scattering (DLS) were used to analyse the release process of Cur at different pH. The cell viability assay and cell imaging experiment demonstrated that Cur-loaded hydrogel has much higher cytotoxicity and better cell uptake compared to free Cur. Overall, the AGC/NTS hydrogel is a prospective material for use in encapsulation and controlled-release of hydrophobic drug molecules.

摘要

在本研究中,一种通过阳离子双子表面活性剂1,3 - 双(,-二甲基--十六烷基铵)-2 - 丙基丙烯酸二溴化物(AGC)与阴离子芳香族化合物1,3,6 - 萘三磺酸钠(NTS)分子自组装制备的新型超分子水凝胶体系,简称为AGC/NTS,用于包封疏水性模型药物姜黄素(Cur),构建了一种pH响应型药物递送系统。通过核磁共振氢谱(H NMR)测量证实,Cur通过疏水相互作用有效地包封在AGC/NTS的疏水区域中。采用流变学和低温扫描电子显微镜(cryo-SEM)方法表征了Cur对AGC/NTS的机械强度、相变行为和形态的影响。获得了Cur从AGC/NTS的pH响应释放,且Cur的释放量随着pH值从7.4降至3.0而增加。通过动态光散射(DLS)测定释放的Cur聚集体的流体动力学尺寸,以分析Cur在不同pH下的释放过程。细胞活力测定和细胞成像实验表明,与游离Cur相比,负载Cur的水凝胶具有更高的细胞毒性和更好的细胞摄取能力。总体而言,AGC/NTS水凝胶是一种用于包封和控制释放疏水性药物分子的有前景的材料。

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