Nanostructured lipid carrier-based pH and temperature dual-responsive hydrogel composed of carboxymethyl chitosan and poloxamer for drug delivery
Nanostructured lipid carrier-based pH and temperature dual-responsive hydrogel composed of carboxymethyl chitosan and poloxamer for drug delivery
复制标题
由羧甲基壳聚糖和泊洛沙姆组成的基于纳米结构脂质载体的 pH 和温度双响应水凝胶用于药物递送
DOI：
10.1016/j.ijbiomac.2018.03.117
复制
发表时间：
2018-07-15
影响因子：
8.2
通讯作者：
Li, Sanming
中科院分区：
文献类型：
--
作者：
Yu, Yibin;Feng, Ruoxi;Li, Sanming
本研究的目的是开发一种新型的纳米结构脂质载体（NLC）为基础的双重响应水凝胶的眼部药物输送的槲皮素（QN）。采用熔融乳化结合超声技术制备了槲皮素负载纳米液晶（QN-NLC）。采用三因素五水平中心组合设计对QN-NLC的处方进行优化。优化后的QN-NLC粒径为75.54 nm，粒径分布窄，包封率高（97.14%）。此外，通过与天然存在的无毒交联剂京尼平（GP）的交联反应，构建了由羧甲基壳聚糖（CMCS）和泊洛沙姆407（F127）组成的pH和温度双响应水凝胶。FT-IR结果表明，成功合成了F127/CMCS水凝胶。SEM分析和溶胀实验结果表明，F127/CMCS水凝胶具有温度响应性和pH响应性。从体外释放研究的结果，证明了水凝胶的双重温度和pH响应性，并且在3天内从基于QN-NLC的水凝胶（QN-NLC-Gel）释放80.52%的总槲皮素，表明QN-NLC-Gel可持续地释放药物。总之，开发的基于NLC的水凝胶是用于眼科应用的有前途的药物递送系统。(C)2018爱思唯尔B. V.保留所有权利。
The aim of this study was to develop a novel nanostructured lipid carrier (NLC) based dual-responsive hydrogel for ocular drug delivery of quercetin (QN). NLC loaded with quercetin (QN-NLC) was prepared using melt emulsification combined with ultra-sonication technique. A three-factor five-level central composite design (CCD) was employed to optimize the formulation of QN-NLC. The optimized QN-NLC presented a particle size of 75.54 nm with narrow size distribution and high encapsulation efficiency (97.14%).QN-NLC was characterized by TEM and DSC. In addition, a pH and temperature dual-responsive hydrogel composed of carboxymethyl chitosan (CMCS) and poloxamer 407(F127) was constructed by a cross-linking reaction with a naturally occurring nontoxic crosslinking agent genipin (GP). FT-IR was employed to demonstrate that F127/CMCS hydrogel was successfully synthesized. The results of SEM analysis and swelling experiments indicated that F127/CMCS hydro gel was both temperature-responsive and pH-responsive. From the results of In vitro release studies, dual temperature and pH responsiveness of the hydrogel was demonstrated, and 80.52% of total quercetin was released from the QN-NLC based hydrogel (QN-NLC-Gel) within 3 days, revealing QN-NLC-Gel released drug sustainably. Taken together, the developed NLC-based hydrogel is a promising drug delivery system for the ophthalmic application. (C) 2018 Elsevier B.V. All rights reserved.