Responsive nanogels for application as smart carriers in endocytic pH-triggered drug delivery systems
Responsive nanogels for application as smart carriers in endocytic pH-triggered drug delivery systems
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DOI：
10.1016/j.eurpolymj.2016.02.022
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发表时间：
2016-05-01
影响因子：
6
通讯作者：
Marcelino Gugliotta, Luis
中科院分区：
文献类型：
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作者：
Cesar Cuggino, Julio;Molina, Maria;Marcelino Gugliotta, Luis
采用沉淀/分散聚合法合成了不同NIPA/AAc摩尔比的聚（N-异丙基丙烯酰胺-co-丙烯酸）（NIPA-co-AAc）纳米凝胶（NG），并将其作为盐酸阿霉素（DOXO-HCl）药物释放系统（DDS）的载体。如动态光散射（DLS）所示，NG在生理环境（pH 7.4和5，37 ℃）中表现出优异的分散性。此外，由于阳离子药物与阴离子NG的离子相互作用，NG表现出高的载药能力和效率。NG-DOXO-HCl制剂在37 ℃下在血浆模拟介质（pH 7.4和0.14 M NaCl）中表现出优异的水中分散性和最小的货物泄漏，并在溶酶体模拟介质（pH 5和0.14 M NaCl）中触发释放。这种释放行为连同它们的大小和通过MTT测定确定的低细胞毒性一起将这些NG转化为它们作为癌症治疗中的载体的应用的最佳候选者，所述癌症治疗基于在肿瘤细胞中内吞作用后具有药物pH触发释放的增强的渗透性和保留效应（EPR）。(C)2016爱思唯尔有限公司版权所有
Various specially designed poly(N-isopropylacrylamide-co-acrylic acid) (NIPA-co-AAc) nanogels (NGs) with different NIPA/AAc molar composition were synthesized by precipitation/dispersion polymerization and evaluated as carriers for drug delivery systems (DDSs) of doxorubicin hydrochloride (DOXO-HCl) for cancer therapies. The NGs presented excellent dispersability in physiological environments (pH 7.4 and 5 at 37 degrees C), as shown by dynamic light scattering (DLS). Moreover, the NGs exhibited high drug loading capacity and efficiency due to the ionic interaction of the cationic drug with the anionic NGs. NG-DOXO-HCl formulation presented excellent dispersability in water and minimal leakage of the cargo at plasma simulated medium (pH 7.4 and 0.14 M NaCl) at 37 degrees C and.a triggered release at lysosomal simulated medium (pH 5 and 0.14 M NaCl). This release behavior together with their size and the low cytotoxicity determined by the MTT assay converts these NGs in great candidates for their application as carriers in cancer therapies based on the enhanced permeability and retention effect (EPR) with drug pH-triggered release after endocytosis in tumor cells. (C) 2016 Elsevier Ltd. All rights reserved.