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用于姜黄素递送的双pH和温度敏感型聚(N-异丙基丙烯酰胺-共-烯丙胺)纳米凝胶:溶胀-消溶胀行为及相变机制

Dual pH- and Thermo-Sensitive Poly(N-isopropylacrylamide-co-allylamine) Nanogels for Curcumin Delivery: Swelling-Deswelling Behavior and Phase Transition Mechanism.

作者信息

Santhamoorthy Madhappan, Kim Seong-Cheol

机构信息

School of Chemical Engineering, Yeungnam University, Gyeongsan 38541, Republic of Korea.

出版信息

Gels. 2023 Jul 1;9(7):536. doi: 10.3390/gels9070536.

DOI:10.3390/gels9070536
PMID:37504415
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10379092/
Abstract

Curcumin (Cur) is a beneficial ingredient with numerous bioactivities. However, due to its low solubility and poor bioavailability, its therapeutic application is limited. In this work, we prepared poly-N-isopropylacrylamide p(NIPAm) and polyallylamine p(Am)-based nanogel (p(NIPAm-co-Am)) NG for a dual pH- and temperature-sensitive copolymer system for drug delivery application. In this copolymer system, the p(NIPAm) segment was incorporated to introduce thermoresponsive behavior and the p(Am) segment was incorporated to introduce drug binding sites (amine groups) in the resulting (p(NIPAm-co-Am)) NG system. Various instrumental characterizations including H nuclear magnetic resonance (H NMR) spectroscopy, Fourier transform infrared (FT-IR) analysis, scanning electron microscopy (SEM), zeta potential, and particle size analysis were performed to confirm the copolymer synthesis. Curcumin (Cur), an anticancer bioactive substance, was employed to assess the in vitro drug loading and release performance of the resulting copolymer nanogels system at varied pH levels (pH 7.2, 6.5, and 4.0) and temperatures (25 °C, 37 °C, and 42 °C). The cytocompatibility of the p(NIPAm-co-Am) NG sample was also tested on MDA-MB-231 cells at various sample concentrations. All the study results indicate that the p(NIPAm-co-Am) NG produced might be effective for drug loading and release under pH and temperature dual-stimuli conditions. As a result, the p(NIPAm-co-Am) NG system has the potential to be beneficial in the use of drug delivery applications in cancer therapy.

摘要

姜黄素(Cur)是一种具有多种生物活性的有益成分。然而,由于其低溶解度和低生物利用度,其治疗应用受到限制。在本研究中,我们制备了基于聚N-异丙基丙烯酰胺p(NIPAm)和聚烯丙胺p(Am)的纳米凝胶(p(NIPAm-co-Am))NG,用于药物递送应用的双pH和温度敏感共聚物系统。在该共聚物系统中,引入p(NIPAm)链段以引入热响应行为,引入p(Am)链段以在所得的(p(NIPAm-co-Am))NG系统中引入药物结合位点(胺基)。进行了各种仪器表征,包括氢核磁共振(H NMR)光谱、傅里叶变换红外(FT-IR)分析、扫描电子显微镜(SEM)、zeta电位和粒径分析,以确认共聚物的合成。使用抗癌生物活性物质姜黄素(Cur)评估所得共聚物纳米凝胶系统在不同pH水平(pH 7.2、6.5和4.0)和温度(25°C、37°C和42°C)下的体外药物负载和释放性能。还在不同样品浓度下对MDA-MB-231细胞测试了p(NIPAm-co-Am)NG样品的细胞相容性。所有研究结果表明,所制备的p(NIPAm-co-Am)NG在pH和温度双刺激条件下可能对药物负载和释放有效。因此,p(NIPAm-co-Am)NG系统在癌症治疗的药物递送应用中具有潜在的益处。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7571/10379092/71d5b902ff9a/gels-09-00536-sch002.jpg
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