采用“点击”化学技术制备的用于结肠靶向药物传递应用的双 pH/温度响应性壳聚糖基水凝胶。
Dual pH-/thermo-responsive chitosan-based hydrogels prepared using "click" chemistry for colon-targeted drug delivery applications.
机构信息
Department of Smart Green Technology Engineering, Pukyong National University, Busan, 48513, South Korea.
Department of Biomedical Engineering, Pukyong National University, Busan, 48513, South Korea.
出版信息
Carbohydr Polym. 2021 May 15;260:117812. doi: 10.1016/j.carbpol.2021.117812. Epub 2021 Feb 24.
A dual pH-/thermo-responsive hydrogel was designed based on a polyelectrolyte complex of polyacrylic acid (PAA) and norbornene-functionalized chitosan (CsNb), which was synergized with chemical crosslinking using bistetrazine-poly(N-isopropyl acrylamide) (bisTz-PNIPAM). The thermo-responsive polymeric crosslinker, bisTz-PNIPAM, was synthesized via reversible addition-fragmentation transfer polymerization of NIPAM. FTIR, XRD, rheological and morphological analyses demonstrated the successful formation of the polyelectrolyte network. The highly porous structure generated through the in-situ "click" reaction between Tz and Nb resulted in a higher drug loading (29.35 %). The hydrogel (COOH/NH mole ratio of 3:1) exhibited limited drug release (8.5 %) of 5-ASA at a pH of 2.2, but it provided an almost complete release (92 %) at pH 7.4 and 37 °C within 48 h due to the pH responsiveness of PAA, hydrogel porosity, and shrinkage behavior of PNIPAM. The hydrogels were biodegradable and non-toxic against human fibroblast cells, suggesting their considerable potential for a colon-targeted drug delivery system.
设计了一种基于聚丙烯酸（PAA）和降冰片烯功能化壳聚糖（CsNb）的聚电解质复合物的双 pH-/温度响应水凝胶，该水凝胶通过双四嗪-聚（N-异丙基丙烯酰胺）（bisTz-PNIPAM）的化学交联协同作用得到增强。温敏性聚合物交联剂 bisTz-PNIPAM 通过 NIPAM 的可逆加成-断裂链转移聚合合成。FTIR、XRD、流变和形态分析证明了聚电解质网络的成功形成。Tz 和 Nb 之间的原位“点击”反应产生的高度多孔结构导致更高的药物负载（29.35%）。水凝胶（COOH/NH 摩尔比为 3:1）在 pH 2.2 时仅释放 5-ASA 的有限药物（8.5%），但在 pH 7.4 和 37°C 下在 48 小时内几乎完全释放（92%），这归因于 PAA 的 pH 响应性、水凝胶的多孔性和 PNIPAM 的收缩行为。水凝胶可生物降解且对人成纤维细胞无毒，表明其在结肠靶向药物递送系统方面具有很大的潜力。
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