Glyn O. Philips Hydrocolloid Research Centre at HUT, Hubei University of Technology, Wuhan 430068, PR China.
Hubei Collaborative Innovation Center for Advanced Organic Chemical Materials, Key Laboratory for the Green Preparation and Application of Functional Materials of Ministry of Education, Hubei University, Wuhan, Hubei 430062, PR China.
Carbohydr Polym. 2017 Sep 1;171:9-17. doi: 10.1016/j.carbpol.2017.04.094. Epub 2017 May 1.
Amphiphilic aliphatic amines grafted konjac glucomannan (KGM-g-AH, KGM-g-AH and KGM-g-AH) micelles were prepared via a simple two-step synthesis with Schiff's base as the "switch" to achieve intracellular acid-triggered curcumin release. The KGM-g-AH self-assembled into spherical nano-micelles (107.6±11.6nm) in an aqueous medium, and presented high curcumin loading capacity as well as good physical stability in 28 days. The in vitro curcumin release behaviors proved the controlled release property and the endosomal/lysosomal pH response of KGM-g-AH micelles. The cytotoxicity and cellular uptake studies were also investigated to exhibit the intracellular pH-sensitivity, safety and biocompatibility of KGM-g-AH micelles. This research focuses on the feasibility of KGM-based micelles to be extrapolated as promising strategies for cancer therapy and offers new potential options for intracellular drug delivery.
通过简单的两步合成，用席夫碱作为“开关”制备了双亲性脂肪族胺接枝魔芋葡甘聚糖（KGM-g-AH、KGM-g-AH 和 KGM-g-AH）胶束，实现了细胞内酸触发姜黄素释放。在水介质中，KGM-g-AH 自组装成球形纳米胶束（107.6±11.6nm），具有较高的姜黄素载药能力和 28 天内的良好物理稳定性。体外姜黄素释放行为证明了 KGM-g-AH 胶束具有控制释放性能和内体/溶酶体 pH 响应性。还研究了细胞毒性和细胞摄取，以显示 KGM-g-AH 胶束的细胞内 pH 敏感性、安全性和生物相容性。本研究重点关注基于 KGM 的胶束作为癌症治疗有前途的策略的可行性，并为细胞内药物递送提供了新的潜在选择。
