Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.
Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan.
Int J Biol Macromol. 2018 Dec;120(Pt B):2579-2588. doi: 10.1016/j.ijbiomac.2018.09.034. Epub 2018 Sep 7.
Redox-sensitive micelles based onhydrophilic hyaluronic acid-ss-hydrophobic curcumin conjugate were designed as a novel delivery system for gliomas targeting. Furthermore, the obtained micelles were further functionalized with Tween 80 (CUR-THSC) for better brain penetration. Dynamic light scattering experiment and in vitro release study showed that the synthetic disulfide-linked conjugate possessed redox-sensitivity under high glutathione conditions. Spherical micelles with a mean particle size of 74.2 nm, negative zeta potential (-30.25 mV), high entrapment efficiency (94.12%) and drug loading (8.9%) were obtained. XRD analysis of micelles revealed amorphous form of the encapsulated drug. CUR-THSC micelles showed good plasma stability and did not induce any hemolysis in erythrocytes. In addition, highest cytotoxicity in G422 cells was observed compared to the free curcumin group and non-sensitive micelles group. These results indicate that the Tween 80-modified hyaluronic acid-ss-curcumin micelles could emerge as a promising platform for the delivery of curcumin in the treatment of gliomas.
基于亲水性透明质酸-ss-疏水性姜黄素缀合物的氧化还原敏感胶束被设计为用于靶向神经胶质瘤的新型递药系统。此外，所得胶束进一步用吐温 80（CUR-THSC）进行功能化以增强脑穿透。动态光散射实验和体外释放研究表明，合成的二硫键连接的缀合物在高谷胱甘肽条件下具有氧化还原敏感性。获得了平均粒径为 74.2nm、负 zeta 电位（-30.25mV）、高包封效率（94.12%）和载药量（8.9%）的球形胶束。胶束的 XRD 分析表明包封药物呈无定形形式。CUR-THSC 胶束在血浆中具有良好的稳定性，不会引起红细胞溶血。此外，与游离姜黄素组和非敏感胶束组相比，G422 细胞中观察到最高的细胞毒性。这些结果表明，Tween 80 修饰的透明质酸-ss-姜黄素胶束可能成为治疗神经胶质瘤中姜黄素递送的有前途的平台。
