DSAPM Lab and PCFM Lab, School of Materials Science and Engineering, School of Chemistry, Sun Yat-sen University, Guangzhou 510275, China.
Department of Otorhinolaryngology Head and Neck Surgery, Zhuhai City People's Hospital, Jinan University, Zhuhai 519000, China.
Mater Sci Eng C Mater Biol Appl. 2020 Apr;109:110636. doi: 10.1016/j.msec.2020.110636. Epub 2020 Jan 7.
Though curcumin has potential treatment value for most chronic diseases, it exerts little potency in the clinic because of its low aqueous solubility, high chemical instability and poor pharmacokinetics. To enhance its potency, we developed a zein-based micelle as a nanocarrier to encapsulate curcumin. Herein, superhydrophilic zwitterionic polymers, poly(sulfobetaine methacrylate) (PSBMA), were conjugated to zein to obtain an amphiphilic zein-PSBMA conjugate. These conjugates could self-assemble into micelles composed of antifouling PSBMA shells and zein cores. The results from the cytokine secretion assay showed that the micelles induced a low level of macrophage activation. Moreover, the results from the in vivo fluorescence imaging experiment confirmed their long-circulating property, exceeding 72 h in mice. In comparison with native curcumin, micelle-encapsulated curcumin had a 230-fold increase in stability in vitro, and its half-life was 22-fold longer, according to a pharmacokinetic study on mice. Overall, this work presents a zein-PSBMA micelle with a long circulation time as a useful nanocarrier for effective curcumin delivery.
尽管姜黄素对大多数慢性疾病具有潜在的治疗价值，但由于其水溶性低、化学稳定性差和药代动力学差，在临床上的效果甚微。为了提高其效力，我们开发了一种基于玉米醇溶蛋白的胶束作为纳米载体来包封姜黄素。在这里，超亲水两性离子聚合物聚（磺酸甜菜碱甲基丙烯酸酯）（PSBMA）被共轭到玉米醇溶蛋白上，以获得两亲性玉米醇溶蛋白-PSBMA 缀合物。这些缀合物可以自组装成由抗污 PSBMA 壳和玉米醇溶蛋白核组成的胶束。细胞因子分泌测定的结果表明，胶束诱导了低水平的巨噬细胞活化。此外，体内荧光成像实验的结果证实了它们的长循环特性，在小鼠体内超过 72 小时。与天然姜黄素相比，胶束包封的姜黄素在体外稳定性提高了 230 倍，根据对小鼠的药代动力学研究，其半衰期延长了 22 倍。总的来说，这项工作提出了一种具有长循环时间的玉米醇溶蛋白-PSBMA 胶束作为一种有效的姜黄素递送的有用纳米载体。
