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，化学稳定性高和药代动力学差，因此在临床上几乎没有效力。为了增强其效力，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封装姜黄素。在此，将超亲水性两性离子聚合物聚甲基磺基甜菜碱（PSBMA）与玉米醇溶蛋白共轭以获得两亲性玉米醇溶蛋白-PSBMA共轭物。这些结合物可以自组装成由防污PSBMA外壳和玉米醇溶蛋白核心组成的胶束。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。而且，来自体内的结果荧光成像实验证实了它们的长循环特性，在小鼠中超过72小时。根据对小鼠的药代动力学研究，与天然姜黄素相比，胶束包裹的姜黄素在体外的稳定性提高了230倍，半衰期延长了22倍。总的来说，这项工作提出了具有长循环时间的玉米醇溶蛋白-PSBMA胶束，作为有效姜黄素递送的有用纳米载体。