Wuya College of Innovation, Shenyang Pharmaceutical University , Shenyang , China.
Department of Pharmacology, Shenyang Pharmaceutical University , Shenyang , China.
Drug Dev Ind Pharm. 2019 Nov;45(11):1788-1798. doi: 10.1080/03639045.2019.1660365. Epub 2019 Sep 10.
Ternary mixed micelles constituted of Soluplus, sodium cholate, and phospholipid were prepared as nano-delivery system of the anticancer drug, docetaxel. The formulation of docetaxel-loaded ternary mixed micelles (DTX-TMMs) with an optimized composition (Soluplus/sodium cholate/phospholipid= 3:2:1 by weight) were obtained. The main particle size of DTX-TMMs was 76.36 ± 2.45 nm, polydispersity index (PDI) was 0.138 ± 0.039, and the zeta potential was -8.46 ± 0.55 mv. The encapsulation efficiency was 94.24 ± 4.30% and the drug loading was 1.25%. The critical micelle concentration value was used to assess the ability of carrier materials to form micelles. The results indicated that the addition of Soluplus to sodium cholate-phospholipid mixed micelles could reduce the critical micelle concentration and improve the stability. release studies demonstrated that compared with DTX-Injection group, the DTX-TMMs presented a controlled release property of drugs. pharmacodynamics results suggested that DTX-TMMs had the most effective inhibitory effect on tumor proliferation and had good biosafety. In addition, the relative bioavailability of mixed micelles was increased by 1.36 times compared with the DTX-Injection pharmacokinetic study indicated that a better therapeutic effect could be achieved. In summary, the ternary mixed micelles prepared in this study are considered to be promising anticancer drug delivery systems.
由 Soluplus、胆酸钠和磷脂组成的三元混合胶束被制备为抗癌药物多西他赛的纳米递药系统。用优化的组成(Soluplus/胆酸钠/磷脂=3:2:1 重量比)制备载多西他赛的三元混合胶束(DTX-TMMs)的制剂。DTX-TMMs 的主要粒径为 76.36±2.45nm,多分散指数(PDI)为 0.138±0.039,zeta 电位为-8.46±0.55mv。包封效率为 94.24±4.30%,载药量为 1.25%。临界胶束浓度值用于评估载体材料形成胶束的能力。结果表明,向胆酸钠-磷脂混合胶束中添加 Soluplus 可以降低临界胶束浓度并提高稳定性。释放研究表明,与 DTX-Injection 组相比,DTX-TMMs 表现出药物的控制释放特性。药效学结果表明,DTX-TMMs 对肿瘤增殖具有最有效的抑制作用,且具有良好的生物安全性。此外,与 DTX-Injection 相比,混合胶束的相对生物利用度提高了 1.36 倍。药代动力学研究表明,可实现更好的治疗效果。综上所述,本研究制备的三元混合胶束被认为是有前途的抗癌药物递药系统。
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