School of Pharmacy, Second Military Medical University, Shanghai, China.
Drug Dev Ind Pharm. 2011 May;37(5):597-605. doi: 10.3109/03639045.2010.533276.
A novel mixed micelle made of Tween 80 and soybean phospholipids (S80) was prepared and used as the delivery system for paclitaxel (PTX), with the purpose of improving the stability, therapeutic index, and security of PTX in comparison with Taxol® injection. The micelle size, morphological features, dilution stability, and critical micelle concentration (CMC) were measured. The in vitro antitumor activity, pharmacokinetics, and hemolysis effect of the optimal PTX-loaded mixed micelles (PTX-M) were evaluated and compared with Taxol®. The results showed that PTX-M was more stable than Taxol® upon dilution. PTX-M had a higher antitumor efficacy against HeLa and A549 cells than that of Taxol®. The plasma AUC of PTX-M was 1.3-fold higher than that of Taxol® and the hemolysis test revealed that PTX-M was safe for intravenous injection. In conclusion, PTX-M had a higher dilution stability and antitumor efficacy than Taxol®, but significantly reduced the toxicity while improving the bioavailability of PTX. Therefore, Tween 80-S80 mixed micelles could be a promising drug carrier for intravenous administration of PTX.
一种由吐温 80 和大豆磷脂（S80）组成的新型混合胶束被制备出来，并被用作紫杉醇（PTX）的递送系统，目的是提高 PTX 的稳定性、治疗指数和安全性，与 Taxol®注射液相比。测量了胶束的粒径、形态特征、稀释稳定性和临界胶束浓度（CMC）。评估了最佳紫杉醇负载混合胶束（PTX-M）的体外抗肿瘤活性、药代动力学和溶血作用，并与 Taxol®进行了比较。结果表明，PTX-M 稀释后比 Taxol®更稳定。PTX-M 对 HeLa 和 A549 细胞的抗肿瘤疗效均高于 Taxol®。PTX-M 的血浆 AUC 是 Taxol®的 1.3 倍，溶血试验表明 PTX-M 静脉注射安全。总之，PTX-M 具有比 Taxol®更高的稀释稳定性和抗肿瘤疗效，但显著降低了毒性，同时提高了 PTX 的生物利用度。因此，Tween 80-S80 混合胶束可能是 PTX 静脉给药的一种有前途的药物载体。
