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目的研制紫杉醇聚合物胶束(PTX PM)和白蛋白紫杉醇聚合物胶束(HSA-PTX PM)制剂,比较该两组制剂与市售紫杉醇注射液(PTX injection)的抑瘤效果。方法用激光动态光散射粒度仪检测这两组制剂的粒度分布,透射电镜观察粒子形态。采用传统抑瘤率实验方法和活体动物成像技术方法同时评价抑瘤效果。建立荷B16黑色素瘤C57小鼠模型,考察制剂组对小鼠生存期的影响。结果 2种制剂的粒径有效光强粒径均在100 nm左右。透射电镜显示粒子呈圆整的球形。活体成像图片显示PTX PM和HSA-PTX PM制剂的抑瘤效果优于PTX injection,其中HSA-PTX PM的抑瘤效果更佳。HSA-PTX PM的抑瘤率为72.92%,优于PTX PM(66.49%),明显优于PTX injection(47.68%)(P<0.05)。用传统实验方法计算得到的结果基本一致。生存期实验显示,与市售相比HSA-PTX PM更能延长荷瘤小鼠的平均生存期。结论 PTX PM和HSA-PTX PM的抑瘤效果要优于市售紫杉醇注射液,并且HSA-PTX PM更优。聚合物胶束和白蛋白两种载体联用在抗肿瘤药物制剂技术领域有很好的发展前景。
OBJECTIVE To study the antitumor effects of paclitaxel polymer micelles (PTX PM) and albumin paclitaxel polymer micelles (HSA-PTX PM), and to compare the antitumor effects of the two formulations with PTX injection. Methods The particle size distribution of the two preparations was detected by laser light scattering particle size analyzer. The morphology of the particles was observed by transmission electron microscope. The antitumor effect was evaluated simultaneously by the traditional method of inhibiting tumor rate and living animal imaging technique. B16 melanoma C57 mice model was established to investigate the effect of the preparation group on the survival of mice. Results The effective particle size of the two formulations were all about 100 nm. Transmission electron microscopy showed spherical particles are round. In vivo imaging showed that the anti-tumor effect of PTX PM and HSA-PTX PM preparations was better than that of PTX injection, and the anti-tumor effect of HSA-PTX PM was better. The inhibition rate of HSA-PTX PM was 72.92%, which was better than that of PTX PM (66.49%), which was significantly better than that of PTX injection (47.68%) (P <0.05). The results obtained by traditional experimental methods are basically the same. Survival experiments showed that HSA-PTX PM prolongs the mean survival of tumor-bearing mice more than is commercially available. Conclusions The antitumor effects of PTX PM and HSA-PTX PM are better than those of paclitaxel injection, and HSA-PTX PM is better. Polymer micelles and albumin carrier in combination with the antitumor pharmaceutical technology has good prospects.