Department of Medicinal Chemistry and Natural Products, Faculty of Medicine, School of Pharmacy, The Hebrew University in Jerusalem, Jerusalem, Israel.
J Biomed Mater Res A. 2010 Mar 15;92(4):1283-91. doi: 10.1002/jbm.a.32429.
The effectiveness of an injectable polymeric formulation, based on poly(sebacic acid-co-ricinoleic acid) and paclitaxel against a heterotopic tumor model was studied. An injectable pasty polymer that releases an incorporated drug over a period of weeks was used. The degradation rate of formulations with paclitaxel was examined in vitro and in vivo. The effectiveness of the polymeric carrier of paclitaxel was investigated using a melanoma heterotopic model in C57BL/6 mice. Tumor bearing animals were injected intratumorally with 0.1 ml of formulations containing 5%, 10%, 15%, and 20% paclitaxel. Formulations with 5% and 10% paclitaxel content degraded faster in vivo then in vitro. Changes in tumor progression, survival time, and body weight were observed over a period of 77 days. The highest tumor size was reported for the control groups that did not receive paclitaxel in their treatment regiment: 3.6 g on day 20, while in all groups treated with polymer loaded with paclitaxel the tumor size was much smaller than that in the blank polymer or non treatment groups and ranged from 1.3 g to 0.3 g. Intratumoral injection of paclitaxel loaded in the polymer was found to be an effective treatment for localized tumors.
研究了一种基于聚(癸二酸-co-蓖麻酸)和紫杉醇的可注射聚合物制剂对异位肿瘤模型的疗效。使用了一种可注射的糊状聚合物,它可以在数周内释放所包含的药物。在体外和体内研究了含有紫杉醇的制剂的降解速率。使用 C57BL/6 小鼠的黑色素瘤异位模型研究了紫杉醇聚合物载体的有效性。荷瘤动物瘤内注射 0.1 毫升含有 5%、10%、15%和 20%紫杉醇的制剂。5%和 10%紫杉醇含量的制剂在体内的降解速度快于体外。在 77 天的时间内观察到肿瘤进展、生存时间和体重的变化。未接受紫杉醇治疗的对照组报告的肿瘤最大尺寸最大:第 20 天为 3.6 克,而所有接受载有紫杉醇的聚合物治疗的组的肿瘤尺寸均小于空白聚合物或未治疗组,范围从 1.3 克到 0.3 克。研究发现,紫杉醇在聚合物中的瘤内注射是治疗局部肿瘤的有效方法。