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Formulation of liposomal taxol and process development

机译:制剂脂质体紫杉醇和过程开发

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Paclitaxel, an effective anticance agent, has been applied as the first-line drug against breast and ovarian cancers. However, this application is limited owing to its low water solubility and high inflammatory response of the current excipient (Cremophore EL) for injection.~1 Thus, efforts to eliminate its side effects during administration have been numerous.~2,3,4 Among those methods, liposome is regarded as the most promising drug carrier. Despite a few drawbacks of liposome, such as limited paclitaxel content and long term stability, it appears to be biocompatible and has been speculated to decrease toxicity without changing its efficacy against tumor cells.~2,3 Besides, liposome is easily modified to improve the surface property and/or assemble with special ligands, which has the potential to increase circulation time in body and affinity to tumor cells. Therefore, this study develops a liposomal formulation capable of incorporating paclitaxel with high content and improving circulation time by embellishing liposome with MPEG.
机译:紫杉醇,有效anticance剂,已被应用于作为对乳腺癌和卵巢癌的一线药物。然而,该申请是由于它的低的水溶性和当前赋形剂(克列莫佛EL)用于注射的高炎症反应的限制。〜1因此,努力消除施用期间其副作用得到了众多。〜2,3,4在这些方法,脂质体被认为是最有前途的药物载体。尽管脂质体的一些缺点,如有限的紫杉醇含量和长期稳定性,这似乎是生物相容的和被推测以降低毒性,而不会针对肿瘤细胞的改变其效果。〜2,3此外,脂质体容易地修改,以提高表面性质和/或装配的特殊的配体,其具有增加的循环时间在身体和亲和力的肿瘤细胞的潜力。因此,本研究开发能够合并具有高含量紫杉醇,并通过与MPEG美化脂质体改善循环时间的脂质体制剂。

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