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Formulation of liposomal taxol and process development

机译:脂质紫杉醇的配方和工艺开发

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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:紫杉醇是一种有效的抗癌剂,已被用作抗乳腺癌和卵巢癌的一线药物。然而,由于其低水溶性和当前注射用赋形剂(Cremophore EL)的高炎症反应,该应用受到了限制。〜1因此,为消除其在给药过程中的副作用做出了许多努力。〜2,3,4这些方法中,脂质体被认为是最有希望的药物载体。尽管脂质体有一些缺点,例如紫杉醇的含量有限和长期稳定性,但它似乎具有生物相容性,并被认为可以降低毒性而不改变其对肿瘤细胞的功效。2,3此外,脂质体易于修饰以改善脂质体的稳定性。表面性质和/或与特殊的配体组装在一起,这有可能增加体内循环时间和对肿瘤细胞的亲和力。因此,本研究开发了一种脂质体制剂,该脂质体制剂能够以高含量掺入紫杉醇并通过用MPEG修饰脂质体来改善循环时间。

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