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发明公开
CN104971044A 一种米托蒽醌雌激素靶向PEG修饰脂质体及其应用 无效 - 驳回

一种米托蒽醌雌激素靶向PEG修饰脂质体及其应用
摘要：
本发明公开了一种抗癌药物雌激素靶向PEG修饰脂质体制备方法和用途。该脂质体是通过以下方法制备得到的：将活化的雌酮合成为雌酮-聚乙二醇化磷脂，然后取40～80重量份的磷脂，5～45重量份的胆固醇，5～40重量份的聚乙二醇化磷脂溶于甲醇，旋转蒸发后加入硫酸铵水溶液，透析，加入0.5～10重量份的米托蒽醌孵育，透析，再加入0.1～20重量份的雌酮-聚乙二醇化磷脂孵育，过膜后得脂质体制剂。与现有技术相比，所获得雌激素靶向PEG修饰脂质体包封率高、粒径均一、药动学行为改善、抗肿瘤疗效增强、毒性降低；并且制备工艺简单，易于放大生产，有望成为癌症治疗的新型药物制剂。其用途在于靶向治疗乳腺癌、白血病等癌症。
摘要（英）：

The present invention discloses a preparation method and uses of an anti-cancer drug estrogen targeting PEG-modified liposome. The liposome preparation method comprises: synthesizing estrone-pegylated phospholipid from activated estrone, taking 40-80 parts by weight of phospholipid, 5-45 parts by weight of cholesterol, and 5-40 parts by weight of pegylated phospholipid, dissolving in methanol, carrying out rotary evaporation, adding an ammonium sulfate aqueous solution, carrying out dialysis, adding 0.5-10 parts by weight of mitoxantrone, carrying out incubation, carrying out dialysis, adding 0.1-20 parts by weight of the estrone-pegylated phospholipid, carrying out incubation, and filtering with a membrane to obtain the liposome preparation. Compared with the liposome in the prior art, the obtained estrogen targeting PEG-modified liposome has characteristics of high encapsulation efficiency, uniform particle size, pharmacokinetics improving, anti-tumor efficacy enhancing, toxicity reducing, simple preparation process and easy scale-up production, and is expected to become the novel pharmaceutical preparation for cancer therapy. The uses are targeted treatments of breast cancer, leukemia and other cancers.

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