Invention Grant
US08765181B2 Nano anticancer micelles of vinca alkaloids entrapped in polyethylene glycolylated phospholipids 有权
长春花生物碱的纳米抗癌胶束包埋在聚乙二醇乙酰化磷脂中

Nano anticancer micelles of vinca alkaloids entrapped in polyethylene glycolylated phospholipids
Abstract:
The present invention provides a nano-micellar preparation containing vinca alkaloids antitumor agent for intravenous injection, which cincludes a therapeutically effective amount of vinca alkaloids antitumor agent (vinblastine, vincristine, vindesine and vinorelbine), a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants. The preparation is prepared by encapsulating the medicament with a nano-micelle to obtain the nano-micellar preparation containing vinca alkaloids antitumor agent for injection. The vinca alkaloids antitumor agent and the phosphatide derivatized with polyethylene glycol form a nano-micelle with a highly uniform particle size. In the micelle, the hydrophobic core of encapsulated medicament is surrounded by polyethylene glycol molecules to form a hydrophilic protective layer, so that the medicament is prevented from contacting with the enzymes and other protein molecules in blood and being recognized and phagocytozed by reticuloendothelial system in body, and the circulation time in vivo of the micelle is prolonged.
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