NANO ANTICANCER MICELLES OF VINCA ALKALOIDS ENTRAPPED IN POLYETHYLENE GLYCOLYLATED PHOSPHOLIPIDS

摘要

Injectable nano micelles of anticancer agents which contain vinca alkaloids as the actives, namely Vinbastine, Vincrisitin, Vindesine, Vinorelbine, in a therapeutically effective amount, and polyethylene glycolylated phospholipids as well as pharmaceutically acceptable adjuvants. The manufacturing method comprises preparing the injectable nano micelles of vinca alkaloids by encapsuling them into pre-formed nano micelles. Vinca alkaloids and polyethylene glycol-derived phospholipids form the nano micelles of uniform particle size distribution. The polyethylene glycol molecules form a hydrophilic overlayer around the hydrophobic core of the loaded therapeutic agents. And this overlayer serves to protect the drugs of interest from the interaction with certain proteins in the blood, such as enzymes, and from being recognized and phagocytized by the internal reticuloendothelial system, which allow for achieving longevity in circulation in vivo. In addition, the micelles further increase the storage stability and efficacy against cancers with a lower toxicity.