Micelles as Carriers for Poorly Soluble Drugs: Preparation and Anticancer Activity In Vitro of Paclitaxel in Mixed Micelles of PEG-PE and Positively Charged Lipids

摘要

Mixed micelles (MM) consisting of poly (ethylene glycol)-phosphatidylethanolamine conjugates (PEGPE) and cationic Lipofectin? lipids (LL) and loaded with paclitaxel (MM-PT) were prepared. The average size of such micelles was ca. 98 nm, zeta-potential ca. -6 mV, and paclitaxel content ca. 4 wt %. In vitro cytotoxicity of MM-P was significantly greater than that of free paclitaxel (PT) or paclitaxel in LL-free PEG-PE micelles (M-PT). MM seem to be able to escape from endosomes and deliver the drug into the cytoplasm of cancer cells.