Mu L, Elbayoumi T A, Torchilin V P
Department of Pharmaceutical Sciences, Northeastern University, 360 Huntington Avenue Boston, MA 02115, USA.
Int J Pharm. 2005 Dec 8;306(1-2):142-9. doi: 10.1016/j.ijpharm.2005.08.026. Epub 2005 Oct 19.
Micelles from the mixture of poly(ethylene glycol)-phosphatidyl ethanolamine conjugate (PEG-PE) and d-alpha-tocopheryl polyetheyene glycol 1000 succinate (TPGS) were prepared loaded with the poorly soluble anticancer drug camptothecin (CPT). The solubilization of CPT by the mixed micelles was more efficient than with earlier described micelles made of PEG-PE alone. CPT-loaded mixed micelles were stable upon storage and dilution and firmly retained the incorporated drug. The cytotoxicity of the CPT-loaded mixed micelles against various cancer cells in vitro was remarkably higher than that of the free drug. PEG-PE/TPGS mixed micelles may serve as pharmaceutical nanocarriers with improved solubilization capacity for poorly soluble drugs.
制备了由聚乙二醇 - 磷脂酰乙醇胺共轭物(PEG - PE)和d-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)混合物形成的胶束,并负载了难溶性抗癌药物喜树碱(CPT)。与之前仅由PEG - PE制成的胶束相比,混合胶束对CPT的增溶效果更显著。负载CPT的混合胶束在储存和稀释时稳定,并能牢固保留包封的药物。负载CPT的混合胶束对多种癌细胞的体外细胞毒性显著高于游离药物。PEG - PE/TPGS混合胶束可作为对难溶性药物具有改善增溶能力的药物纳米载体。