Layek Buddhadev, Mukherjee Biswajit
Department of Pharmaceutical Technology, Division of Pharmaceutics, Jadavpur University, Kolkata-700032, India.
Sci Pharm. 2010 Jul-Sep;78(3):507-15. doi: 10.3797/scipharm.0911-11. Epub 2010 Jul 12.
The present study was designed for the development of a stable sustained release liposomal drug delivery system for tamoxifen citrate (TC) using soya phosphatidylcholine (SPC), cholesterol (CH) and span 20 as main ingredients. Liposomes were prepared by formation of thin lipid film followed by hydration. The mean vesicle diameter was found to be 203.5 Â 19.5 nm with 21% of the liposomal population having average diameter below 76.72 Â 6.7 nm. There was a good vesicular distribution with the polydispersity index of 0.442 Â 0.03. The maximum loading of drug was determined to be 53.60% of the initial amount that is 34.58 Îg of drug per mg of lipid. Amongst the different storage conditions, liposomes stored at 2â8ÂC were found to be most stable and only 4% of the drug was lost over the storage period of 5 weeks. In vitro release studies of liposomes showed that 50% of drug was released within 3 hours (h) whereas 95% drug was released in 30 h. This indicates the usefulness of the liposomal delivery system for sustaining the in vitro release of tamoxifen citrate.
本研究旨在开发一种以大豆磷脂酰胆碱（SPC）、胆固醇（CH）和司盘20为主要成分的用于柠檬酸他莫昔芬（TC）的稳定缓释脂质体药物递送系统。通过形成脂质薄膜然后水化来制备脂质体。发现平均囊泡直径为203.5±19.5nm，21%的脂质体群体平均直径低于76.72±6.7nm。囊泡分布良好，多分散指数为0.442±0.03。药物的最大载药量确定为初始量的53.60%，即每毫克脂质含34.58μg药物。在不同的储存条件中，发现储存在2-8℃的脂质体最稳定，在5周的储存期内仅损失4%的药物。脂质体的体外释放研究表明，50%的药物在3小时内释放，而95%的药物在30小时内释放。这表明脂质体递送系统对于维持柠檬酸他莫昔芬的体外释放是有用的。
