Institute of Medicinal Biotechnology, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China.
Int J Pharm. 2012 Apr 4;425(1-2):53-61. doi: 10.1016/j.ijpharm.2012.01.011. Epub 2012 Jan 14.
The aim of the present study was to develop an oil-free o/w microemulsion, composed of pluronic F68, propylene glycol and saline, which solubilized poorly soluble anesthetic drug propofol for intravenous administration. The ternary diagram was constructed to identify the regions of microemulsions, and the optimal composition of microemulsion was determined by in vitro evaluation such as globule size upon dilution and rheology. The droplet size of the diluent emulsion corresponding to oil-in-water type ranged from 200 to 300nm in diameter. Stability analysis of the microemulsions indicated that they were stable upon storage for at least 6 months. Hemolysis percent of propofol microemulsions was lower than that of commercial lipid emulsion (CLE) at 4h. Acute toxicity test showed that median lethal dose of propofol microemulsion was the same as that of CLE. No significant difference in time for unconsciousness and recovery of righting reflex was observed between the prepared microemulsions and CLE. In conclusion, microemulsion would be a promising intravenous delivery system for propofol.
本研究旨在开发一种不含油的油包水乳状液，由泊洛沙姆 F68、丙二醇和生理盐水组成，可增溶脂溶性差的麻醉药物丙泊酚用于静脉给药。通过构建三元相图来确定微乳液区域，并通过体外评价（如稀释后的粒径和流变学）来确定微乳液的最佳组成。与油包水型对应的稀释乳液的液滴大小直径在 200 至 300nm 之间。微乳液的稳定性分析表明，在至少 6 个月的储存期内它们是稳定的。丙泊酚微乳液在 4 小时时的溶血百分比低于商用脂质乳剂 (CLE)。急性毒性试验表明，丙泊酚微乳液的半数致死剂量与 CLE 相同。在意识丧失和恢复翻正反射的时间方面，制备的微乳液与 CLE 之间没有观察到显著差异。总之，微乳液可能是丙泊酚有前途的静脉给药系统。
