【摘要】 制备多西他赛pH敏感脂质体(DTX-PSL)并对其理化性质进行考察。采用薄膜分散法,以磷脂酰乙醇胺(PE)、胆固醇(CHOL)、亚油酸(LA)为载体材料,通过正交实验筛选出最优处方。并且对制剂的包封率(EE%)、载药量(DL%)、重现性、外观形态、粒径分布、Zeta电位及体外释放进行考察。结果表明制备的DTX-PSL EE%为(81.9±2.2)%,DL%为(4.8±0.1)%,平均粒径为146.4 nm,Zeta电位为-35.19 mV,体外释放表现出制剂的显著pH敏感性。DTX-PSL具有较高EE%、DL%及显著p H敏感性,是一种较为理想的载药体系。更多还原

【Abstract】 To prepare and investigate the physico-chemical properties of the p H sensitive liposome( DTX-PSL) as novel drug delivery systems,p H sensitive liposome was composed of phosphatidyl ethanolamine( PE),cholesterol( CHOL) and linoleic acid( LA). The p H sensitive liposome was prepared by the thin-film evaporation method. The novel preparation was also estimated by encapsulation efficiency( EE%),drug loading capacity( DL%),reproducibility,appearance,diameter distribution,Zeta potential and the appreance of release in vitro of the liposomes. The results suggested that DTX-PSL EE% was( 81. 9 ± 2. 2) % and DL% was( 4. 8 ± 0. 1) %. Mean diameter and Zeta potential were about 146. 4 nm and-35. 19 m V respectively. There was a highlighted burst effect of DTX from DTX-PSL in p H 5. 0 releasing medium compared with p H 7. 4 releasing medium,but no significant difference was found of DTX from Doupafei in different p H releasing medium. In vitro release experiment showed that the clever DTX-PSL had a significant p H sensitivity. DTX-PSL may be a potential drug delivery system with good EE% 、DL% and a significant p H sensitivity.更多还原