摘要
研究目的是提高脂质体的稳定性，延长在血循环中的时间，增强在非ＲＥＳ部位的靶向性。将不同分子量的ＰＥＧ－ＰＥ（聚乙二醇单甲醚磷脂酰乙醇胺衍生物）掺入脂质体，比较其在体外的稳定性和体内的分布情况。结果表明，该类脂质体在血循环中的滞留时间显著延长。并且与ＰＥＧ的分子量有密切关系。本研究方法简便易行，从而省去同位素标记的困难，具有良好的应用前景。
PEG-PE(polyethylene glycol-phosphatidyl ethanolamine)of different molecularweight(2000 and 5 000)were used to medify the membrane of liposomes.Large unilamellarliposomes containing PEG-PE were prepared by reversed phase evaporation,Fluorescent label-calceinwas encapsulated at the internal water phase.To compare the differance between the medified and unmedified membrane,the stability in vitro and distribution in vivo were investigated.The results indicated that the circulation half-life forliposomes unmedified, modified by PEG(2000)-PE and modified by PEG(5000)-PE were 13,21and 75(min)respectively.At 6 h after injection,the ratio b/R(b:distribution in blood,R:distribution in liver and spleen)were 0,0.8 and 1.4,respectively. The results mean that the stability incrcased and circulation time was prolonged by the PEG-PEmedified membrane,The effect of PEG-PE on membrane was found to be directly proportional to thechain length of the polymer.
出处
《药学学报》
CAS
CSCD
北大核心
1996年第6期451-454,共4页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
