摘要
应用薄膜法制备小单层脂质体，阿霉素包封率为３８．４３％±３．４６％，平均每个单抗携带阿霉素分子９．６个，每个单抗携带脂质体阿霉素分子３３６个。应用ＡＤＭ、ＡＤＭ脂质体、ＭｃＡｂ－ＡＤＭ－脂质体各４ｍｇ／４ｍｌ，分别给三组家兔腹腔注射。结果发现腹腔组织中，ＡＵＣ（μｇ·ｈｒ／ｇ）０～２４在脂质体ＡＤＭ组为３１１．９３３，ＡＤＭ组为１１１．８６（Ｐ＜０．０１）。心肌组织中ＡＵＣ（μｇ·ｈｒ／ｇ）０～２４在ＡＤＭ组为７５．３３，脂质全ＡＤＭ组为１１．２９（Ｐ＜０．０１）。说明脂体ＡＤＭ腹腔注射后能在腹腔组织中形成较高浓度，心肌组织内浓度较低，有利于提高化疗效果，降低心肌毒性。
We used thin membrane method to prepare small unilamellar liposomes,the encapsulated percentage of ADM was 38.43±3。46% and every McAb carried 9.6 free ADM molecules and 336 lipsome ADM molecules.ADM,ADM McAb ADM liposome (4mg/4ml)were injected into the peritoneal cavity of rabbits randomised into three groups.ADM AUC 0～24 in the liposome was 311.93 ug.hr/g in peritoneal tissues,a signficant difference was found in comparison with free ADM(111.86ug.hr/g)(p<0.01).In cardiac free ADM AUC 0～24 in the liposome was 11.9hr/g,a significant difference was found in comparision with free ADM(75.33ug.hr/g)(P<0.01).The higher ADM concentration in peritoneal tissues and the lower in cardial tissues.The method can enhance the effect of target therapy and reduce the cardiac toxity.
