用强化靶向材料修饰斑蟊素多相脂质体与其肝脏定向作用的实验研究

The Research on Liver Targeting Delivery System of Cantharidin Polyphase Liposome Modified by Strengthened Targeting Material

本试验合成了一种含氧乙基的半乳糖衍生物Galβ1－（CH2－CH2－O）3－C14H29做为强化靶向材料，使其与卵磷脂（EYL）制得的斑蟊素脂质体相融合，测定其一系列理化性质。结果表明，此种强化靶向材料的加入并不影响脂质体的常规理化性质。小鼠尾静脉注射3．5h后，强化斑蟊素脂质体是普通斑蟊素脂质体在肝内浓度的3．6倍（P＜0．05），滞留时间亦显著延长。因为半乳糖可识别的动物凝聚素存在于肝内，所以此种半乳糖衍生物修饰的脂质体可充当治疗肝病药物的理想载体。

Liposomes have been studied as a useful tool for drug delivery system to carry therapeutic substances to a specific cell or tissue. For this purpose, so called targeting, liposomes must have an ability to interact selectively with the targeting cells. Therefore, it is necessary to modify the surface of the liposoems to render this ability. One galactose (Gal) derivative, Galβ1 - (CH2- CH2- O) 3- C14H29 was synthesized and incorporated into cantharidn liposomes prepared from egg yolk lectin (EYL). We compared a series of physicochemical characters between the strengthened cantharidin liposomes and the common cantharidin liposomes and tbe results showed that there was little difference. The concentration of the former in liver was 3. 6-fold as high as the later after iv 3. 5 h (P< 0. 05). The lag time was lengthened, too. As the Gal recognizing animal lectin exists in liver, the liposomes modified by mo]ecu]es of the strengthened targeting material seem to act as an excellent carrier of the liver therapeutic substances.