抄録
Isocarbacyclin (TEI 7165), an analogue of prostacyclin, and its methylester (TEI 9090) were incorporated in lipid microspheres (LM) with a diameter of 0.2μm, in an attempt to increase the efficacy, probably by way of targeting the drugs to the vessel wall. When the two LM-preparations were incubated in 2% BSA-saline, it was shown that TEI 9090 was released from LM much more slowly than TEI 7165. It indicates that TEI 9090 in LM, injected intravenously, may not be released largely in plasma, and delivered to the target sites.
Compared with TEI 9090 as such, TEI 9090 incorporated in LM was more than 500 times more potent as an inhibitor of ADP-induce thrombus growth in the hamster cheek pouch model. These data suggest that prostacyclin analogues incorporated in LM may be used safely as potent antithrombotic agents in the clinical application.
