Restenosis remains a serious complication that can occur after angioplasty. This study investigated the efficiency of an active targeting
chemotherapy using
liposomes, including
doxorubicin, whose surface was decorated with
sialyl Lewis X (SLX) (Dox-Lipo-SLX) to prevent
stenosis after angioplasty. Its delivery was controlled via the affinity between SLX and
E-selectin proteins, which are expressed on vessel walls with injury. In vitro experiments confirmed the accumulation of
doxorubicin as a consequence of Dox-Lipo-SLX adhering to
E-selectin-positive cells. Significant
doxorubicin accumulation was observed on injured vessel walls in rats treated with Dox-Lipo-SLX. In contrast, there was little accumulation using free
doxorubicin or a
liposome containing
doxorubicin (Dox-Lipo), but without SLX. Rats were assigned to one of four groups: Dox-Lipo-SLX, Dox-Lipo, free
doxorubicin, or no treatment. Dox-Lipo-SLX, Dox-Lipo, and free
doxorubicin, including a dose of 0.08mg/kg
doxorubicin, were intravenously administered three times in each group after angioplasty. The residual lumen area of rats in the group treated with Dox-Lipo-SLX was significantly larger than those in all other groups. These results demonstrate that an active targeting drug delivery system utilizing Dox-Lipo-SLX effectively prevents
stenosis after angioplasty.