Application of liposome decorated with sugar chains to prevent vascular stenosis after angioplasty

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Restenosis remains a serious complication that can occur after angioplasty. This study investigated the efficiency of an active targeting chemotherapy using liposomes,including doxorubicin, which 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 injured arteries. In vitro experiments confirmed that doxorubicin accumulated owing to Dox-Lipo-SLX by adhering to E-selectin-positive cells. Rats with balloon-injured arteries were intravenously injected with Dox-Lipo-SLX. A significant doxorubicin accumulation was observed on the injured vessel walls in rats treated with Dox-Lipo-SLX. The efficiency of stenosis prevention was evaluated. The residual lumen area of the group treated with Dox-Lipo-SLX was significantly larger than all of the other groups. These results demonstrate that an active targeting drug delivery system with Dox-Lipo-SLX effectively prevents stenosis after angioplasty.