Synthesis of sialyl Lewis X-polysaccharide conjugates

Sialyl Lewis X (SLe(X)) is well known as a ligand of the cell adhesion mole cule E-selectin which is specifically expressed at inflammatory lesion site s. We have synthesized several SLe(X)-polysaccharide conjugates and examine d their potential for drug delivery to inflammatory lesions. The AUC (area under the blood concentration-time curve) 0-24 h of SLe(X)-CMCht (1), SLe(X )-CMPul (2) and SLe(X)-DSH (3) at the inflammatory lesion was about 60-, 30 0-, and 30-fold higher than that of the monovalent SLe(X) (7), respectively . Moreover, 1 showed 2-fold higher accumulation in the inflammatory lesion than SLN-CMCht (4), and 2 showed 2.5-fold higher accumulation than SLN-CMPu l (5).