NOVEL LIPOSACCHARIDE CONJUGATES FOR DRUG AND PEPTIDE DELIVERY

Sugar-lipid conjugates with general structure 1-4 were prepared by cou pling amino sugars with N-Boc-protected lipoamino acids and oligomers. Conjugates with general structure 5 were also prepared from glucuroni c acid and methyl 2-aminohexadecanoate. The physicochemical properties of the conjugates were modified by varying the nature and number of s ugars or the number of lipoamino acids or their alkyl chain length. Th e ability of the liposaccharides to aggregate was examined. These prel iminary experiments have demonstrated the ability of the liposaccharid es to form particulate systems per se and also their ability to be inc orporated into conventional liposomal systems. The structure of the re spective liposaccharides and the molar ratio of liposaccharide to dimy ristoyl lecithin and cholesterol were found to have a profound effect on the type of colloidal systems produced.