Application of biodegradable Nanoparticles coated with sugar-carrying polymer to targetted drug delivery

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A novel method of preparing nanoparticles bearing high density carbohydrate chains on their surface was developed. Carbohydrate-bearing nanoparticles of poly (lactic acid) or polystirene were prepared by the solvent evaporation method using a carbohydrate-carrying polystirene derivative which served as both an emulsifier and a surface coating. The diameter of the obtained nanoparticles ranged from 80 to 300 nm depending on the concentration of the polystirene derivative. As the concentration of the polystirene derivatives increased the nanoparticle diameter decreased, indicating that the polystirene derivatives worked as an emulsifier. The obtained particles were specifically aggregated by carbohydrate-specific lectin, showing that the polystirene derivative was retained on the particle surfaces and expressed carbohydrate residues. The density of carbohydrates on the particle surfaces was determined to be 3-5 molecules per square nanometer. The particles prepared by the present method were stably dispersed and hardly aggregated in aqueous media during storage and centrifugal treatment compared with the post-coated particles that were prepared by adsorbing polystirene particles with the polystirene derivative. In vitro study with isolated rat hepatocytes revealed that surface carbohydrate chains were recognized by hepatocytes. Biomaterials (1994) 15, (13) 1035-1042