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

提出了一种制备表面具有高密度糖链的纳米粒子的新方法。使用携带碳水化合物的聚苯乙烯衍生物作为乳化剂和表面涂层，通过溶剂蒸发法制备了携带碳水化合物的聚乳酸或聚苯乙烯纳米颗粒。根据聚苯乙烯衍生物的浓度，所得纳米颗粒的直径在80至300 nm的范围内。随着聚苯乙烯衍生物的浓度增加，纳米颗粒直径减小，表明聚苯乙烯衍生物作为乳化剂。所获得的颗粒被碳水化合物特异性凝集素特异性聚集，表明聚苯乙烯衍生物保留在颗粒表面并表达碳水化合物残基。颗粒表面上的碳水化合物的密度被确定为每平方纳米3-5个分子。与通过用聚苯乙烯衍生物吸附聚苯乙烯颗粒而制备的后涂覆颗粒相比，通过本方法制备的颗粒在储存和离心处理期间稳定分散并且几乎不聚集在水性介质中。离体大鼠肝细胞的体外研究表明，表面糖链被肝细胞识别。生物材料（1994）15，（13）1035-1042

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