Ishihara H, Hara T, Aramaki Y, Tsuchiya S, Hosoi K
Tokyo College of Pharmacy, Japan.
Pharm Res. 1990 May;7(5):542-6. doi: 10.1023/a:1015833220179.
The selective delivery of human recombinant interferon (IFN)-gamma to isolated rat hepatocytes was studied with asialofetuin (AF)-labeled liposomes. AF-liposomes containing buffer solution were initially prepared by the detergent removal method, and IFN-gamma was subsequently encapsulated by the freeze-thawing method without loss of activity. Virtually no free [32P]IFN-gamma was internalized into isolated rat hepatocytes, whereas AF-liposomes containing [32P]IFN-gamma were taken up to a significant degree. Liposomal binding to the hepatocytes (estimated at 4 degrees C) was one-fifth of the uptake (estimated at 37 degrees C). Since the uptake was inhibited by the addition of free AF, AF-liposomes may be taken up by the action of galactose-binding protein on the hepatocytic cell surface. The liposome preparation method reported in this paper provides a useful means for the encapsulation of unstable macromolecules into AF-liposomes. AF-liposomes were found effectively to carry IFN-gamma into hepatocytes in vitro.
用去唾液酸胎球蛋白（AF）标记的脂质体研究了人重组干扰素（IFN）-γ对分离的大鼠肝细胞的选择性递送。含缓冲溶液的AF-脂质体最初通过去污剂去除法制备，随后通过冻融法包封IFN-γ，且活性未损失。实际上，游离的[32P]IFN-γ几乎没有被分离的大鼠肝细胞内化，而含[32P]IFN-γ的AF-脂质体被大量摄取。脂质体与肝细胞的结合（在4℃下测定）是摄取量（在37℃下测定）的五分之一。由于加入游离AF可抑制摄取，AF-脂质体可能通过半乳糖结合蛋白作用于肝细胞表面而被摄取。本文报道的脂质体制备方法为将不稳定大分子包封到AF-脂质体中提供了一种有用的手段。发现AF-脂质体在体外能有效地将IFN-γ携带到肝细胞中。
