Medda S, Mukherjee S, Das N, Naskar K, Mahato S B, Basu M K
Biomembrane Division, Indian Institute of Chemical Biology, Calcutta.
Biotechnol Appl Biochem. 1993 Feb;17(1):37-47.
The uptake of glycoside-bearing liposomes by macrophages has been studied in vitro. Since the uptake was found to be specific for the end sugar attached to the glycoside, the possibility is raised that glycoside-bearing liposomes might be used in vivo as systems to deliver drugs to macrophages. Using the antileishmanial drug urea stibamine, these delivery systems have been tested in vivo against model leishmaniasis. The results indicate that the drug encapsulated in sugar-coated liposomes is much more potent in comparison with normal liposome-encapsulated drug or to the free drug. Mannose-grafted liposomes are more efficient in transportation of drugs compared with those bearing glucose. Toxicity studies involving blood parameters, histological staining of tissues and specific enzyme activities related to liver function, show no apparent toxicity with the drugs. Hence, drug encapsulated sugar-coated liposomes may have possible applications to humans.
巨噬细胞对含糖苷脂质体的摄取已在体外进行了研究。由于发现摄取对糖苷上连接的末端糖具有特异性，因此有人提出含糖苷脂质体可能在体内用作将药物递送至巨噬细胞的系统。使用抗利什曼原虫药物尿素锑胺，这些递送系统已在体内针对模型利什曼病进行了测试。结果表明，与正常脂质体包裹的药物或游离药物相比，包裹在糖包被脂质体中的药物效力更强。与携带葡萄糖的脂质体相比，甘露糖嫁接的脂质体在药物运输方面更有效。涉及血液参数、组织组织学染色和与肝功能相关的特定酶活性的毒性研究表明，这些药物没有明显毒性。因此，包裹药物的糖包被脂质体可能对人类有潜在应用价值。
