Desiderio J V, Campbell S G
J Infect Dis. 1983 Sep;148(3):563-70. doi: 10.1093/infdis/148.3.563.
Multilamellar liposomes (lipid bilayer vesicles) composed of phosphatidylcholine, cholesterol, and phosphatidylserine (molar ratio, 6:3:1) were produced and then made to entrap an aqueous solution of cephalothin. Resident murine peritoneal macrophages were shown to be capable of interiorizing the liposome-antibiotic complex; this event resulted in a relatively high intracellular concentration of cephalothin. In macrophages infected in vitro with Salmonella typhimurium, intracellular killing of the bacteria was maximal at 60 min of incubation; at this time, 60% of the interiorized organisms had been killed. Treatment of infected macrophages with liposome-encapsulated cephalothin enhanced the intraphagocytic killing of S typhimurium over that by macrophages treated with free cephalothin. These results demonstrate the superiority of liposome-encapsulated antibiotics to free antibiotics in effecting the elimination of a facultative intracellular bacterium from its intracellular site. This type of complex may find application in the treatment of diseases caused by this group of microorganisms.
制备了由磷脂酰胆碱、胆固醇和磷脂酰丝氨酸（摩尔比为6:3:1）组成的多层脂质体（脂质双层囊泡），然后使其包裹头孢噻吩水溶液。结果表明，常驻小鼠腹腔巨噬细胞能够摄取脂质体 - 抗生素复合物；这一过程导致细胞内头孢噻吩浓度相对较高。在体外感染鼠伤寒沙门氏菌的巨噬细胞中，孵育60分钟时细菌的细胞内杀伤作用最强；此时，60% 被摄取的细菌已被杀死。用脂质体包裹的头孢噻吩处理感染的巨噬细胞，与用游离头孢噻吩处理的巨噬细胞相比，增强了对鼠伤寒沙门氏菌的吞噬细胞内杀伤作用。这些结果表明，在从细胞内部位清除兼性细胞内细菌方面，脂质体包裹的抗生素比游离抗生素具有优越性。这种复合物可能在治疗由这类微生物引起的疾病中得到应用。
