Khalil R M, Murad F E, Yehia S A, El-Ridy M S, Salama H A
Department of Pharmaceutical Sciences, National Research Centre, Cairo, Egypt.
Pharmazie. 1996 Mar;51(3):182-4.
Streptomycin sulfate liposomes were prepared by the vortex dispersion method. The liposomes were formulated from a mixture of L-alpha-dipalmitoyl phosphatidyl choline (DPPC), cholesterol with or without (neutral) a charge inducing agent. Two phospholipid molar ratios were considered, namely, DPPC cholesterol 7:2 and 7:4. The amount of streptomycin sulfate entrapped was estimated, microbiologically, and found to range from 0.080 to 1.323% of the initial amount of drug used for preparation of liposomes, depending on the surface charge of the liposomal vesicles. Particle size analysis, measured by the coulter counter, showed a mean particle diameter ranging from 4.417-8.424 microns. Drug targeting experiments were done using Swiss mice as the experimental animals. The in-vivo results indicated that the streptomycin sulfate concentration targeted to the liver and spleen by the liposome encapsulated drug was 2-3 times that exhibited by the free drug. This effect occurred after one day of liposome injection, but it decreased over time from one to seven days. The amount of streptomycin sulfate targeted to the lung, by the liposome formulation 7:2:1 was more than that exhibited by the free drug. This is true only after 7 d from injection. On the other hand, the liposomes of molar ratio 7:4:1 showed much less effect even when compared to the free drug. The survival rate experiments indicated a definite protection against Salmonella enteritidis, exhibited by the liposome-encapsulated streptomycin compared to the free drug.
采用涡旋分散法制备硫酸链霉素脂质体。脂质体由L-α-二棕榈酰磷脂酰胆碱(DPPC)、胆固醇与有或无(中性)电荷诱导剂的混合物制成。考虑了两种磷脂摩尔比,即DPPC:胆固醇为7:2和7:4。通过微生物学方法估计包封的硫酸链霉素量,发现其占用于制备脂质体的初始药物量的0.080%至1.323%,这取决于脂质体囊泡的表面电荷。通过库尔特计数器测量的粒度分析显示平均粒径范围为4.417 - 8.424微米。使用瑞士小鼠作为实验动物进行药物靶向实验。体内结果表明,脂质体包裹药物靶向肝脏和脾脏的硫酸链霉素浓度是游离药物的2 - 3倍。这种效应在注射脂质体一天后出现,但从一天到七天随时间下降。脂质体制剂7:2:1靶向肺部的硫酸链霉素量比游离药物多。这仅在注射7天后成立。另一方面,摩尔比为7:4:1的脂质体即使与游离药物相比也显示出小得多的效果。存活率实验表明,与游离药物相比,脂质体包裹的链霉素对肠炎沙门氏菌有明确的保护作用。