Nacucchio M C, Bellora M J, Sordelli D O, D'Aquino M
Antimicrob Agents Chemother. 1985 Jan;27(1):137-9. doi: 10.1128/AAC.27.1.137.
This study showed that encapsulation of the beta-lactam antibiotic piperacillin (PIP) by liposomes prepared with phosphatidylcholine and cholesterol (1:1) protected the drug from hydrolysis by staphylococcal beta-lactamase. This was demonstrated by growth inhibition of Staphylococcus aureus in the presence of the liposomal preparation containing PIP at a 50% MIC. Growth inhibition was also seen when exogenous beta-lactamase was added. Furthermore, adsorption of PIP onto the surface of liposomes containing buffer conferred a significant degree of protection against enzymatic hydrolysis of the drug, thus enhancing its antistaphylococcal activity.
本研究表明，用磷脂酰胆碱和胆固醇（1:1）制备的脂质体包裹β-内酰胺抗生素哌拉西林（PIP）可保护该药物免受葡萄球菌β-内酰胺酶的水解。在含有50% MIC的含PIP脂质体制剂存在的情况下，金黄色葡萄球菌的生长受到抑制，这证明了这一点。当加入外源性β-内酰胺酶时也观察到生长抑制。此外，PIP吸附到含有缓冲液的脂质体表面可对药物的酶促水解提供显著程度的保护，从而增强其抗葡萄球菌活性。
