Mayer L D, Bally M B, Cullis P R
Biochim Biophys Acta. 1986 May 9;857(1):123-6. doi: 10.1016/0005-2736(86)90105-7.
Previous work has shown that adriamycin can be accumulated into large unilamellar vesicle (LUV) systems in response to K+ diffusion potential established by valinomycin. It is demonstrated here that adriamycin can also be rapidly and efficiently accumulated into egg phosphatidylcholine (egg PC) and egg PC-cholesterol (1:1) LUVs in response to a transmembrane pH gradient (interior acidic) in the absence of ionophores. This 'active' loading gives rise to trapping efficiencies as high as 98%, interior drug concentrations as high as 100 mM and significantly enhances drug retention within the vesicles. This procedure may be of general utility for loading liposomal systems for in vivo drug delivery.
先前的研究表明，阿霉素可以响应缬氨霉素建立的钾离子扩散电位而积累到大单室囊泡（LUV）系统中。本文证明，在没有离子载体的情况下，阿霉素也可以响应跨膜pH梯度（内部呈酸性）而快速有效地积累到鸡蛋磷脂酰胆碱（鸡蛋PC）和鸡蛋PC-胆固醇（1:1）的LUV中。这种“主动”装载产生的捕获效率高达98%，内部药物浓度高达100 mM，并显著提高了药物在囊泡内的保留率。该方法可能对装载用于体内药物递送的脂质体系统具有普遍实用性。
