ACCUMULATION OF DRUGS INTO LIPOSOMES BY A PROTON GRADIENT

摘要

The present invention relates to pharmaceutical compositions and methods of making liposome containing compositions exhibiting characteristics of great uptake. This uptake may be greater than what would be expected by the relationship defined by the Henderson-Hasselbach equation. The present invention also relates to lipososmal compositions wherein the liposome comprises in part a membrane-stabilizing component, for example, cholesterol, which exhibits favorable characteristics in preventing rapid release of a pharmaceutical agent selected from the group consisting of quinine, quinidine and diphenhydramine after it has been formulated in liposomes. The present invention also relates to novel liposomal compositions comprising the bronchodilators metaproterenol, isoproterenol and terbutaline. The present invention also relates to minimum buffering capacity required to achieve liposomal encapsulation of pharmaceutical agents with maintenance of a major portion of the initial pH gradient.