ADVANCED ACTIVE LIPOSOMAL LOADING OF POORLY WATER-SOLUBLE SUBSTANCES

摘要

The present invention relates to the field of encapsulation of substances with low aqueous solubility in liposomes, especially via active loading. The present inventors have surprisingly found that efficient active loading of liposomes with high liposome loading can be achieved by first solubilizing a functional compound, which is itself hardly soluble in water using a solubility enhancer. This significantlyincreases the functional-substance-to-lipid mass ratio to levels above those attained by conventional active or passive loading techniques and enlarges the range of functional compounds, including drugs, amenable to encapsulation in liposomes. One aspect of the invention provides the active loading process. Liposomal compositions with high drug-load are provided by the present invention as well.