Pieter Jaap Gaillard,Chantal Catharina Maria Appeldoorn,Jacob Rip
申请号:
US14002559
公开号:
US20130337051A1
申请日:
2012.03.01
申请国别(地区):
US
年份:
2013
代理人:
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 significantly increases 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.