CULLIS, PIETER,BALLY, MARCEL,CIUFOLINI, MARCO,MAURER, NORBERT,JIGALTSEV, IGOR
申请号：
CA2910133
公开号：
CA2910133C
申请日:
2009.05.26
申请国别(地区):
CA
年份:
2018
代理人:
摘要：
Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
