公开(公告)号：EP2282724A2

公开(公告)日：2011-02-16

申请号：EP09750195.1

申请日：2009-05-26

申请人： The University of British Columbia

发明人： CULLIS, Pieter ,  BALLY, Marcel ,  CIUFOLINI, Marco ,  MAURER, Norbert ,  JIGALTSEV, Igor

IPC分类号： A61K9/127 ,  A61K31/337 ,  A61K45/00

CPC分类号： A61K9/127 ,  A61K9/1278 ,  A61K31/337 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/573 ,  A61K31/706 ,  A61K47/542 ,  C07D305/14 ,  C07D405/12 ,  C07D498/14 ,  C07H17/04 ,  C07J41/005 ,  C07J43/003 ,  C07K7/645

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.

公开(公告)号：EP2282724B1

公开(公告)日：2018-09-05

申请号：EP09750195.1

申请日：2009-05-26

申请人： The University of British Columbia

发明人： CULLIS, Pieter ,  BALLY, Marcel ,  CIUFOLINI, Marco ,  MAURER, Norbert ,  JIGALTSEV, Igor

IPC分类号： A61K9/127 ,  A61K31/337 ,  A61K45/00

CPC分类号： A61K9/127 ,  A61K9/1278 ,  A61K31/337 ,  A61K31/4525 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/573 ,  A61K31/706 ,  A61K47/542 ,  A61P29/00 ,  C07D305/14 ,  C07D405/12 ,  C07D498/14 ,  C07H17/04 ,  C07J41/005 ,  C07J43/003 ,  C07K7/645

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.