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Title:
MODIFIED DRUGS FOR USE IN LIPOSOMAL NANOPARTICLES
Document Type and Number:
Japanese Patent JP2019048851
Kind Code:
A
Abstract:
To provide modified drugs for use in liposomal nanoparticles.SOLUTION: Provided herein is a drug derivative suitable for loading into liposomal nanoparticle (LN) carriers. In some preferred aspects, the derivative comprises a drug with low water solubility derivatized with a weak-base moiety that facilitates active loading of the drug through the LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety may optionally comprise a lipophilic domain that facilitates active loading of the drug into the inner monolayer of the liposome membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy and/or other benefits in comparison with the corresponding free drugs.SELECTED DRAWING: Figure 10

Inventors:
PIETER CULLIS
MARCEL BALLY
MARCO CIUFOLINI
NORBERT MAURER
IGOR JIGALTSEV
Application Number:
JP2018214441A
Publication Date:
March 28, 2019
Filing Date:
November 15, 2018
Export Citation:
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Assignee:
UNIV BRITISH COLUMBIA
International Classes:
C07J41/00; A61K9/10; A61K9/127; A61K31/337; A61K31/4523; A61K31/496; A61K31/52; A61K31/5377; A61K31/573; A61K31/58; A61K31/7048; A61K31/7056; A61K38/08; A61K47/02; A61K47/12; A61K47/24; A61K47/28; A61K47/34; A61K47/54; A61P29/00; A61P35/00; C07D305/14; C07D473/38; C07H15/04; C07H17/04; C07J5/00; C07J43/00
Domestic Patent References:
JP2006508126A2006-03-09
JP2007517909A2007-07-05
JP2002542302A2002-12-10
JP2002519392A2002-07-02
JP2004501158A2004-01-15
JPH01279896A1989-11-10
JPH01117885A1989-05-10
Foreign References:
US20050004169A12005-01-06
WO2008076333A22008-06-26
Other References:
BIOCONJUGATE CHEMISTRY, vol. 16, no. 4, JPN6019045973, 2005, pages 873 - 884, ISSN: 0004289243
JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 2, JPN6019045975, 2005, pages 593 - 603, ISSN: 0004289244
JOURNAL OF CONTROLLED RELEASE, vol. 61, no. 3, JPN6019045977, 1999, pages 281 - 294, ISSN: 0004289245
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, vol. 11, no. 1, JPN6019045979, 1995, pages 79 - 83, ISSN: 0004289246
Attorney, Agent or Firm:
Takeshi Oshio