The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 29, 2014

Filed:

May. 26, 2009
Applicants:

Pieter Cullis, Vancouver, CA;

Marcel Bally, Bowen Island, CA;

Marco Ciufolini, Vancouver, CA;

Norbert Maurer, Vancouver, CA;

Igor Jigaltsev, Vancouver, CA;

Inventors:

Pieter Cullis, Vancouver, CA;

Marcel Bally, Bowen Island, CA;

Marco Ciufolini, Vancouver, CA;

Norbert Maurer, Vancouver, CA;

Igor Jigaltsev, Vancouver, CA;

Assignee:
Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
A61K 9/127 (2006.01); C07D 405/12 (2006.01); C07D 413/12 (2006.01); C07D 305/14 (2006.01); C07J 43/00 (2006.01); C07J 41/00 (2006.01); C07D 493/04 (2006.01); C07D 498/16 (2006.01); C07K 7/64 (2006.01); A61K 31/496 (2006.01); A61K 31/5377 (2006.01); A61K 31/4523 (2006.01); A61K 31/337 (2006.01); A61K 31/58 (2006.01); A61K 31/573 (2006.01); A61K 38/13 (2006.01); B82Y 5/00 (2011.01);
U.S. Cl.
CPC ...
Abstract

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.


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