Children's Hospital Research Center at Oakland

University of Washington

Michael N Oda

Robert O Ryan

Jay W Heinecke

John F Oram

The invention provides compositions and methods for delivery of a bioactive agent to an individual. Delivery vehicles are provided that include a bioactive agent in disc shaped particles that include one or more lipid binding polypeptides circumscribing the perimeter of a lipid bilayer in which the bioactive agent is localized. Chimeric lipid binding polypeptides are also provided and may be used to add additional functional properties to the delivery particles.

Lipophilic drug delivery vehicle and methods of use thereof

Bioactive agent delivery particles

In one aspect, the present invention provides isolated oxidation resistant mutant apoA-I polypeptides comprising an amino acid sequence substantially homologous to SEQ ID NO:4, the mutant apoA-I polypeptide comprising a combination of: (1) a conservative amino acid substitution at residue Tyr192; and (2) at least one conservative amino acid substitution at residue Met86, Met112, or Met148, wherein the mutant apoA-I polypeptide is resistant to modification by an oxidizing agent. In another aspect, the invention provides a method of promoting cholesterol efflux activity in a mammalian subject in need thereof, the method comprising the step of administering an effective amount of an oxidation resistant apoA-I agonist to the subject to promote cholesterol efflux.

Mutant apolipoprotein A-1 polypeptide with increased resistance to oxidation and reactive carbonyls

Processes for the preparation of lipophilic drug delivery vehicles

Growing community of inventors

Fairfield, CA, United States of America

Michael N Oda