Coacervate Microparticles Useful for the Sustained Release Administration of Therapeutics Agents
Description of Invention:
The described technology is a biodegradable microbead or microparticle, useful for the sustained localized delivery of biologically active proteins or other molecules of pharmaceutical interest. The microbeads are produced from several USP grade materials, a cationic polymer, an anionic polymer and a binding component (e.g., gelatin, chondroitin sulfate and avidin), in predetermined ratios. Biologically active proteins are incorporated into preformed microbeads via an introduced binding moiety under nondenaturing conditions.
Proteins or other biologically active molecules are easily denatured, and once introduced into the body, rapidly cleared. These problems are circumvented by first incorporating the protein into the microbead. Microbeads with protein payloads are then introduced into the tissue of interest, where the microbeads remain while degrading into biologically innocuous materials while delivering the protein/drug payload for adjustable periods of time ranging from hours to weeks. This technology is an improvement of the microbead technology described in U.S. Patent No. 5,759,582.
Applications:
This technology has two commercial applications. The first is a pharmaceutical drug delivery application. The bead allows the incorporated protein or drug to be delivered locally at high concentration, ensuring that therapeutic levels are reached at the target site while reducing side effects by keeping systemic concentration low. The microbead accomplishes this while protecting the biologically active protein from harsh conditions traditionally encountered during microbead formation/drug formulation.
The microbeads are inert, biodegradable, and allow a sustained release or multiple-release profile of treatment with various active agents without major side effects. In addition, the bead maintains functionality under physiological conditions.
Second, the microbeads and microparticles can be used in various research assays, such as isolation and separation assays, to bind target proteins from biological samples. A disadvantage of the conventional methods is that the proteins become denatured. The denaturation results in incorrect binding studies or inappropriate binding complexes being formed. The instant technology corrects this disadvantage by using a bead created in a more neutral pH environment. It is this same environment that is used for the binding of the protein of interest as well.
Inventors:
Phillip F. Heller (NIA)
Patent Status:
DHHS Reference No. E-116-2004/0 --
U.S. Provisional Application No. 60/602,651 filed 19 Aug 2004
PCT Application No. PCT/US2005/026257 filed 25 Jul 2005, which published as WO 2006/023207 on 02 Mar 2006
U.S. Patent Application No. 11/659,976 filed 12 Feb 2007
Licensing Status: Available for non-exclusive or exclusive licensing.
Portfolios: Infectious Diseases
Infectious Diseases -Therapeutics
For Additional Information Please Contact: Susan Ano Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: (301) 435-5515
Email: anos@mail.nih.gov
Fax: (301) 402-0220
