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Last Updated: September 26, 2020

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Patent: 6,103,216

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Summary for Patent: 6,103,216
Title: Hepatocyte-selective oil-in-water emulsion
Abstract:A heat and shelf-stable oil-in-water emulsion useful as a tissue or cell-selective delivery vehicle. Radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate] or 2-oleoylglycerol-1,3-bis[.omega.-(3,5-bis-trifluoromethyl)-heptanoate] or phenyl acetate, can be incorporated into the lipophilic core of a lipoprotein-like emulsion particle. The lipophilic core is surrounded by a phospholipid membrane comprising cholesterol and apolipoproteins. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm as measured by number weighting analysis with a narrow size distribution (<2% greater than 300 nm) and having a composition simulating naturally-occurring chylomicron remnants. Use of cholesterol in the emulsion formula facilitates association of apolipoproteins, especially Apo E which are recognized by liver cells and necessary for binding and uptake. Stability and size constraints can be achieved by ultra high energy mixing equipment, such as the MicroFluidizer (Microfluidics Corp., Newton, Mass.) to form the emulsion. In preferred embodiments, osmolality of the emulsion is controlled by glycerol rather than normal saline.
Inventor(s): Counsell; Raymond E. (Ann Arbor, MI), Longino; Marc A. (Ann Arbor, MI), Weichert; Jamey P. (Ann Arbor, MI), Bakan; Douglas A. (San Diego, CA)
Assignee: The Board of Regents acting for and on behalf of the University of (Ann Arbor, MI)
Application Number:08/737,429
Patent Claims:see list of patent claims

Details for Patent 6,103,216

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck Sharp & Dohme Corp. ZOSTAVAX zoster vaccine live INJECTION, POWDER, LYOPHILIZED, FOR SUSPENSION 125123 001 2006-05-25   Start Trial The Board of Regents acting for and on behalf of the University of (Ann Arbor, MI) 2014-05-16 search
Merck Sharp & Dohme Corp. ZOSTAVAX zoster vaccine live INJECTION, POWDER, LYOPHILIZED, FOR SUSPENSION 125123 1 2006-05-25   Start Trial The Board of Regents acting for and on behalf of the University of (Ann Arbor, MI) 2014-05-16 search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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