US Patent No: 6,749,868

Number of patents in Portfolio can not be more than 2000

Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof

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Abstract

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In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful election of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein.

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Patent Owner(s)

Patent OwnerAddressTotal Patents
ABRAXIS BIOSCIENCE, LLCLOS ANGELES, CA45

International Classification(s)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Desai, Neil P Santa Monica, CA 204 5021
Louie, Leslie Montebello, CA 5 186
Magdassi, Shlomo Jerusalem, IL 58 508
Soon-Shiong, Patrick Los Angeles, CA 175 2843
Tao, Chunlin Tallahassee, FL 66 376
Yang, Andrew Rosemead, CA 36 603
Yao, Zhiwen Culver City, CA 4 203

Cited Art Landscape

Patent Info (Count) # Cites Year
 
ABRAXIS BIOSCIENCE, LLC (5)
5,439,686 Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful therefor 172 1993
5,498,421 Composition useful for in vivo delivery of biologics and methods employing same 237 1994
5,916,596 Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof 126 1996
6,096,331 Methods and compositions useful for administration of chemotherapeutic agents 94 1997
6,537,579 Compositions and methods for administration of pharmacologically active compounds 71 2000
 
ZENECA LIMITED (4)
5,714,520 Propofol compostion containing edetate 45 1995
5,731,355 Pharmaceutical compositions of propofol and edetate 43 1997
5,731,356 Pharmaceutical compositions of propofol and edetate 27 1997
5,908,869 Propofol compositions containing edetate 26 1998
 
FAULDING PHARMACEUTICAL CO. (2)
6,028,108 Propofol composition comprising pentetate 22 1998
6,177,477 Propofol formulation containing TRIS 18 1999
 
AMERICAN HOME PRODUCTS CORPORATION (1)
4,344,934 Therapeutic compositions with enhanced bioavailability 42 1980
 
AMPHASTAR PHARMACEUTICALS, INC. (1)
6,399,087 Propofol formulation with enhanced microbial inhibition 15 2000
 
BAXTER INTERNATIONAL INC. (1)
6,100,302 Propofol formulation with enhanced microbial characteristics 22 1999
 
BRISTOL-MYERS SQUIBB COMPANY (1)
5,504,102 Stabilized pharmaceutical composition and stabilizing solvent 56 1995
 
CEPHALON LIMITED (1)
5,683,715 Taxane-containing phosphatidylcholine liposomes 29 1995
 
ELAN PHARMA INTERNATIONAL LIMITED (1)
5,399,363 Surface modified anticancer nanoparticles 198 1992
 
GENSIA SICOR INC. (1)
6,147,122 Propofol composition containing sulfite 19 1999
 
GENSIA SICOR PHARMACEUTICALS, INC. (1)
6,469,069 Propofol composition containing sulfite 18 2000
 
GEORGETOWN UNIVERSITY (1)
5,648,090 Liposome encapsulated toxol and a method of using the same 22 1995
 
HOSPIRA, INC. (1)
6,140,373 Propofol composition 20 1998
 
IVX ANIMAL HEALTH, INC. (1)
6,150,423 Propofol-based anesthetic and method of making same 17 1998
 
MASSACHUSETTS INSTITUTE OF TECHNOLOGY (1)
5,626,862 Controlled local delivery of chemotherapeutic agents for treating solid tumors 170 1994
 
NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT (1)
5,565,478 Combination therapy using signal transduction inhibitors with paclitaxel and other taxane analogs 40 1994
 
NOVARTIS;CORPORATE INTELLECTUAL PROPERTY (1)
5,744,460 Combination for treatment of proliferative diseases 32 1996
 
PG-TXL Company, L.P. (1)
5,977,163 Water soluble paclitaxel prodrugs 184 1997
 
Research Triangle Pharmaceuticals (1)
5,637,625 Propofol microdroplet formulations 44 1996
 
TEKMIRA PHARMACEUTICALS CORPORATION (1)
5,543,152 Sphingosomes for enhanced drug delivery 83 1994
 
The Scripps Research Institute (1)
5,731,334 Method for treating cancer using taxoid onium salt prodrugs 6 1995
 
VETERINARY RESEARCH ASSOCIATES, INC. (1)
5,962,536 Injectable propofol formulations 15 1998
 
VYREXIP HOLDINGS, INC. (1)
6,362,234 Water-soluble prodrugs of propofol for treatment of migrane 20 2000
 
Westy AG (1)
6,326,406 Clear, injectable formulation of an anesthetic compound 16 2000

Patent Citation Ranking

Forward Cite Landscape

Patent Info (Count) # Cites Year
 
ABRAXIS BIOSCIENCE, LLC (14)
8,034,375 Combinations and modes of administration of therapeutic agents and combination therapy 0 2006
8,034,765 Compositions and methods for preparation of poorly water soluble drugs with increased stability 17 2006
7,771,751 Compositions comprising poorly water soluble pharmaceutical agents and antimicrobial agents 3 2006
8,137,684 Formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof 1 2006
8,257,733 Methods and compositions for treating proliferative diseases 2 2006
7,820,788 Compositions and methods of delivery of pharmacological agents 4 2006
7,780,984 Methods and compositions for treating proliferative diseases 2 2007
7,758,891 Combinations and modes of administration of therapeutic agents and combination therapy 2 2008
7,981,445 Compositions and methods for preparation of poorly water soluble drugs with increased stability 2 2009
8,735,394 Combinations and modes of administration of therapeutic agents and combination therapy 0 2009
7,923,536 Compositions and methods of delivery of pharmacological agents 3 2010
8,138,229 Compositions and methods of delivery of pharmacological agents 1 2010
8,314,156 Compositions and methods of delivery of pharmacological agents 1 2011
8,268,348 Combinations and modes of administration of therapeutic agents and combination therapy 1 2011
 
SYNTA PHARMACEUTICALS CORP. (9)
7,763,658 Treatment for cancers 7 2004
8,017,654 Combination cancer therapy with bis(thiohydrazide) amide compounds 0 2006
7,939,564 Combination with bis(thiohydrazide amides) for treating cancer 1 2007
7,671,092 Paclitaxel enhancer compounds 8 2008
7,750,042 Paclitaxel enhancer compound 7 2008
7,652,168 Synthesis of taxol enhancers 7 2008
7,795,313 Bis(thio-hydrazide amide) salts for treatment of cancers 9 2009
8,048,925 Bis(thio-hydrazide amide) salts for treatment of cancers 2 2010
8,461,208 Bis(thio-hydrazide amide) salts for treatment of cancers 0 2011
 
CERULEAN PHARMA INC. (6)
8,497,365 Cyclodextrin-based polymers for therapeutics delivery 0 2011
8,404,662 Cyclodextrin-based polymers for therapeutics delivery 0 2012
8,609,081 Cyclodextrin-based polymers for therapeutics delivery 0 2013
8,580,242 Cyclodextrin-based polymers for therapeutics delivery 0 2013
8,518,388 Cyclodextrin-based polymers for therapeutics delivery 0 2013
8,603,454 Cyclodextrin-based polymers for therapeutics delivery 0 2013
 
BIOMED REALTY, L.P. (2)
7,964,196 Self-assembling nanoparticle drug delivery system 0 2005
8,067,011 Compositions and methods for treating B-cell malignancies 0 2007
 
NITTO DENKO CORPORATION (2)
8,197,828 Compositions that include a hydrophobic compound and a polyamino acid conjugate 0 2008
8,329,199 Compositions that include a hydrophobic compound and a polyamino acid conjugate 0 2012
 
PEYMAN, GHOLAM A. (2)
7,722,581 Crystalline lens drug delivery 2 2005
7,458,953 Ocular drainage device 7 2006
 
CHEVRON PHILLIPS CHEMICAL COMPANY LP (1)
8,809,562 Use of metallocene compounds for cancer treatment 0 2012
 
DUKE UNIVERSITY (1)
8,013,022 Stabilized products, process and devices for preparing same 0 2007
 
INTERHEALTH NUTRACEUTICALS, INC. (1)
8,748,499 Collagen dispersion and method of producing same 0 2010
 
LUMINUS BIOSCIENCES, INC. (1)
8,728,527 Solid nanoparticle formulation of water insoluble pharmaceutical substances with reduced ostwald ripening 0 2007
 
SALPIETRA, JOHN M. "PETE",ROCHESTER HILLS,MI, SALPIETRA JOSEPH ANTHONY JR,"SALPIETRA, JOSEPH ANTHONY, JR. (1)
8,273,560 Coated substrates and methods of preparing the same 0 2011
 
TEIKOKU PHARMA USA, INC. (1)
8,569,357 Taxane pro-emulsion formulations and methods making and using the same 0 2011
 
UNIVERSITY OF NORTH TEXAS (1)
8,048,450 Aqueous dispersion of hydrogel nanoparticles with inverse thermoreversible gelation 0 2004
 
Other [Check patent profile for assignment information] (2)
6,995,145 Methods and compositions for modulating drug activity through telomere damage 2 2000
8,449,919 Composition and method for preparing alginate nanocapsules 0 2006

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