US5439686A
Expired / Lapsed
US
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Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful therefor
Assignee: Abraxis Bioscience LLC
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Filing: 1993-02-22
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Granted: 1995-08-08
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Expires: 2013-02-22
Abstract
Abstract In accordance with the present invention, there are provided compositions for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug taxol) in which the pharmacologically active agent is delivered in a soluble form or in the form of suspended particles. In particular, the soluble form may comprise a solution of pharmacologically active agent in a biocompatible dispersing agent contained within a protein walled shell. Alternatively, the protein walled shell may contain particles of taxol. In another aspect, the suspended form comprises particles of pharmacologically active agent in a biocompatible aqueous liquid.
Inventors
- 👤 Neil P. Desai
- 👤 Patrick Soon-Shiong
- 👤 Paul A. Sandford
- 👤 Mark W. Grinstaff
- 👤 Kenneth S. Suslick
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 19:37
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K9/0026; A23; A23L; A23L33/00; A23L33/40; A61K47/00; A61K47/50; A61K47/69; A61K47/6921; A61K47/6925; A61K47/6927; A61K49/00; A61K49/0002; A61K49/22; A61K49/222; A61K49/223; A61K49/226; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5052; A61K9/51; A61K9/5107; A61K9/513; A61K9/5138; A61K9/5146; A61K9/5161; A61K9/5169; A61P; A61P35/00; B; B82; B82Y; B82Y5/00
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
78 words
A composition for in vivo delivery of a substantially water insoluble pharmacologically active agent, wherein said agent is a solid or liquid substantially completely contained within a polymeric shell, wherein the largest cross-sectional dimension of said shell is no greater than about 10 microns, wherein said polymeric shell comprises a biocompatible polymer which is substantially crosslinked by way of disulfide bonds, and wherein said polymeric shell containing pharmacologically active agent therein is suspended in a biocompatible aqueous liquid.
Claim 2
Dependent Claim
78 words
A composition for in vivo delivery of a substantially water insoluble pharmacologically active agent, wherein said agent is a solid or liquid substantially completely contained within a polymeric shell, wherein the largest cross-sectional dimension of said shell is no greater than about 10 microns, wherein said polymeric shell comprises a biocompatible polymer which is substantially crosslinked by way of disulfide bonds, and wherein said polymeric shell containing pharmacologically active agent therein is suspended in a biocompatible aqueous liquid.
Claim 3
Dependent Claim
30 words
A composition according to claim 1 wherein said substantially water insoluble pharmacologically active agent is selected from a pharmaceutically active agent, a diagnostic agent, or an agent of nutritional value.
Claim 4
Dependent Claim
42 words
A composition according to claim 2 wherein said pharmaceutically active agent is selected from taxol, taxotere, campothecin, aspirin, ibuprofen, piroxicam, cimetidine, substantially water insoluble steroids, phenesterine, duanorubicin, doxorubicin, mitotane, visadine, halonitrosoureas, anthrocylines, ellipticine, diazepam, methoxyfluorane, isofluorane, enfluorane, halothane, benzocaine, dantrolene, or barbiturates.
Claim 5
Dependent Claim
22 words
A composition according to claim 2 wherein said diagnostic agent is selected from ultrasound contrast agents, radiocontrast agents, or magnetic contrast agents.
Claim 6
Dependent Claim
31 words
A composition according to claim 2 wherein said agent of nutritional value is selected from amino acids, sugars, proteins, carbohydrates, fat-soluble vitamins, fat, or combinations of any two or more thereof.
Claim 7
Dependent Claim
21 words
A composition according to claim 2 wherein said pharmacologically active agent within said shell is dissolved in a biocompatible dispersing agent.
Claim 8
Dependent Claim
89 words
A composition according to claim 6 wherein said biocompatible dispersing agent is selected from soybean oil, coconut oil, olive oil, safflower oil, cotton seed oil, aliphatic, cycloaliphatic or aromatic hydrocarbons having 4-30 carbon atoms, aliphatic or aromatic alcohols having 2-30 carbon atoms, aliphatic or aromatic esters having 2-30 carbon atoms, alkyl, aryl, or cyclic ethers having 2-30 carbon atoms, alkyl or aryl halides having 1-30 carbon atoms, optionally having more than one halogen substutuent, ketones having 3-30 carbon atoms, polyalkylene glycol, or combinations of any two or more thereof.
Claim 9
Dependent Claim
21 words
A composition according to claim 2 wherein said pharmacologically active agent within said shell is suspended in a biocompatible dispersing agent.
Claim 10
Dependent Claim
89 words
A composition according to claim 8 wherein said biocompatible dispersing agent is selected from soybean oil, coconut oil, olive oil, safflower oil, cotton seed oil, aliphatic, cycloaliphatic, or aromatic hydrocarbons having 4-30 carbon atoms, aliphatic or aromatic alcohols having 2-30 carbon atoms, aliphatic or aromatic esters having 2-30 carbon atoms, alkyl, aryl, or cyclic ethers having 2-30 carbon atoms, alkyl or aryl halides having 1-30 carbon atoms, optionally having more than one halogen substutuent, ketones having 3-30 carbon atoms, polyalkylene glycol, or combinations of any two or more thereof.
Claim 11
Dependent Claim
17 words
A composition according to claim 2 wherein said pharmacologically active agent within said shell is not diluted.
Claim 12
Dependent Claim
37 words
A composition according to claim 1 wherein said crosslinked polymer is a naturally occurring polymer, a synthetic polymer, or a combination thereof, wherein said polymer, prior to crosslinking, has covalently attached thereto sulfhydryl groups or disulfide linkages.
Claim 13
Dependent Claim
20 words
A composition according to claim 11 wherein said naturally occurring polymers are selected from proteins, lipids, polynucleic acids or polysaccharides.
Claim 14
Dependent Claim
107 words
A composition according to claim 11 wherein said synthetic polymers are selected from synthetic polyamino acids containing cysteine residues and/or disulfide groups, polyvinyl alcohol modified to contain free sulfhydryl groups and/or disulfide groups, polyhydroxyethyl methacrylate modified to contain free sulfhydryl groups and/or disulfide groups, polyacrylic acid modified to contain free sulfhydryl groups and/or disulfide groups, polyethyloxazoline modified to contain free sulfhydryl groups and/or disulfide groups, polyacrylamide modified to contain free sulfhydryl groups and/or disulfide groups, polyvinyl pyrrolidinone modified to contain free sulfhydryl groups and/or disulfide groups, polyalkylene glycols modified to contain free sulfhydryl groups and/or disulfide groups, as well as mixtures of any two or more thereof.
Claim 15
Dependent Claim
18 words
A composition according to claim 1 wherein the disulfide bonds on the crosslinked polymer are formed by sonication.
Claim 16
Dependent Claim
15 words
A composition according to claim 1 wherein said biocompatible polymer is the crosslinked protein albumin.
Claim 17
Dependent Claim
42 words
A composition according to claim 1 wherein said biocompatible aqueous liquid is selected from water, buffered aqueous media, saline, buffered saline, solutions of amino acids, solutions of sugars, solutions of vitamins, solutions of carbohydrates, or combinations of any two or more thereof.
Claim 18
Dependent Claim
30 words
A method for the delivery of substantially water insoluble pharmaceutical agents to a subject, said method comprising administering to said subject an effective amount of composition according to claim 1.
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