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US5560933A
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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: 1995-03-29
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Granted: 1996-10-01
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Expires: 2015-03-29
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
- 👤 Patrick Soon-Shiong
- 👤 Neil P. Desai
- 👤 Mark W. Grinstaff
- 👤 Paul A. Sandford
- 👤 Kenneth S. Suslick
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 07:54
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: 30
Claim 1
Independent Claim
76 words
A method for the preparation of a substantially water insoluble pharmacologically active agent for in vivo delivery, said method comprising subjecting a mixture comprising: a dispersing agent containing said pharmacologically active agent dispersed therein, and aqueous medium containing a biocompatible polymer capable of being crosslinked by disulfide bonds to sonication conditions for a time sufficient to promote crosslinking of said biocompatible polymer by disulfide bonds to produce a polymeric shell containing the pharmacologically active agent therein.
Claim 2
Independent Claim
76 words
A method for the preparation of a substantially water insoluble pharmacologically active agent for in vivo delivery, said method comprising subjecting a mixture comprising: a dispersing agent containing said pharmacologically active agent dispersed therein, and aqueous medium containing a biocompatible polymer capable of being crosslinked by disulfide bonds to sonication conditions for a time sufficient to promote crosslinking of said biocompatible polymer by disulfide bonds to produce a polymeric shell containing the pharmacologically active agent therein.
Claim 3
Independent Claim
45 words
A method for the preparation of substantially water insoluble pharmaceutical agents for in vivo delivery, said method comprising subjecting taxol and suitable medium to sonication conditions for a time sufficient to produce particles having a maximum cross-sectional dimension of no greater than about 10 microns.
Claim 4
Independent Claim
45 words
A method for the preparation of substantially water insoluble pharmaceutical agents for in vivo delivery, said method comprising subjecting taxol and suitable medium to sonication conditions for a time sufficient to produce particles having a maximum cross-sectional dimension of no greater than about 10 microns.
Claim 5
Dependent Claim
88 words
The method according to claim 1 wherein said 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 substituent, ketones having 3-30 carbon atoms, polyalkylene glycol, or combinations of any two or more thereof.
Claim 6
Dependent Claim
15 words
The method according to claim 3 wherein said dispersing agent comprises a volatile dispersing agent.
Claim 7
Dependent Claim
23 words
The method according to claim 4 wherein the volatile dispersing agent is selected from benzene, toluene, hexane, ethyl ether, dichloromethane, or ethyl acetate.
Claim 8
Dependent Claim
30 words
The method 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 9
Dependent Claim
42 words
The method according to claim 6 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 10
Dependent Claim
28 words
The method according to claim 6 where said pharmaceutically active agent is a substantially water insoluble immunosuppressive agent selected from cyclosporines, azathioprine, 17-ally-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0 4 ,9 ]octacos-18-ene-2,3,10,16-tetraone, or prednisone.
Claim 11
Dependent Claim
22 words
The method according to claim 6 wherein said diagnostic agent is selected from ultrasound contrast agents radiocontrast agents, or magnetic contrast agents.
Claim 12
Dependent Claim
17 words
The method according to claim 9 wherein said radiocontrast agent is selected from iodo-octanes, halocarbons, or renografin.
Claim 13
Dependent Claim
17 words
The method according to claim 9 wherein said magnetic contrast agent is a lipid soluble paramagnetic compound.
Claim 14
Dependent Claim
32 words
The method according to claim 6 wherein said agent of nutritional value is selected from amino acids, sugars, proteins, carbohydrates, fat-soluble vitamins, or fat, or combinations of any two or more thereof.
Claim 15
Dependent Claim
21 words
The method according to claim 12 wherein said pharmacologically active agent within said shell is dissolved in a biocompatible dispersing agent.
Claim 16
Dependent Claim
21 words
The method according to claim 1 wherein said pharmacologically active agent within said shell is suspended in a biocompatible dispersing agent.
Claim 17
Dependent Claim
17 words
The method according to claim 1 further comprising suspending the polymeric shells in a biocompatible aqueous liquid.
Claim 18
Dependent Claim
27 words
The method according to claim 15 wherein said biocompatible aqueous liquid is selected from water, saline, a solution containing appropriate buffers, or a solution containing nutritional agents.
Claim 19
Dependent Claim
37 words
The method according to claim 1 wherein said biocompatible 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 20
Dependent Claim
20 words
The method according to claim 17 wherein said naturally occurring polymers are selected from proteins, lipids, polynucleic acids or polysaccharides.
Claim 21
Dependent Claim
22 words
The method according to claim 18 wherein said protein is selected from albumin, insulin, hemoglobin, lysozyme, immunoglobulins, alpha-2-macroglobulin, fibronectin, vitronectin, or fibrinogen.
Claim 22
Dependent Claim
11 words
The method according to claim 19 wherein said protein is albumin.
Claim 23
Dependent Claim
21 words
The method according to claim 18 wherein said polysaccharide is selected from starch, cellulose, dextrans, alginates, chitosan, pectin, or hyaluronic acid.
Claim 24
Dependent Claim
107 words
The method according to claim 17 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 pyrrolidone 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 25
Dependent Claim
28 words
The method according to claim 1 wherein the mixture is subjected to sonication conditions comprising acoustic power in the range of 1 up to 1000 watts/cm 2 .
Claim 26
Dependent Claim
28 words
The method according to claim 1 wherein the mixture is subjected to sonication conditions comprising acoustic power in the range of 50 up to 500 watts/cm 2 .
Claim 27
Dependent Claim
18 words
The method according to claim 1 wherein the mixture is subjected to sonication for less than 5 minutes.
Claim 28
Dependent Claim
22 words
The method according to claim 1 wherein the mixture is subjected to sonication for a time ranging from 15 to 60 seconds.
Claim 29
Dependent Claim
15 words
The method according to claim 1 further comprising removing the dispersing agent from the mixture.
Claim 30
Dependent Claim
21 words
The method according to claim 1 wherein the largest cross-sectional dimension of said shell is no greater than about 10 microns.
References Cited (Backward Citations)
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