EP0202017A2
Expired / Lapsed
EP
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Artificial microcompartmentalised structures and process for the manufacture thereof
Assignee: Rafa Laboratories Ltd
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Filing: 1986-04-08
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Granted: —
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Expires: 2006-04-08
Abstract
Abstract A semipermeable microcompartment which is artificially prepared by reassembly of proteinaceous substances and which is defined by a peripheral membrane which consists substantially of a layer of macromolecules each of which comprises a relatively hydrophilic moiety and a relatively hydrophobic moiety and wherein the majority of such macromolecules forming the membrane are disposed with their relatively hydrophobic moieties orientated inwardly towards the interior of the microcompartment.
Inventors
- 👤 Shmuel Ben-Sasson
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-07 12:53
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5063; A61K9/5068; A61K9/5021; A61K9/5052
Claims Analysis
Total Claims: 83
Claim 1
Independent Claim
77 words
A semipermeable microcompartment which is artificially prepared by reassembly of proteinaceous macromolecules and which is defined by a peripheral membrane consisting substantially of a layer of said macromolecules, each of which comprises a relatively hydrophilic moiety and a reta- tively hydrophobic moiety and wherein the majority of such macromolecules forming the membrane are disposed with their relatively hydrophilic moities orientated outwardly from the microcompartment and their relatively hydrophobic moieties orientated inwardly towards the interior of the microcompartment.
Claim 2
Dependent Claim
77 words
A semipermeable microcompartment which is artificially prepared by reassembly of proteinaceous macromolecules and which is defined by a peripheral membrane consisting substantially of a layer of said macromolecules, each of which comprises a relatively hydrophilic moiety and a reta- tively hydrophobic moiety and wherein the majority of such macromolecules forming the membrane are disposed with their relatively hydrophilic moities orientated outwardly from the microcompartment and their relatively hydrophobic moieties orientated inwardly towards the interior of the microcompartment.
Claim 3
Dependent Claim
16 words
A microcompartment according to claim 1 wherein substantially all of said macromolecules are disposed as aforesaid.
Claim 4
Dependent Claim
17 words
A microcompartment according to claim 1 or claim 2 which has the shape generally of a sphere.
Claim 5
Dependent Claim
19 words
A microcompartment according to claim 1 or claim 2 which has the shape generally of a partially collapsed sphere.
Claim 6
Dependent Claim
28 words
A microcompartment according to claim 1 or claim 2 which has the shape generally of a sphere inserted to fit into the central space of an annular disc.
Claim 7
Dependent Claim
26 words
A microcompartment according to any of claims 3 to 5 which has an overall diameter in the range of from about 0.1 to about 100 microns.
Claim 8
Dependent Claim
25 words
A microcompartment according to any of claims 3 to 6 which has a wall thickness in the range of from about 100A to about 1000A.
Claim 9
Dependent Claim
16 words
A microcompartment according to any of the preceding claims wherein the said macromolecules comprise protein molecules.
Claim 10
Dependent Claim
17 words
A microcompartment according to any of claims 1 to 7 wherein the said macromolecules comprise glycoprotein molecules.
Claim 11
Dependent Claim
24 words
A microcompartment according to any of claims 1 to 7 wherein the said macromolecules comprise at least two of protein, glycolipid and glycoprotein molecules.
Claim 12
Dependent Claim
24 words
A microcompartment according to any of claims 8 to 10 wherein the membrane is derived from materials comprised in a naturally occurring cell membrane.
Claim 13
Dependent Claim
22 words
A microcompartment according to any of claims 8 to 10 wherein the membrane is derived from eukaryotic cells or cells of prokaryotes.
Claim 14
Dependent Claim
30 words
A microcompartment according to any of claims 8 to 10 wherein the membrane is derived from materials comprised in whole blood, red blood cell membranes, casein or egg white constituents.
Claim 15
Dependent Claim
26 words
A microcompartment according to any of claims 11 to 13 wherein the membrane contains about 90% of the proteinaceous materials in a naturally occurring cell membrane.
Claim 16
Dependent Claim
14 words
A microcompartment according to any of the preceding claims wherein the membrane encloses phospholipids.
Claim 17
Dependent Claim
18 words
A microcompartment according to any of the preceding claims wherein the membrane encloses one or more magnetic particles.
Claim 18
Dependent Claim
16 words
A microcompartment according to any of the preceding claims wherein the membrane encloses an inert bead.
Claim 19
Dependent Claim
16 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses an antibody.
Claim 20
Dependent Claim
21 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a naturally-occurring or artificially produced proteinaceous substance.
Claim 21
Dependent Claim
19 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses an enzyme or an apo-enzyme.
Claim 22
Dependent Claim
17 words
A microcompartment according to claim 20 wherein the membrane encloses an apo-enzyme together with a corresponding coenzyme.
Claim 23
Dependent Claim
17 words
A microcompartment according to any of the preceding claims wherein the membrane surface presents a specific ligand.
Claim 24
Dependent Claim
31 words
A microcompartment according to claim 22 wherein the membrane surface presents one or more substances selected from the group consisting of a hormone receptor, an antigen, an antibody and an enzyme.
Claim 25
Dependent Claim
25 words
A microcompartment according to any of the preceding claims wherein the ' membrane is comprised of pharmaceutically compatible materials and encloses a pharmacologically active substance.
Claim 26
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has anti-inflammatory properties.
Claim 27
Dependent Claim
14 words
A microcompartment according to claim 25 wherein the pharmacologically active substance is a steroid.
Claim 28
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has anticancer properties.
Claim 29
Dependent Claim
13 words
A microcompartment according to claim 27 wherein the pharmacologically active substance is cisplatin.
Claim 30
Dependent Claim
13 words
A microcompartment according to claim 27 wherein the pharmacologically active substance is doxorubicin.
Claim 31
Dependent Claim
16 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has central nervous system activity.
Claim 32
Dependent Claim
16 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has peripheral nervous system activity.
Claim 33
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has analgetic activity.
Claim 34
Dependent Claim
15 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has local anesthetic activity.
Claim 35
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has narcotic activity.
Claim 36
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has antidepressant activity.
Claim 37
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has antibacterial activity.
Claim 38
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has antifungal activity.
Claim 39
Dependent Claim
14 words
A microcompartment according to claim 37 wherein the pharmacologically active substance is Amphotericin B.
Claim 40
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has antiparasitic activity.
Claim 41
Dependent Claim
20 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has properties beneficial in the treatment of heart disease.
Claim 42
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has immunomodulating activity.
Claim 43
Dependent Claim
14 words
A microcompartment according to claim 41 wherein the pharmacologically active substance has immunostimulafing activity.
Claim 44
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance has immunosuppressive activity.
Claim 45
Dependent Claim
14 words
A microcompartment according to claim 41 wherein the pharmacologically active substance is a leukotriene.
Claim 46
Dependent Claim
14 words
A microcompartment according to claim 41 wherein the pharmacologically active substance is an interleukin.
Claim 47
Dependent Claim
14 words
A microcompartment according to claim 43 wherein the pharmacologically active substance is Cyclosporin A.
Claim 48
Dependent Claim
14 words
A microcompartment according to claim 24 wherein the pharmacologically active substance is a vaccine.
Claim 49
Dependent Claim
27 words
A microcompartment according to any of claims 1 to 15 wherein the membrane is composed of edible materials and encloses a foodstuff or a substance compatible therewith.
Claim 50
Dependent Claim
14 words
A microcompartment according to claim 48 wherein the membrane encloses a food flavoring substance.
Claim 51
Dependent Claim
23 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a substance with herbicidal, fungicidal, acaricidal or insecticidal activity.
Claim 52
Dependent Claim
20 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a substance with growth control activity.
Claim 53
Dependent Claim
16 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a pheremone.
Claim 54
Dependent Claim
19 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses one or more hydrophobic substances.
Claim 55
Dependent Claim
21 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a perfume composition or perfume concentrate composition.
Claim 56
Dependent Claim
17 words
A microcompartment according to any of claims 1 to 17 wherein the membrane encloses a particulate catalyst.
Claim 57
Dependent Claim
30 words
A microcompartment according to any of claims 1 to 21 and 55 wherein the membrane encloses one or more reactant macromolecular substances of molecular weight of at least about 6000.
Claim 58
Independent Claim
56 words
A method of effecting a chemical reaction wherein one or more reactant macromolecular substances of molecular weight of at least about 6000 which is enclosed in a microcompartment as defined in any of claims 1 to 21 and 55 is reacted in a suitable medium with a substance of molecular weight of up to about 1000.
Claim 59
Dependent Claim
33 words
A microcompartment according to claim 20 wherein the enzyme or apoenzyme is selected from the group consisting of alkaline phosphatase, asparaginase, catatase, cholesterol oxidase, cholinesterase, apo-glucoseoxidase, glucoseoxidase, peroxidase, urease, glycerolphosphate oxidase and uricase.
Claim 60
Dependent Claim
13 words
A microcompartment according to claim 58 wherein the enzyme or apo-enzyme is glucoseoxidase.
Claim 61
Dependent Claim
84 words
A process for preparing microcompartments as claimed in any of claims 1 to 14, which comprises exposing a proteinaceous macromolecular substance, which contains a relatively hydrophilic moiety and a relatively hydrophobic moiety, to the solubilization action of a homogeneous mixture of chaotropic ions in water and a dialyzable organic solvent which is not completely miscible with water, if necessary or desired subjecting the mixture to filtration or centrifugation, forming microglubules containing the microcompartment precursors, and dialyzing out the organic solvent and the chaotropic ions.
Claim 62
Dependent Claim
129 words
A process for preparing microcompartments as defined in any of claims 15 to 56, 58 and 59, which comprises exposing a proteinaceous macromolecular substance, which contains a relatively hydrophilic moiety and a relatively hydrophobic moiety, to the solubilization action of a homogeneous mixture of chaotropic ions in water and a dialyzable organic solvent which is not completely miscible with water, if necessary or desired subjecting the mixture to filtration or centrifugation, forming microglobules containing the microcompartment precursors, and dialyzing out the organic solvent and the chaotropic ion, the process being additionally characterized by the features that any soluble or insoluble substances which it is desired be enclosed by the said microcompartments are either present in the original reaction mixture or are added after the optional filtration or centrifugation step.
Claim 63
Dependent Claim
59 words
A process for solubilizing a proteinaceous macromolecular substance, which contains a relatively hydrophilic moiety and a relatively hydrophobic moiety, which comprises subjecting it to the action of a homogeneous mixture of chaotropic ions in water and a dialyzable organic solvent which is not completely miscible with water, and if necessary or desired subjecting the mixture to filtration or centrifugation.
Claim 64
Dependent Claim
59 words
A process for solubilizing a proteinaceous macromolecular substance, which contains a relatively hydrophilic moiety and a relatively hydrophobic moiety, which comprises subjecting it to the action of a homogeneous mixture of chaotropic ions in water and a dialyzable organic solvent which is not completely miscible with water, and if necessary or desired subjecting the mixture to filtration or centrifugation.
Claim 65
Dependent Claim
20 words
A process according to either claim 60 or claim 61, wherein the dialysis step is effected in a dialysis bag.
Claim 66
Dependent Claim
29 words
A process according to any of claims 60, 61 or 63, wherein prior to dialysis the mixture is subjected to vigorous agitation to ensure fine division of the microglobules.
Claim 67
Dependent Claim
15 words
A process according to claim 64 wherein the vigorous agitation is effected by ultrasonic means.
Claim 68
Dependent Claim
25 words
A process according to any of claims 60 to 65 wherein the organic solvent is an aliphatic alcohol containing 4, 5 or 6 carbon atoms.
Claim 69
Dependent Claim
12 words
A process according to claim 66 wherein the aliphatic alcohol is n-butanol.
Claim 70
Dependent Claim
18 words
A process according to any of claims 60 to 67 wherein the chaotropic ion is -SCN or CCI,COOA
Claim 71
Dependent Claim
43 words
A process according to any of claims 60 to 68 wherein substantially equal parts by volume of an aqueous solution of chaotropic ions of concentration in the range of about 20 to about 50 % w/v, and of the organic solvent are used.
Claim 72
Dependent Claim
52 words
A process according to any of claims 60, 61 and 63 to 69, wherein depending upon whether the organic solvent is one the water-solubility of which decreases or increase with a rise in temperature, microglobule formation is effected by respectively raising or lowering the temperature, and/or by diluting the solution with water.
Claim 73
Dependent Claim
127 words
A process for preparing microcompartments in which the peripheral fabric is formed of proteinaceous macromolecules having their relatively hydrophobic and relatively hydrophilic moieties orientated in the reverse sense from that defined in claim 1, which comprises exposing a macromolecular substance, which contains a relatively hydrophilic moiety and a relatively hydrophobic moiety, to the solubilization action of a homogeneous mixture of chaotropic ions in water and a dialyzable organic solvent which is not completely miscible with water, if necessary or desired subjecting the mixture to filtration or centrifugation, forming microglobules containing the microcompartment precursors by the addition of a substantially water immiscible organic solvent and the subsequent creation of a water-in-oil emulsion, and dialyzing out the organic solvent and the chaotropic ions into a substantially immiscible organic solvent.
Claim 74
Dependent Claim
14 words
A process according to claim 71 wherein the substantially immiscible organic solvent is n-decanol.
Claim 75
Dependent Claim
15 words
A microcompartment produced by the process of any of claims 60,61 and 63 to 72.
Claim 76
Dependent Claim
31 words
A pharmaceutical composition comprising as active ingredient one or more pharmacologically active substances enclosed in microcompartments as defined in any of claims 24 to 47, together with a carrier or diluent.
Claim 77
Dependent Claim
30 words
A pharmaceutical composition according to claim 74, wherein at least part of the carrier or diluent is enclosed in the microcompartments together with the one or more pharmacologically active substances.
Claim 78
Dependent Claim
15 words
A pharmaceutical composition according to either claim 74 or claim 75, in unit dosage form.
Claim 79
Dependent Claim
31 words
A pharmaceutical composition according to any of claims 74 to 76, which is constituted in a form suitable for oral, parenteral or rectal administration, or for administration by inhalation or insufflation.
Claim 80
Dependent Claim
28 words
A microcompartment as claimed in any of claims 1 to 56, 58, 59 and 73, wherein the peripheral membrane consists essentially of a monomolecular layer of said macromolecules.
Claim 81
Dependent Claim
77 words
A semipermeable microcompartment which is artificially prepared by reassembly of synthetic polymeric macromolecules and which is defined by a peripheral membrane consisting substantially of a layer of said macromolecules, each of which comprises a relatively hydrophilic moiety and a relatively hydrophobic moiety and wherein the majorityy of such macromolecules forming the membrane are disposed with their relatively hydrophilic moieties orientated outwardly from the microcompartment and their relatively hydrophobic moieties orientated inwardly towards the interior of the microcompartment.
Claim 82
Dependent Claim
77 words
A semipermeable microcompartment which is artificially prepared by reassembly of synthetic polymeric macromolecules and which is defined by a peripheral membrane consisting substantially of a layer of said macromolecules, each of which comprises a relatively hydrophilic moiety and a relatively hydrophobic moiety and wherein the majorityy of such macromolecules forming the membrane are disposed with their relatively hydrophilic moieties orientated outwardly from the microcompartment and their relatively hydrophobic moieties orientated inwardly towards the interior of the microcompartment.
Claim 83
Dependent Claim
26 words
A microcompartment according to claim 79, wherein the said synthetic polymeric macromolecules result from the attachment of a relatively hydrophilic polymer to a relatively hydrophobic residue.
References Cited (Backward Citations)
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