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EP0272091A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Delivery vehicles with amphiphile-associated active ingredient

Assignee: Nexstar Pharmaceuticals Inc
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Filing: 1987-12-15
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Granted: —
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Expires: 2007-12-15
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Abstract

Abstract Delivery vehicles comprising an outer biocompatible encapsulating layer, an inner amphiphilic active ingredient-associated layer and an active ingredient are described. The delivery vehicles are biocompatible and are capable of solubilizing the active ingredient for in vivo delivery to bodily tissue or other bodily systems. Uses include nuclear magnetic resonance imaging and therapeutic drug delivery.

Inventors

  • 👤 Crispin George Stewart Eley
  • 👤 Paul Gardner Schmidt
  • 👤 Gary Fujii

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-23 09:04
CPC Classifications
H; H02; H02M; H02M1/00; H02M1/08; A; A61; A61K; A61K49/00; A61K49/06; A61K49/18; A61K49/1806; A61K49/1812; A61K9/00; A61K9/10; A61K9/127; A61K9/1277; H02M1/06

Claims Analysis

Total Claims: 31
Claim 1
Independent Claim 81 words
A delivery vehicle for an active ingredient, said delivery vehicle having a size from about 20 nm to about 10,000 nm in diameter and comprising an active ingredient phase or phases, an amphiphilic material associated with said active ingredient phase or phases to form one or more amphiphile-associated substrates, and at least one encapsulating layer including at least one said layer associated with one or more of said amphiphile-associated substrates, the outer of said encapsulating layers being a biocompatible encapsulating layer.
Claim 2
Dependent Claim 81 words
A delivery vehicle for an active ingredient, said delivery vehicle having a size from about 20 nm to about 10,000 nm in diameter and comprising an active ingredient phase or phases, an amphiphilic material associated with said active ingredient phase or phases to form one or more amphiphile-associated substrates, and at least one encapsulating layer including at least one said layer associated with one or more of said amphiphile-associated substrates, the outer of said encapsulating layers being a biocompatible encapsulating layer.
Claim 3
Dependent Claim 20 words
The delivery vehicle of claim 1 wherein said active ingredient comprises a material selected from diagnostic agents and therapeutic agents.
Claim 4
Dependent Claim 30 words
The delivery vehicle of any one of the preceding claims wherein said amphiphilic material comprises at least one fatty acid, phospholipid, phosphatidic acid, diglyceride, triglyceride, alcohol, amine, phosphate and/or sulfate.
Claim 5
Dependent Claim 18 words
The delivery vehicle of claim 3 wherein said amphiphilic material comprises a fatty acid or a phosphatidic acid.
Claim 6
Dependent Claim 44 words
The delivery vehicle of claim 4 wherein said amphiphilic material comprises a fatty acid having an aliphatic chain of from 10 to 28 carbons in length and/or a phosphatidic acid having an aliphatic chain or chains of from 10 to 28 carbons in length.
Claim 7
Dependent Claim 36 words
The delivery vehicle of any one of the preceding claims wherein said amphiphilic material includes a hydrophilic portion associated with said active ingredient phase or phases and a hydrophobic portion associated with a said encapsulating layer.
Claim 8
Dependent Claim 19 words
The delivery vehicle of claim 6 wherein said hydrophilic portion comprises a carboxylic, hydroxyl, amino, phosphato or sulfato group.
Claim 9
Dependent Claim 27 words
The delivery vehicle of claim 6 or 7 wherein said hydrophobic portion comprises an aliphatic hydrocarbon, cycloaliphatic hydrocarbon, aromatic-substituted aliphatic hydrocarbon, cycloaliphatic-substituted aliphatic hydrocarbon or polyoxyethylene group.
Claim 10
Dependent Claim 27 words
The delivery vehicle of any one of claims 6 - 8 wherein said hydrophobic portion comprises an aliphatic chain of from 10 to 28 carbons in length.
Claim 11
Dependent Claim 19 words
The delivery vehicle of any one of the preceding claims wherein said biocompatible encapsulating layer comprises a phospholipid material.
Claim 12
Dependent Claim 25 words
The delivery vehicle of any one of the preceding claims having a single said encapsulating layer, which layer further constitutes said outer biocompatible encapsulating layer.
Claim 13
Dependent Claim 25 words
A delivery vehicle according to any one of the preceding claims having a size of from about 20 nm to about 10,000 nm in diameter.
Claim 14
Dependent Claim 28 words
The delivery vehicle of any one of the preceding claims wherein said delivery vehicle has a size of from about 35 nm to about 100 nm in diameter.
Claim 15
Dependent Claim 24 words
The delivery vehicle of claim 13 wherein said delivery vehicle has a size of from about 50 nm to about 80 nm in diameter.
Claim 16
Dependent Claim 20 words
The delivery vehicle of claim 12 having a size of from about 20 nm to about 100 nm in diameter.
Claim 17
Dependent Claim 80 words
The delivery vehicle of any one of the preceding claims wherein said amphiphilic material comprises fatty acid having an aliphatic chain of from 12 to 18 carbons in length, fatty acid having an aliphatic chain of from 22 to 24 carbons in length, and/or a phosphatidic acid having an aliphatic chain or chains of from 12 to 18 carbons in length, and wherein said phospholipid material comprises an aliphatic chain or chains of from 10 to 20 carbons in length.
Claim 18
Dependent Claim 61 words
The delivery vehicle of claim 16 wherein said amphiphilic material comprises at least one fatty acid selected from lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, docosanoic acid, tetra­cosanoic acid, dimyristoylphosphatidic acid, di­palmitoylphosphatidic acid, and distearoylphosphatidic acid, and wherein said phospholipid material comprises a phosphatidylcholine having an aliphatic chain or chains of from 10 to 20 carbons in length.
Claim 19
Dependent Claim 73 words
The delivery vehicle of any one of the preceding claims wherein the amphiphilic material comprises lauric acid, myristic acid, or palmitic acid and having at least one encapsulating layer, including an outer biocompatible encapsulating layer and at least one encapsulating layer associated with one or more of said magnetite amphiphile-associated substrates, at least one of said layer or layers comprising a mixture of cholesterol and a phosphatidylcholine selected from dimyristoylphosphatidylcholine, di­palmitoylphosphatidylcholine and distearoylphos­phatidylcholine.
Claim 20
Dependent Claim 16 words
The delivery vehicle of any one of the preceding claims wherein the active ingredient is magnetite.
Claim 21
Dependent Claim 19 words
The delivery vehicle of any one of claims 1 to 18 wherein the active ingredient is a therapeutic agent.
Claim 22
Dependent Claim 15 words
The delivery vehicle of claim 20 wherein said therapeutic active ingredient comprises an anti­neoplastic agent.
Claim 23
Dependent Claim 14 words
The delivery vehicle of claim 21 wherein said antineoplastic agent is bisanthrene or cisplatin.
Claim 24
Dependent Claim 15 words
The delivery vehicle of claim 20 wherein said therapeutic active ingredient comprises an antifungal agent.
Claim 25
Dependent Claim 15 words
The delivery vehicle of claim 23 wherein said antifungal agent is amphotericin B or miconazole.
Claim 26
Dependent Claim 68 words
A process for preparing a delivery vehicle as defined in any one of the preceding claims which comprises forming an association between the active ingredient phase and the amphiphilic material to form an amphiphile-associated substrate, and encapsulating said amphiphile-associated substrate within at least one encapsulating layer including at least one said layer associated with said amphiphile-associated substrate, the outer of said encapsulating layers being a biocompatible encapsulating layer.
Claim 27
Dependent Claim 42 words
The process of claim 25 including the steps of forming an association between the hydrophilic portion of said amphiphilic material and said active ingredient phase, and forming an association between the hydrophobic portion of said amphiphilic material and a said encapsulating layer.
Claim 28
Dependent Claim 41 words
A delivery vehicle according to any one of claims 1 to 24 for use in a method of treatment of the human or animal body by therapy or surgery or in a diagnostic method practised on the human or animal body.
Claim 29
Dependent Claim 24 words
A delivery vehicle according to claim 19 for use in a method of nuclear magnetic resonance imaging practised on the human or animal body.
Claim 30
Dependent Claim 25 words
A delivery vehicle according to claim 21 or 22 for use in a method of treatment of neoplastic disease in the human or animal body.
Claim 31
Dependent Claim 24 words
A delivery vehicle according to claim 23 or 24 for use in a method of anti-fungal treatment practised on the human or animal body.

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