EP0272091B1
Expired / Lapsed
EP
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Delivery vehicles with amphiphile-associated active ingredient
Assignee: Nexstar Pharmaceuticals Inc
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Filing: 1987-12-15
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Granted: 1993-05-26
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Expires: 2007-12-15
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 05:39
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: 27
Claim 1
Independent Claim
119 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 a lipid material enclosing an amphiphile-associated substrate in the essential absence of a solution - phase inner volume, which includes: an active ingredient phase, an amphiphilic material capable of associating with said active ingredient and having a polar hydrophilic portion and a lipophilic portion, said polar hydrophilic portion of said amphiphilic material being associated with said active ingredient phase to form the said amphiphile - associated substrate; and a single, biocompatible encapsulating monolayer surrounding the said amphiphile-associated substrate, comprising molecules having lipophilic tails associated with the lipophilic portion of the amphiphile - associated substrate.
Claim 2
Dependent Claim
119 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 a lipid material enclosing an amphiphile-associated substrate in the essential absence of a solution - phase inner volume, which includes: an active ingredient phase, an amphiphilic material capable of associating with said active ingredient and having a polar hydrophilic portion and a lipophilic portion, said polar hydrophilic portion of said amphiphilic material being associated with said active ingredient phase to form the said amphiphile - associated substrate; and a single, biocompatible encapsulating monolayer surrounding the said amphiphile-associated substrate, comprising molecules having lipophilic tails associated with the lipophilic portion of the amphiphile - associated substrate.
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
34 words
The delivery vehicle of any one of the preceding claims wherein said amphiphilic material comprises at least one of fatty acids, phosphatidyl glycerols, phosphatidic acids, diglycerides, triglycerides, hydrophobic substituted alcohols, amines, phosphates and/or sulfates.
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
48 words
The delivery vehicle of claim 4 wherein said amphiphilic material comprises a fatty acid having a lipophilic portion aliphatic chain of from 10 to 28 carbons in length and/or a phosphatidic acid having a lipophilic portion aliphatic chain or chains of from 10 to 28 carbons in length.
Claim 7
Dependent Claim
23 words
The delivery vehicle of any one of the preceding claims wherein said hydrophilic portion comprises a carboxylic, hydroxyl, amino, phosphato or sulfato group.
Claim 8
Dependent Claim
25 words
The delivery vehicle of claim 6 wherein said lipophilic portion comprises an aliphatic hydrocarbon, cycloaliphatic hydrocarbon, aromatic-substituted aliphatic hydrocarbon, cycloaliphatic-substituted aliphatic hydrocarbon or polyoxyethylene group.
Claim 9
Dependent Claim
24 words
The delivery vehicle of claim 6 or 7 wherein said lipophilic portion comprises an aliphatic chain of from 10 to 28 carbons in length.
Claim 10
Dependent Claim
19 words
The delivery vehicle of any one of the preceding claims wherein said biocompatible encapsulating monolayer comprises a phospholipid material.
Claim 11
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 12
Dependent Claim
24 words
The delivery vehicle of claim 10 wherein said delivery vehicle has a size of from about 50 nm to about 80 nm in diameter.
Claim 13
Dependent Claim
25 words
The delivery vehicle of any one of claims 1 to 10 having a size of from about 20 nm to about 100 nm in diameter.
Claim 14
Dependent Claim
85 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 biocompatible encapsulating monolayer comprises a phospholipid material comprising an aliphatic chain or chains of from 10 to 20 carbons in length.
Claim 15
Dependent Claim
63 words
The delivery vehicle of claim 13 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 a lipophilic portion aliphatic chain or chains of from 10 to 20 carbons in length.
Claim 16
Dependent Claim
41 words
The delivery vehicle of any one of the preceding claims wherein the amphiphilic material comprises lauric acid, myristic acid, or palmitic acid and said biocompatible encapsulating monolayer comprises a mixture of cholesterol and a phosphatidylcholine selected from dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine.
Claim 17
Dependent Claim
16 words
The delivery vehicle of any one of the preceding claims wherein the active ingredient is magnetite.
Claim 18
Dependent Claim
19 words
The delivery vehicle of any one of claims 1 to 15 wherein the active ingredient is a therapeutic agent.
Claim 19
Dependent Claim
15 words
The delivery vehicle of claim 17 wherein said therapeutic active ingredient comprises an antineoplastic agent.
Claim 20
Dependent Claim
14 words
The delivery vehicle of claim 18 wherein said antineoplastic agent is bisanthrene or cisplatin.
Claim 21
Dependent Claim
15 words
The delivery vehicle of claim 17 wherein said therapeutic active ingredient comprises an antifungal agent.
Claim 22
Dependent Claim
15 words
The delivery vehicle of claim 20 wherein said antifungal agent is amphotericin B or miconazole.
Claim 23
Dependent Claim
104 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 in an aqueous phase to form an amphiphile - associated substrate wherein the polar hydrophilic portion of the amphiphilic material is associated with the active ingredient, and encapsulating said amphiphile - associated substrate within an encapsulating monolayer comprising molecules having lipophilic tails associated with the lipophilic portion of said amphiphile - associated substrate so as to enclose the amphiphile - associate substrate in the absence of a solution - phase volume inside said monolayer.
Claim 24
Dependent Claim
41 words
A delivery vehicle according to any one of claims 1 to 21 for use in a method of treatment of the human or animal body by therapy or surgery or in a diagnostic method practiced on the human or animal body.
Claim 25
Dependent Claim
24 words
A delivery vehicle according to claim 16 for use in a method of nuclear magnetic resonance imaging practiced on the human or animal body.
Claim 26
Dependent Claim
25 words
A delivery vehicle according to claim 18 or 19 for use in a method of treatment of neoplastic disease in the human or animal body.
Claim 27
Dependent Claim
26 words
A delivery vehicle according to claim 20 or 21 for use in a method of anti - fungal treatment practiced on the human or animal body.
References Cited (Backward Citations)
No citation records indexed.
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