EP0198765A2
Expired / Lapsed
EP
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Preparation of liposomes
Assignee: Georgetown University
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Filing: 1986-04-03
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Granted: —
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Expires: 2006-04-03
Abstract
Abstract A process for encapsulating a drug or physiologically active substance in a liposome, which comprises forming a dispersion of a liposome-forming lipid, a physiologically active substance, and a lipophilic chelating agent, wherein liposomes are produced in the dispersion, and recovering the liposome-encapsulated drug or physiologically active substance from the dispersion, is disclosed along with liposomes produced in this manner.
Inventors
- 👤 Aquilur Rahman
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-25 07:25
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1277; A61K9/1271
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
77 words
A process for encapsulating a physiologically active substance in a liposome which comprises: (a) forming a dispersion of a liposome-forming lipid, a physiologically active substance, and a compound of formula R-K, wherein R is a lipophilic portion of said compound which is capable of inserting into a liposomal lipid bilayer and K is a chelating portion of said compound, whereby liposomes are produced in said dispersion; and (b) recovering the liposome-encapsulated physiologically active substance from said dispersion.
Claim 2
Dependent Claim
77 words
A process for encapsulating a physiologically active substance in a liposome which comprises: (a) forming a dispersion of a liposome-forming lipid, a physiologically active substance, and a compound of formula R-K, wherein R is a lipophilic portion of said compound which is capable of inserting into a liposomal lipid bilayer and K is a chelating portion of said compound, whereby liposomes are produced in said dispersion; and (b) recovering the liposome-encapsulated physiologically active substance from said dispersion.
Claim 3
Dependent Claim
26 words
The process of Claim 1, wherein said dispersion is formed by stirring a mixture comprising water, the liposome-forming lipid, compound R-K, and the physiologically active substance.
Claim 4
Dependent Claim
15 words
The process of Claim 1, wherein said dispersion is sonicated prior to recovering the liposomes.
Claim 5
Dependent Claim
15 words
The process of Claim 1 wherein the physiologically active substance is doxorubicin, daunorubicin or cis-platinum.
Claim 6
Dependent Claim
33 words
The process of Claim 1, wherein said compound of formula R-K is a covalent compound formed by the condensation reaction of a polycarboxylic chelating agent and an alkyl or alkenyl amine or hydroxide.
Claim 7
Dependent Claim
65 words
In a process for producing a liposome-encapsulated physiologically active substance, an improvement which comprises incorporating a compound of formula R-K, wherein R is a lipophilic portion of said compound that is capable of inserting into a liposomal lipid bilayer and K is a chelating portion of said compound, into a mixture of liposome-forming lipid and physiologically active substance from which said liposomes are being prepared.
Claim 8
Dependent Claim
65 words
In a process for producing a liposome-encapsulated physiologically active substance, an improvement which comprises incorporating a compound of formula R-K, wherein R is a lipophilic portion of said compound that is capable of inserting into a liposomal lipid bilayer and K is a chelating portion of said compound, into a mixture of liposome-forming lipid and physiologically active substance from which said liposomes are being prepared.
Claim 9
Dependent Claim
12 words
The liposome-encapsulated physiologically active substance produced by the process of Claim 1.
Claim 10
Dependent Claim
17 words
In a liposome-encapsulated drug composition, an improvement which comprises a lipophilic chelating agent entrapped in said composition.
Claim 11
Dependent Claim
17 words
In a liposome-encapsulated drug composition, an improvement which comprises a lipophilic chelating agent entrapped in said composition.
Claim 12
Dependent Claim
61 words
The composition of Claim 8, wherein the lipophilic chelating agent is formed by a condensation reaction between diethylenetriaminepentaacetic acid or ethylenediaminetetracetic acid and an amine of the formula RNH 2 , wherein R is an alkyl group containing from 12 to 22 carbon atoms or an alkenyl group containing from 12 to 22 carbon atoms and at least one double bond.
Claim 13
Dependent Claim
41 words
A liposome-encapsulated physiologically active substance, wherein said liposome comprises a bilayer having inserted therein an R portion of a compound of formula R-K wherein R is a lipophilic portion of said compound and K is a chelating portion of said compound.
Claim 14
Dependent Claim
41 words
A liposome-encapsulated physiologically active substance, wherein said liposome comprises a bilayer having inserted therein an R portion of a compound of formula R-K wherein R is a lipophilic portion of said compound and K is a chelating portion of said compound.
Claim 15
Dependent Claim
20 words
The liposome-encapsulated physiologically active substance of Claim 10, wherein R comprises a hydrocarbyl portion comprising at least 6 carbon atoms.
Claim 16
Dependent Claim
18 words
The liposome-encapsulated physiologically active substance of Claim 11, wherein said hdyrocarbyl portion comprises at least 12 carbon atoms.
Claim 17
Dependent Claim
14 words
The liposome-encapsulated physiologically active substance of Claim 11, wherein R is an alkenyl group.
Claim 18
Dependent Claim
14 words
The liposome-encapsulated physiologically active substance of Claim 11, wherein R is an alkyl group.
Claim 19
Dependent Claim
25 words
The liposome-encapsulated physiologically active substance of Claim 14, wherein R is a dodecyl, tridecyl, tetradecyl, pentadecyl, hexadecyl, heptadecyl, octadecyl, nonadecyl, icosyl, henicosyl, or docosyl group.
Claim 20
Dependent Claim
18 words
The liposome-encapsulated physiologically active substance of Claim 10, where K chelates through at least one carboxylic acid group.
Claim 21
Dependent Claim
19 words
The liposome-encapsulated physiologically active substance of Claim 16, where K comprises an aminocarboxylic acid, hydroxycarboxylic acid, or polycarboxylic acid.
Claim 22
Dependent Claim
65 words
The liposome-encapsulated physiologically active substance of Claim 16, wherein K comprises a portion of formula -N(K 1 )CH 2 CH 2 N(R 2 )(R 3 ) wherein K 1 , K 2 , and K 3 independently represent H or -CH 2 C0 2 H, with the proviso that no more than two of K l , K 2 , and K 3 are H.
Claim 23
Dependent Claim
31 words
The liposome-encapsulated physiologically active substance Claim 18, wherein R-K is a condensation product of diethylenetriaminepentaacetic acid or ethylenediaminetetraacetic acid and an amine formula RNH 2 or an alcohol of formula ROH.
Claim 24
Dependent Claim
16 words
The liposome-encapsulated physiologically active substance Claim 10, wherein said physiologically active substance is doxarubicen or daunorubicin.
References Cited (Backward Citations)
No citation records indexed.
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