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Claims for Patent: 6,171,613

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Claims for Patent: 6,171,613

Title: Method for producing liposomes with increased percent of compound encapsulated
Abstract:The efficiency of encapsulating a drug into a liposomal formulation is increased by use of a lipid having a carbon chain containing from about 13 to about 28 carbons during preparation of the liposomes. Preferably the liposomes are multivesicular liposomes.
Inventor(s): Ye; Qiang (San Diego, CA), Sankaram; Mantripragada Bhima (San Diego, CA)
Assignee: SkyePharma Inc. (San Diego, CA)
Application Number:09/431,525
Patent Claims: 1. A method for encapsulating at least one biologically active compound in a liposome comprising

a) obtaining a liposome, by any conventional means, having the substance encapsulated therein and having at least one first amphipathic lipid having a carbon chain from about 1 to about 12 carbons in the lipid component of the formulation;

b) determining the percent amount of the encapsulated compound; and

c) substituting said at least one first amphipathic lipid having a carbon chain from about 1 to about 12 carbons in the lipid component of the formulation with at least one second amphipathic lipid with a substantially similar chemical structure having from one to 16 more carbons in a fatty acyl chain of the second lipid;

wherein the resulting percent of the compound encapsulated is from about 0.2 to about 85 percent.

2. The method of claim 1 wherein the liposome is multilamellar.

3. The method of claims 1 wherein the liposome is multivesicular.

4. The method of claim 1 wherein the number of carbons in the amphipathic lipid is in the range from about 14 to 22.

5. The method of claim 2 wherein the amphipathic lipid is selected from the group consisting of










1,2-dipalmitoyl-sn-glycero-3-phosphoglycerol and


6. The method of claim 2 wherein the amphipathic lipid is saturated.

7. The method of claim 2 wherein the amphipathic lipid is unsaturated.

8. The method of claim 1 wherein subsequent batches of liposome formulations are made by repeating step c).
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