Liposomal composition containing mild acidic active agent
AssigneesTaiwan Liposome Co., Ltd., Tlc Biopharmaceuticals, Inc.
InventorsKe-Ming Huang, He-Ru Chen, Keelung Hong
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Abstract
Provided is a method for preparing a liposomal composition. The method comprises the step of contacting a liposome solution with a mild acidic agent for a limited time. The liposome solution comprises a weak acid salt encapsulated within an aqueous interior space separated from the aqueous medium by a membrane comprised of a lipid mixture containing one or more lipids and a hydrophilic polymer conjugated lipid at a molar percentage of less than 3% based on the total amount of the lipid mixture. The time for encapsulating the agent to a desired amount at a predetermined ratio to lipids is dramatically reduced even under a condition without elevating the temperature to above ambient environment.
Claims15
A delivery vehicle, comprising a liposome in an aqueous medium and a mild acidic agent encapsulated within the liposome, wherein the liposome has an aqueous interior space with a combination of a weak acid salt and a polyprotic acid therein, and the aqueous interior space is separated from the aqueous medium by a membrane of the liposome;
- wherein the membrane comprises a lipid mixture containing one or more lipids and a polyethylene glycol-derived lipid, wherein the polyethylene glycol-derived lipid is at a molar percentage of 0.5 to 3% based on the total amount of the lipid mixture;
- the weak acid salt is sodium acetate or potassium acetate;
- the polyprotic acid is selected from the group consisting of citric acid, succinic acid, tartaric acid and a combination thereof;
- wherein the concentration of the weak acid salt is between 100 mM and 800 mM;
- wherein the concentration of the polyprotic acid is not greater than 50 mM;
- and
- the combination of the weak acid salt and the polyprotic acid is at a molar ratio of weak acid salt to polyprotic acid ranging from 8:1 to 200:1.
A liposomal composition comprising a liposome in an aqueous medium, wherein the liposome has an aqueous interior space with a combination of a weak acid salt and a polyprotic acid therein at a molar ratio of weak acid salt to polyprotic acid ranging from 8:1 to 200:1, and the aqueous interior space is separated from the aqueous medium by a membrane of the liposome;
- and
- a mild acidic agent encapsulated within the liposome;
- wherein the concentration of the weak acid salt is between 100 mM and 800 mM;
- wherein the concentration of the polyprotic acid is not greater than 50 mM;
- and
- wherein the membrane comprises a lipid mixture containing one or more lipids and a polyethylene glycol-derived lipid, wherein the polyethylene glycol-derived lipid is at a molar percentage of 0.5 to 3% based on the total amount of the lipid mixture.
A liposomal composition comprising:
- a liposome having a membrane comprised of one or more lipids and a polyethylene glycol-derived lipid, wherein the polyethylene glycol-derived lipid is at a molar percentage of 0.5 to 3%;
- and a combination of an acetate salt and a citric acid at a molar ratio of acetate salt to citric acid ranging from 8:1 to 200:1 encapsulated within the liposome;
- wherein the concentration of the acetate salt is between 100 mM and 800 mM;
- wherein the concentration of the citric acid is not greater than 50 mM;
- and
- prostaglandin entrapped by the combination of the acetate salt and the citric acid encapsulated within the liposome.
Dependencies are inferred from the claim text.