Antibiotic formulation and use for bacterial infections
AssigneeNeXstar Pharmaceuticals, Inc.
InventorsEvan M. Hersch, Eskild A. Petersen, Richard T. Proffitt, Kevin R. Bracken, Su-Ming Chiang
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Abstract
A liposomal aminoglycoside formulation comprising a neutral lipid, a negatively charged lipid and a sterol. The formulation contains unilamellar vesicles having an average size below 100 nm. A process of making liposomes containing an aminoglycoside is provided. A method is also provide for the treatment of drug susceptible and drug resistant bacteria.
Claims26
Liposomes comprising an encapsulated aminoglycoside wherein the liposomes are unilamellar vesicles comprised of a neutral lipid, cholesterol and a negatively charged lipid and having an average size of less than 100 nm which are stable in liquid form for at least 2 weeks at 22.degree. C. without significant change in size or loss of more than 10% of the encapsulated aminoglycoside wherein the negatively charged lipid is less than 20% total lipid.
A composition for treating a bacterial infection in a patient comprising an aminoglycoside encapsulated in liposomes, wherein the liposomes are comprised of a cholesterol, a neutral lipid and a negatively charged lipid, wherein said negatively charged lipid is less than 20% of the total lipid and wherein the liposomes consist of unilamellar vesicles having an average size of less than 100 nm.
A composition for inhibiting bacterial growth in a patient comprising an aminoglycoside encapsulated in liposomes, wherein the liposomes are comprised of a cholesterol, a neutral lipid and a negatively charged lipid, wherein the negatively charged lipid is less than 20% of the total lipid and wherein said liposomes consist of unilamellar vesicles having an average size of less than 100 nm.
A method of treating a bacterial infection in a patient comprising the delivery to the patient of an effective amount of liposomes comprising an encapsulated aminoglycoside, wherein the liposomes are comprised of a cholesterol, a neutral lipid and a negatively charged lipid, wherein said negatively charged lipid is less than 20% of the total lipid and wherein the liposomes consist of unilamellar vesicles having an average size of less than 100 nm.
A method of inhibiting bacterial growth in a patient comprising the delivery to the patient of an effective amount of liposomes comprising an encapsulated aminoglycoside, wherein the liposomes are comprised of a cholesterol, a neutral lipid and a negatively charged lipid, wherein the negatively charged lipid is less than 20% of the total lipid and wherein said liposomes consist of unilamellar vesicles having an average size of less than 100 nm.
A method of making liposomes comprising an encapsulated aminoglycoside, said method comprising:
- a) forming a lipid powder comprised of a cholesterol, a neutral lipid, and a negatively charged lipid, wherein the negatively charged lipid is less than 20% of the total lipid;
- b) mixing the powder with an aminoglycoside;
- c) hydrating the mixture whereby the aminoglycoside becomes encapsulated;
- and
- d) applying a shearing force whereby liposomes consisting of unilamellar vesicles having an average size of less than 100 nm are obtained.
Dependencies are inferred from the claim text.