Liposome composition comprising liposomal prodrug of mitomycin c and method of manufacture
AssigneesLipomedix Pharmaceuticals Ltd., Shaare Zedek Scientific Ltd.
InventorsAlberto Gabizon, Patricia Ohana, Hilary Shmeeda
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Abstract
A liposome composition comprising a lipophilic prodrug of mitomycin C having an improved pharmacokinetic profile is described. A method for preparing the composition with a solvent system comprised of ethanol and tertiary butanol mixed at an adequate ratio is also described. In an embodiment, the liposome composition is a population of lipid nanoparticles and a pharmaceutically acceptable vehicle, wherein the population of lipid nanoparticles is comprised of a first fraction of spherical liposomes and a second fraction of rod-shaped lipid nanoparticles, where the second fraction is less than about 15% of the population of lipid nanoparticles.
Claims33
A composition comprising:
- a population of lipid nanoparticles and
- a pharmaceutically acceptable vehicle, wherein the population of lipid nanoparticles is comprised of a first fraction of spherical liposomes and a second fraction of rod-shaped lipid nanoparticles, where the second fraction is less than 15% of the population of lipid nanoparticles, wherein the spherical liposomes are comprised of a vesicle-forming lipid, a lipophilic prodrug of mitomycin C, and an optional lipid component.
A method for the manufacture of liposomes, comprising:
- dissolving a vesicle-forming lipid, a lipophilic prodrug of mitomycin C, and an optional lipid component in a solvent mixture comprised of ethanol and tertiary butanol in an ethanol/tertiary-butanol ratio (v/v) of between about 2:1 to 20:1 to form a dissolved lipid solution, and
- forming a population of lipid nanoparticles, wherein the population of lipid nanoparticles is comprised of a first fraction of spherical liposomes and a second fraction of rod-shaped lipid nanoparticles, where the second fraction is less than about 15% of the population of lipid nanoparticles.
(canceled)
A population of lipid nanoparticles prepared by a process, comprising:
- dissolving a vesicle-forming lipid, a lipophilic prodrug of mitomycin C, and an optional lipid component in a solvent mixture comprised of ethanol and tertiary butanol in an ethanol/tertiary-butanol ratio of between about 2:1 to 20:1 to form a dissolved lipid solution;
- and
- mixing the dissolved lipid solution with an aqueous buffer to form a population of lipid nanoparticles, wherein the population of lipid nanoparticles is comprised of a first fraction of spherical liposomes and a second fraction of rod-shaped lipid nanoparticles, where the second fraction is less than 15% of the population of lipid nanoparticles.
(canceled)
Dependencies are inferred from the claim text.