Non-pegylated long-circulating liposomes
First Claim
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1. A process for manufacture of long circulating non-pegylated liposomes comprising:
- dissolving one or more phospholipids and one or more sterols in a solvent or mixture of solvents;
wherein the one or more phospholipids is a saturated phosphatidylcholine selected from the group consisting of distearoyl phosphatidylcholine (DSPC), hydrogenated soya phosphatidyl-choline (HSPC) and mixtures thereof;
removing the solvent or mixture of solvents and adding an aqueous hydration media to the phospholipids and sterols;
or adding an aqueous hydration media to the phospholipids and sterols in the solution; and
removing the solvent or mixture of solvents;
wherein the aqueous hydration media consists essentially of ammonium sulfate and sucrose and the amount of the aqueous hydration media used is in the range of 10 to 35 ml for each mmole of the phospholipid present to form long circulating non-pegylated liposomes; and
removing ammonium sulphate from extra liposomal hydration medium by dialysis using a sucrose-histidine buffer solution.
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Abstract
The present invention provides a long circulating non-pegylated liposomal doxorubicin hydrochloride composition for parenteral administration and a process for its preparation. The circulation time in Swiss albino mice is at least 25 times longer than conventional non-liposomal formulations. The non-pegylated liposomes are stable, exhibit low toxicity and have been found to be efficacious in different tumor models.
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Citations
26 Claims
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1. A process for manufacture of long circulating non-pegylated liposomes comprising:
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dissolving one or more phospholipids and one or more sterols in a solvent or mixture of solvents; wherein the one or more phospholipids is a saturated phosphatidylcholine selected from the group consisting of distearoyl phosphatidylcholine (DSPC), hydrogenated soya phosphatidyl-choline (HSPC) and mixtures thereof; removing the solvent or mixture of solvents and adding an aqueous hydration media to the phospholipids and sterols;
or adding an aqueous hydration media to the phospholipids and sterols in the solution; and
removing the solvent or mixture of solvents;wherein the aqueous hydration media consists essentially of ammonium sulfate and sucrose and the amount of the aqueous hydration media used is in the range of 10 to 35 ml for each mmole of the phospholipid present to form long circulating non-pegylated liposomes; and removing ammonium sulphate from extra liposomal hydration medium by dialysis using a sucrose-histidine buffer solution. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 26)
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20. A process for manufacture of non-pegylated liposomes comprising:
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forming a lipid film by evaporating a solvent from a lipid solution comprising one or more phospholipids, a sterol, and a solvent; and hydrating the lipid film by adding an aqueous hydration media to form a non-pegylated liposomal composition;
wherein the aqueous hydration media consists essentially of ammonium sulfate and sucrose and wherein the amount of aqueous hydration media used is in the range of 10 to 35 ml for each mmole of phospholipid present in the lipid solution; andremoving ammonium sulphate from extra liposomal hydration medium using a sucrose-histidine buffer solution. - View Dependent Claims (21, 22, 23, 24, 25)
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Specification