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US 12,551,437 B2Granted
Liposome compositions comprising weak acid drugs and uses thereof
AssigneePharmosa Biopharm Inc.
InventorsPei Kan, Yi Fong Lin, Ko Chieh Chen
Life of this patent
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Abstract
The present invention relates to a pharmaceutical composition comprising a weak acid drug, with the use of a bicarbonate salt to achieve a high incorporation of the drug into the liposome and a better therapeutic efficacy. Also disclosed is a method for treating a respiratory disease using the pharmaceutical composition disclosed herein.
Claims20
A pharmaceutical composition comprising liposomes, said liposomes comprising:
- (a) a lipid bilayer, comprising vesicle-forming lipid;
- and
- (b) an internal aqueous medium inside the lipid bilayer, comprising a bicarbonate salt and a weak acid drug with a pKa between about 1 to about 6,
- wherein the liposomes are suspended in an external medium, the concentration of the bicarbonate salt is about 50 mM to less than about 1000 mM, the pH of the external medium is above the pKa of the weak acid drug and the vesicle-forming lipid comprises a mixture of a first phospholipid and a second phospholipid or a mixture of a first phospholipid and a charged lipid, and
- wherein the encapsulation efficiency of the weak acid drug is at least 50%.
2 more elements
A pharmaceutical composition comprising liposomes, said liposomes comprising:
- (a) a lipid bilayer, comprising a mixture of a first phospholipid that is HSPC, DSPC, DPPC, DMPC or any combination thereof, a second phospholipid that is DSPG, DPPG, DMPG, PEG-DSPE, or any combination thereof and cholesterol or a first phospholipid, that is HSPC, DSPC, DPPC, DMPC or any combination thereof, a charged lipid that is stearylamine, 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), 3β-[N-(N′,N′-dimethylaminoethane)-carbamoyl]cholesterol (DC-Cholesterol), (GL67), N4-Cholesteryl-Spermine dimethyldioctadecylammonium (DDAB), 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA), ethylphosphocholine (ethyl PC) or any combination thereof and cholesterol;
- and
- (b) an internal aqueous medium inside the lipid bilayer, comprising 50 mM to 800 mM bicarbonate salt and a prostaglandin,
- wherein the liposomes are suspended in an external medium, the pH of the external medium is above the pKa of the prostaglandin, and the encapsulation efficiency is over 50%.
1 more element
Dependencies are inferred from the claim text.