# US 10,765,633 B2 · Formulation comprising liposomes > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,765,633 B2 - Document ID: US10765633B2 - Status: Granted - Kind: B2 - Application number: 16/713,027 - Filed: 2019-12-13 - Published: 2020-06-18 - Granted: 2020-09-08 - Earliest claimed: 2018-12-17 - Assignees: Eisai R&D Management Co., Ltd. - Applicants: Eisai R&D Management Co., Ltd. - Inventors: Hiroshi Ishihara; Katsura Hata; Hiroki Muto; Geoff Hird - Web page: https://patentgrep.com/patent/US10765633B2 ## CPC - A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911}) - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 9/1277: Preparation processes; Proliposomes - A61K 31/7024: Esters of saccharides - A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) ## Abstract A formulation comprising liposomes, wherein the liposomes comprise, based on the liposome, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 0.5 to 3.0 mol % of a PEGylated phospholipid. ## Claims ### Claim 1 A formulation comprising liposomes, wherein the liposomes comprise, based on the liposome, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof, a PEGylated phospholipid and 0 to 10 mol % of a sterol, wherein the molar ratio range of the eritoran or a pharmaceutically acceptable salt thereof and the PEGylated phospholipid is 1:0.4 to 1:2.5. ### Claim 2 (depends on 1) The formulation according to claim 1, wherein the pharmaceutically acceptable salt is tetrasodium salt. ### Claim 3 (depends on 1) The formulation according to claim 1, wherein the liposomes comprise, based on the liposome, 1.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 1.0 to 2.5 mol % of a PEGylated phospholipid. ### Claim 4 (depends on 1) The formulation according to claim 1, wherein the PEGylated phospholipid is 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]. ### Claim 5 (depends on 4) The formulation according to claim 4, wherein the liposomes comprise, based on the liposome, 1.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 1.0 mol % of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]. ### Claim 6 (depends on 4) The formulation according to claim 4, wherein the liposomes comprise, based on the liposome, 1.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 2.5 mol % of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]. ### Claim 7 (depends on 4) The formulation according to claim 4, wherein the liposomes comprise, based on the liposome, 2.5 mol % of eritoran or a pharmaceutically acceptable salt thereof and 1.0 mol % of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]. ### Claim 8 (depends on 4) The formulation according to claim 4, wherein the liposomes comprise, based on the liposome, 2.5 mol % of eritoran or a pharmaceutically acceptable salt thereof and 2.5 mol % of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]. ### Claim 9 (depends on 1) The formulation according to claim 1, wherein the liposomes further comprise a phosphatidylcholine. ### Claim 10 (depends on 9) The formulation according to claim 9, wherein the phosphatidylcholine is distearoyl phosphatidyl choline. ### Claim 11 (depends on 1) The formulation according to claim 1, wherein the liposomes further comprise an antioxidant. ### Claim 12 (depends on 11) The formulation according to claim 11, wherein the antioxidant is butylated hydroxyanisole. ### Claim 13 (depends on 1) The formulation according to claim 1, wherein the sterol is cholesterol. ### Claim 14 (depends on 1) The formulation according to claim 1, wherein the liposomes do not comprise the sterol. ### Claim 15 (depends on 1) The formulation according to claim 1, wherein the liposomes have an average particle size between 100 to 120 nm, as measured by Dynamic Light Scattering (DLS). ### Claim 16 (depends on 1) The formulation according to claim 1, wherein the liposomes have a polydispersity index of 0.20 or less. ### Claim 17 A method for producing a formulation comprising liposomes, comprising: preparing a solution comprising, based on all components of the liposomes to be used, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof, a PEGylated phospholipid, 0 to 10 mol % of a sterol and a solvent, wherein the molar ratio range of the eritoran or a pharmaceutically acceptable salt thereof and the PEGylated phospholipid is 1:0.4 to 1:2.5; evaporating the solvent from the solution to form a thin film; dispersing the thin film in a buffer solution to form a liquid dispersion; and extruding the liquid dispersion through a filter to form the formulation. ### Claim 18 (depends on 17) The method according to claim 17, wherein the solution further comprises a phosphatidylcholine and an antioxidant. ### Claim 19 (depends on 17) The method according to claim 17, wherein the solvent is a combination of chloroform and methanol. ### Claim 20 (depends on 17) The method according to claim 17, wherein the dispersing step is performed by sonication. ### Claim 21 (depends on 17) The method according to claim 17, wherein the method further comprises adjusting the pH of the formulation formed in the extruding step to 6.2 to 6.8.