Liposome composition and method for producing same

Patent metadata

Field	Value
Publication number	US-11684575-B2
Application number	US-202017121870-A
Country	US
Kind code	B2
Filing date	Dec 15, 2020
Priority date	Apr 30, 2014
Publication date	Jun 27, 2023
Grant date	Jun 27, 2023

Abstract

Provided are a liposome composition which has a practically required long-term preservation stability, and which has a release rate of a drug on the order of several tens of hours due to releasability of a drug being able to be suitably controlled by rendering an inner water phase hyper-osmotic; and a method for producing the same. According to the present invention, it is possible to provide a liposome composition, including liposomes each of which has an inner water phase and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed, in which the content of cholesterols is 10 mol % to 35 mol % with respect to the total amount of lipid components in the liposome composition, and each of the liposomes encapsulates a drug in a dissolved state, and an osmotic pressure of the inner water phase is 2-fold to 8-fold relative to the osmotic pressure of the outer water phase.

First claim

What is claimed is:

1. A liposome composition, comprising:
liposomes each of which has an inner water phase containing a drug and an aqueous solution which constitutes an outer water phase and in which the liposomes are dispersed,
wherein the lipids constituting the liposome include at least hydrogenated soybean phosphatidylcholine, 1,2-distearoyl-3-phosphatidylethanolamine-polyethylene glycol, and cholesterol,
the content of cholesterol is 17 mol % to 21 mol % with respect to the total amount of lipid components in the liposome composition,
the drug is an anticancer agent which is gemcitabine,
the drug is present in a dissolved state in the inner water phase of the liposome, and
an average particle size of the liposomes is 5 nm to 100 nm.

2. The liposome composition according to claim 1 , wherein a release rate of the drug from the liposome composition in blood plasma is 10 wt %/24 h or more relative to an initial encapsulation amount in the liposome composition.

3. The liposome composition according to claim 1 , wherein the content of 1,2-distearoyl-3-phosphatidylethanolamine-polyethylene glycol is 1 mass % to 20 mass % with respect to the total amount of lipid components in the liposome composition.

Assignees

• Fujifilm Corp

Inventors

• Ono Makoto
• Ono Kohei
• Matsumoto Takeshi
• Mori Mikinaga

Classifications

• B01J13/02

  Making microcapsules or microballoons {(for medical preparations A61K9/50)} · CPC title

• A61K47/28

  Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid · CPC title

• A61K9/127 Primary

  Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant · CPC title

• A61K9/1278

  Post-loading, e.g. by ion or pH gradient · CPC title

• B01J13/20

  After-treatment of capsule walls, e.g. hardening · CPC title