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Liposome composition and method for producing the same

a technology of liposomes and compositions, applied in the field of liposome compositions, can solve the problems of inability to obtain effective cytocidal properties, inability to obtain sufficient exposure time in tumors, and inability to obtain expected drug efficacy, etc., and achieve the excellent leakage rate of a nucleic acid analog anticancer agen

Inactive Publication Date: 2018-08-30
FUJIFILM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a method for producing a liposome composition with a high leakage rate of a nucleic acid analog anticancer agent. By controlling the content ratio of a specific lipid and the ratio of the nucleic acid analog anticancer agent to the lipid, the liposome has a leakage rate that is significantly improved compared to existing methods. This results in a more effective delivery of the nucleic acid analog anticancer agent to cancer cells, reducing the likelihood of side effects and improving efficacy. The liposome composition produced using this method has a high leakage rate of the nucleic acid analog anticancer agent and can be used for cancer treatment with reduced risk of side effects.

Problems solved by technology

Therefore, in a case where an exposure time is short, effective cytocidal properties cannot be obtained.
In a case where in vivo metabolism after administration of such a drug is fast, in many cases, sufficient exposure time in tumors cannot be obtained and an expected drug efficacy cannot be obtained.
However, there is a problem in that the quality of life (QOL) is greatly impaired, for example, a problem of restraint of a patient during instillation.
In addition, according to the remote loading method disclosed in Pharmaceutical Research, 2014, 31, 12583-2592, an effect of improving the encapsulation rate cannot be obtained for drugs such as gemcitabine.

Method used

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  • Liposome composition and method for producing the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0172]a) Preparation of Oil Phase

[0173]16.6 g, 2.0 g, and 4.3 g of hydrogenated soybean phosphatidylcholine, cholesterol, and an N-(carbonyl-methoxypolyethylene glycol 2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine sodium salt (hereinafter, also referred to as DSPE-PEG) were respectively taken so as to have a molar ratio of 76 / 19 / 5. Subsequently, 405 mL of an organic solvent (ethanol / ethyl acetate=3 / 1) was added thereto and lipids are dissolved at a heated temperature of 70° C. to obtain an oil phase.

[0174]b) Preparation of Aqueous Phase

[0175]A 4 mM phosphate buffer solution (pH of 7.61) was prepared and used as an aqueous phase.

[0176]c) Preparation of Drug Non-Contained Liposome

[0177]The aqueous phase was heated to 70° C. and the oil phase was added thereto so that the volume ratio of water phase / oil phase=8 / 3, and then, the aqueous phase and the oil phase were mixed using a rotary stirring emulsifier (M Technique Co., Ltd.) at a circumferential speed of 20 m / s at 13,000 rpm...

example 2

[0184]A gemcitabine-contained liposome composition was prepared in the same manner as in the drug loading solution in Example 1 except that the solution was cooled to 40° C. within 5 minutes. The content ratio of the lysophospholipid contained in a lipid forming a liposome with respect to the total amount of phospholipids other than the lysophospholipid contained in the lipid forming the liposome is 0.65 mol %.

example 3

[0194]a) Preparation of Oil Phase

[0195]16.6 g, 2.0 g, and 4.3 g of hydrogenated soybean phosphatidylcholine, cholesterol, and an N-(carbonyl-methoxypolyethylene glycol 2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine sodium salt (hereinafter, also referred to as DSPE-PEG) were respectively taken so as to have a molar ratio of 76 / 19 / 5. Subsequently, 406 mL of an organic solvent (ethanol / ethyl acetate=3 / 1) was added thereto and lipids are dissolved at a heated temperature of 70° C. to obtain an oil phase.

[0196]b) Preparation of Aqueous Phase

[0197]A 4 mM phosphate buffer solution was prepared and used as an aqueous phase.

[0198]c) Preparation of Drug Non-Contained Liposome

[0199]The aqueous phase was heated to 70° C. and the oil phase was added thereto so that the volume ratio of water phase / oil phase=8 / 3, and then, the aqueous phase and the oil phase were mixed using a rotary stirring emulsifier (M Technique Co., Ltd.) at a circumferential speed of 20 m / s at 13,000 rpm for 30 minut...

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Abstract

An object of the present invention is to provide a liposome composition containing a liposome having an excellent leakage rate of a nucleic acid analog anticancer agent, and a method for producing the same. According to the present invention, there are provided a liposome composition containing a liposome which (1) contains a nucleic acid analog anticancer agent and in which (2) a content ratio of a lysophospholipid contained in a lipid forming the liposome with respect to a total amount of phospholipids other than the lysophospholipid contained in the lipid forming the liposome is 0.01 mol % to 5 mol % and (3) a nucleic acid analog anticancer agent / lipid ratio is 2 mass % to 10 mass %, and a method for producing the same.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a Continuation of PCT International Application No. PCT / JP2016 / 082417 filed on Nov. 1, 2016, which claims priority under 35 U.S.C. § 119(a) to Japanese Patent Application No. 2015-215767 filed on Nov. 2, 2015. Each of the above application(s) is hereby expressly incorporated by reference, in its entirety, into the present application.BACKGROUND OF THE INVENTION1. Field of the Invention[0002]The present invention relates to a liposome composition containing a liposome containing a nucleic acid analog anticancer agent, and a method for producing the same.2. Description of the Related Art[0003]As an anticancer agent, there is a drug of which attack on cancer cells is not affected by exposure time and a drug of which attack on cancer cells is significantly affected by exposure time as the anticancer agent is classified through descending classification (Cancer and Chemotherapy, 1976, Vol. 3, 1103-1110).[0004]It is often st...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7068
CPCA61K9/127A61K31/7068A61K9/1271A61K9/1278A61P35/00
Inventor SEKIGUCHI, TAKAHIROMORI, MIKINAGANUMAJIRI, KENTAROKITAOKA, HIROYUKI
Owner FUJIFILM CORP
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