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Liposome including taxane compound

A compound, taxane technology, applied in the field of liposomes encapsulating taxane compounds, can solve problems such as poor water solubility

Active Publication Date: 2018-06-08
ENSUIKO SUGAR REFINING +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Taxane compounds such as paclitaxel or docetaxel have excellent anticancer activity; on the other hand, taxane compounds have disadvantages including poor water solubility

Method used

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  • Liposome including taxane compound
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  • Liposome including taxane compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0207] Liposomes Encapsulating PTX, gPTX, or DTX

[0208] Liposomes encapsulating PTX (paclitaxel), gPTX (7-glucosyloxyacetylpaclitaxel) or DTX (docetaxel) were prepared by thin film hydration method.

[0209] Weigh 9.6 mg hydrogenated soybean lecithin (HPSC), 3.2 mg cholesterol (Chol), 3.2 mg 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxyl (polyethylene glycol) -2000] (mPEG-DSPE) and taxane compound (PTX, gPTX or DTX) and add to the eggplant-shaped flask with the molar ratio of HSPC:Chol:mPEG-DSPE:taxane compound=6:4:0.5:X .

[0210] Specifically, weigh 0.9 mg, 1.8 mg or 3.5 mg (x=0.5 to 2) of PTX, 2.2 mg, 4.4 mg or 6.6 mg (x=1 to 3) of gPTX and 1.7 mg, 3.3 mg or 5.0 mg (x= 1 to 3) DTX and add to eggplant flask.

[0211] 4 mL of an organic solvent (chloroform:methanol=9:1) was added to the eggplant-shaped flask, and the mixed lipids were sufficiently dissolved. Then, the mixed lipids were vacuum-dried using a rotary evaporator to completely remove the organi...

preparation Embodiment 2

[0219] Liposomes Encapsulating Bafilomycin A1 (BafA1)

[0220]Liposomes encapsulating BafA1 were prepared by thin film hydration method. 9.6 mg HSPC, 3.2 mg Chol, 3.2 mg mPEG-DSPE and BafA1 were weighed and added to an eggplant-shaped flask at a molar ratio of HSPC:Chol:mPEG-DSPE=6:4:0.5:x.

[0221] 145 μg or 290 μg (x=0.1 or 0.2) of BafAl was weighed and added thereto.

[0222] 4 mL of an organic solvent (chloroform:methanol=9:1) was added to the eggplant-shaped flask, and the mixed lipids were sufficiently dissolved. Then, the mixed lipids were vacuum-dried using a rotary evaporator to completely remove the organic solvent and form a lipid film encapsulating BafA1.

[0223] The liposome formation process using the thus-produced BafA1-encapsulating lipid film and the evaluation of the properties of the liposome were performed in the same manner as in the preparation of the taxane compound-encapsulating liposome.

[0224] The concentration of BafA1 encapsulated in liposom...

Embodiment 2

[0231] Cytotoxicity Assessment

[0232] Cytotoxicity of liposomes encapsulating PTX, gPTX or DTX was evaluated by using the MTT assay. As test target cells, the cell line HT-29 cells derived from human colon cancer, the cell line SK-OV-3 cells derived from human ovarian cancer, and the cell line SK-BR-3 cells derived from human breast cancer were used. Cancer cells were seeded into 96-well plates at 5000 cells / well.

[0233] After 24 hours of incubation, different concentrations of drugs were added to each well. After 72 hours of drug exposure, MTT solution was added at a final concentration of 0.5 mg / mL, followed by incubation for 4 hours. Then, the resulting A dissolved in nail Solution in liquid (10% SDS + 0.02-adjusted HCl). Calculate the concentration that causes 50% cell death (IC 50 ).

[0234] The cytotoxicity of BafA1 and liposomes encapsulating BafA1 was evaluated by using the following MTT assay. As test target cells, the cell line HT-29 cells derived fr...

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Abstract

The present invention addresses the problem of providing a method for causing a poorly-water-soluble pharmacologically active substance to be included in a liposome with a high efficiency. Provided isa composition comprising a lipid having a phosphatidylcholine group, a cholesterol compound, a lipid having a phosphatidylethanolamine group, and a poorly-water-soluble pharmacologically active substance, wherein the lipid having a phosphatidylcholine group, the cholesterol compound, the lipid having a phosphatidylethanolamine group and the poorly-water-soluble pharmacologically active substanceare contained at a molar ratio of (3 to 8):(2 to 7):(0.1 to 3):(0.001 to 5).

Description

technical field [0001] The present invention relates to liposomes encapsulating taxane compounds. Background technique [0002] Taxane compounds such as paclitaxel or docetaxel have excellent anticancer activity; on the other hand, taxane compounds have disadvantages including poor water solubility. Thus, taxane compounds are administered to cancer patients by dissolving in ethanol containing a surfactant such as cremophor. [0003] However, a new issue of significant side effects of such surfactants on humans has recently drawn attention. In view of this problem, attempts have been made to develop liposomes encapsulating taxane compounds and the use of the liposomes as DDS formulations. [0004] In particular, as disclosed in PTL1, a method for encapsulating taxane compounds in liposomes by a remote loading method using the principle of solubility gradient is known. [0005] Another known method is the method disclosed in NPL1 using the passive loading method, which invo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/24A61K31/337A61K31/357A61K31/4545A61K31/7048A61K39/395A61K45/00A61K47/10A61K47/28A61K47/14A61K9/127A61P35/00
CPCA61K39/395A61K45/00A61K9/127A61K31/337A61K31/357A61K31/4545A61K31/7048A61K9/1278A61P35/00A61K47/10A61K47/24A61K47/28A61K47/34A61K2039/505
Inventor 滨田博喜妹尾昌治笠井智成重广司原浩司伊藤哲也藤原一郎
Owner ENSUIKO SUGAR REFINING
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