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Methotrexate (MTX)-Pluronic copolymer mixed micelle carrying indissoluble medicament and preparation method thereof

A technology of insoluble drugs and mixed micelles, which is applied in the field of biomedicine to achieve the effect of increasing drug loading

Inactive Publication Date: 2013-04-03
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug resistance of tumor cells to MTX has become an important factor limiting its clinical application.

Method used

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  • Methotrexate (MTX)-Pluronic copolymer mixed micelle carrying indissoluble medicament and preparation method thereof
  • Methotrexate (MTX)-Pluronic copolymer mixed micelle carrying indissoluble medicament and preparation method thereof
  • Methotrexate (MTX)-Pluronic copolymer mixed micelle carrying indissoluble medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The mass ratio of PTX to P123:F127:F127-MTX=20:9:1 was placed in a 50mL round-bottomed flask, and 5mL of acetonitrile was added to fully dissolve it. Rotary evaporation was performed at 50°C for 40min, and the organic solvent was evaporated to dryness. , vacuum-dried overnight at room temperature, added 5 mL of deionized water, stirred at a constant speed of 700 rpm in a 70°C water bath for 30 min, cooled to room temperature, and filtered through a 0.22 μm cellulose acetate membrane to obtain the MTX-modified Pluronic mixed micelles solution. Store after lyophilization. The measured particle size was 43.4±3.1 nm.

Embodiment 2

[0039] The mass ratio of Docetaxel to P105:F127:F127-MTX=100:9:1 was placed in a 50mL round-bottomed flask, and 5mL of methanol was added to fully dissolve it. Rotary evaporation was performed at 50°C for 40min, and the organic solvent was evaporated to dryness. , vacuum-dried overnight at room temperature, added 5 mL of deionized water, stirred at a constant speed at 700 rpm in a 60°C water bath for 30 min, cooled to room temperature, and filtered through a 0.22 μm cellulose acetate membrane to obtain the MTX-modified Pluronic mixed micelles solution. Store after lyophilization. The measured particle size was 73.1±1.1 nm.

Embodiment 3

[0041] The mass ratio of PTX to P105:F88:P123-MTX=1:100:4 was placed in a 100mL round-bottomed flask, and 5mL of acetonitrile was added to fully dissolve it, and the organic solvent was evaporated to dryness at 50°C by rotary evaporation for 40min. , vacuum-dried overnight at room temperature, added 50 mL of deionized water, stirred at a constant speed of 700 rpm in a 40°C water bath for 30 min, cooled to room temperature, and filtered through a 0.22 μm cellulose acetate membrane to obtain the MTX-modified Pluronic mixed micelles solution. Store after lyophilization. The measured particle size was 84.2±5.5 nm.

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Abstract

The invention belongs to the technical field of biological medicine and relates to a novel methotrexate (MTX)-Pluronic copolymer mixed micelle carrying an indissoluble medicament and a preparation method thereof. The method comprises the following steps of: performing chemical connection and copolymerization on Pluronic and MTX to obtain an MTX-Pluronic copolymer; and mixing the MTX-Pluronic copolymer with Pluronic-kind matters to prepare an MTX-Pluronic copolymer mixed micelle system, wherein a hydrophobic core of the mixed micelle carries the indissoluble medicament. Tests prove that the mixed micelle can improve the medicament-loading capacity of the indissoluble medicament, effectively reverses the medicament tolerance of tumors and has the medicament-delivery characteristic targeting folate receptors.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a novel methotrexate (MTX)-modified Pluronic copolymer mixed micelle loaded with insoluble drugs and a preparation method thereof. Background technique [0002] With the advent of chemotherapy drugs and their preparations, chemotherapy has become an important means of treatment of malignant tumors. According to reports, due to the poor water solubility of most antineoplastic drugs, large adverse reactions and poor selectivity, the clinical use of antineoplastic drugs is seriously restricted. Studies have shown that the failure of chemotherapy for malignant tumors such as breast cancer, ovarian cancer, lung cancer, liver cancer, nasopharyngeal cancer, esophageal cancer, gastric cancer and leukemia is not uncommon in clinical practice. drug resistance (MDR). MDR has become a major problem in the treatment of cancer today. According to estimates from the American C...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/34A61K31/337A61K31/704A61P35/00A61K47/22A61K47/10
Inventor 沙先谊陈彦佐方晓玲
Owner FUDAN UNIV
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