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Curcumin-containing polymeric micelle drug delivery system and preparation method and application thereof

A drug-carrying system, curcumin technology, applied in antitumor drugs, drug combinations, ketone active ingredients, etc., can solve problems such as failure, drug concentration is difficult to achieve effective therapeutic dose, etc., to improve targeting, good biological Compatibility and biodegradability, effects of strong interactions

Inactive Publication Date: 2016-03-16
江苏万高药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, foreign literature has reported that curcumin has a potential therapeutic effect on Alzheimer's (senile dementia), but due to the blood-brain barrier, it is difficult for the drug concentration in the brain to reach an effective therapeutic dose. Clinical trials of curcumin to treat Alzheimer's all end in failure

Method used

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  • Curcumin-containing polymeric micelle drug delivery system and preparation method and application thereof
  • Curcumin-containing polymeric micelle drug delivery system and preparation method and application thereof
  • Curcumin-containing polymeric micelle drug delivery system and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Preparation of Methoxy Polyethylene Glycol-Polylactide Block Copolymer

[0062] 1) mPEG 2000 -PLA 1300 Synthesis

[0063] 10g of methoxy polyethylene glycol 2000 was added to the polymerization bottle, heated to 130°C and stirred and vacuumed for 1h, after cooling to room temperature, 11g of D, L-lactide and 5.5mg of stannous octoate were added. The reactants were polymerized at 130°C for 15 hours, and the product was dissolved in dichloromethane, precipitated with ice ether and filtered to obtain the white solid as mPEG. 2000 -PLA 1300 For block copolymers, the molecular weight of the polymer calculated by NMR is 3300, and the molecular weight and molecular weight distribution coefficient of the polymer determined by Gel Permeation Chromatography (GPC) are 4596 and 1.06, respectively. (Such as figure 1 and figure 1 Related data table 1).

[0064] Table 1 Generalized relative peak

[0065]

[0066] 2) Capping reaction

[0067] 11.7g of 6-Fluorenylmethoxycarbonylamino-2-tert-but...

Embodiment 2

[0070] 1) mPEG 2000 -PLA 1000 Synthesis

[0071] 10g of methoxy polyethylene glycol 2000 was added to the polymerization bottle, heated to 130°C, stirred and vacuumed for 1h, after cooling to room temperature, 7g of D, L-lactide and 3mg of stannous octoate were added, and the polymerization bottle was sealed in a vacuum. After polymerizing at 130℃ for 15h, the product was dissolved in dichloromethane, precipitated with ice ether and filtered to obtain the white solid as mPEG 2000 -PLA 1000 For block copolymer, the molecular weight of the polymer calculated by NMR is 3000, and the molecular weight and molecular weight distribution coefficient of the polymer determined by GPC are 3943 and 1.05 respectively.

[0072] 2) Capping reaction

[0073] 11.7g 6-Fluorenylmethoxycarbonylamino-2-tert-butoxycarbonylaminocaproic acid was dissolved in 50mL of anhydrous tetrahydrofuran and then 3-10mL of triethylamine was added. After cooling to -10℃, 2-5mL of pivaloyl chloride was added, and it immed...

Embodiment 3

[0076] 1) mPEG 2000 -PLA 1500 Synthesis

[0077] 10g of methoxy polyethylene glycol 2000 was added to the polymerization flask, heated to 130°C, stirred and vacuumed for 1h, after cooling to room temperature, added 13g of D, L-lactide, 6mg of stannous octoate, and sealed the polymerization flask in a vacuum. After polymerizing at 130℃ for 15h, the product was dissolved in dichloromethane, precipitated with ice ether and filtered to obtain the white solid as mPEG 2000 -PLA 1300 For block copolymers, the molecular weight of the polymer calculated by NMR is 3500, and the molecular weight and molecular weight distribution coefficient of the polymer determined by GPC are 4746 and 1.06 respectively.

[0078] 2) Capping reaction

[0079] 11.7g of 6-Fluorenylmethoxycarbonylamino-2-tert-butoxycarbonylaminocaproic acid was dissolved in 50mL of anhydrous tetrahydrofuran and then 3.5mL of triethylamine was added. After cooling to -10°C, pivaloyl chloride (3.05mL) was added. White precipitate imm...

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Abstract

The invention provides a curcumin micelle drug delivery system, a preparation method thereof and application of the curcumin micelle drug delivery system in treating tumor diseases. The drug delivery system is prepared from, by mass, 80-99.9% of amphiphilic segmented copolymer and 0.1-20% of curcumin. The amphiphilic segmented copolymer comprises a hydrophilic chain segment and a hydrophobic chain segment, wherein polyethylene glycol with the molecular weight of 100-6000 or methoxy polyethylene glycol with the molecular weight of 300-6000 serves as the hydrophilic chain segment, polylactide with the molecular weight of 200-6000 serves as the hydrophobic chain segment, the hydrophobic chain segment is subjected to end capping through groups containing fmoc and / or amino acid containing benzene ring structures, and the weight ratio of polyethylene glycol or methoxy polyethylene glycol to polylactide is (0.1-30):1. The invention further provides application of the drug delivery system in preparing tumor treating drugs.

Description

Technical field [0001] The invention provides a curcumin micellar drug-carrying system and a preparation method thereof, and its application in treating tumor diseases, belonging to the field of medicine. Background technique [0002] Curcumin (curcumin) is a polyphenol compound in the traditional Chinese medicine turmeric (Curcumalonga L.). Research in recent years has shown that curcumin has a strong preventive effect on the three stages of tumor carcinogenesis, and is a natural tumor chemopreventive and therapeutic agent with multi-target characteristics. Curcumin achieves anti-tumor effects by regulating genes related to tumor proliferation, apoptosis, infiltration and angiogenesis. [0003] Polymer micelles are a stable colloidal dispersion system developed in recent years. Micelles are usually formed by self-assembly of amphiphilic block polymers, with hydrophobic segments facing inward and hydrophilic chains outward, presenting a typical "core-shell" structure. Polymer mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/12A61K47/34C08G63/91C08G63/664A61P35/00
Inventor 姚俊华
Owner 江苏万高药业股份有限公司
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