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Method for preparing curcumin micelle with high medicine loading

A high drug loading, curcumin technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, antitumor drugs, etc., can solve the problems of low bioavailability and low drug loading in drug delivery systems, and achieve Improved particle size and stability, achieved synergistic therapeutic effect, and improved the effect of burst release

Inactive Publication Date: 2012-07-25
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the drug loading capacity of the drug delivery system is low and the bioavailability is not high
Moreover, the biocompatibility of these inert polymer materials and their metabolites, and the metabolism after administration are the limitations of this type of drug delivery system.

Method used

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  • Method for preparing curcumin micelle with high medicine loading
  • Method for preparing curcumin micelle with high medicine loading
  • Method for preparing curcumin micelle with high medicine loading

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: 5.0 g of MPEG2000 was used as an initiator, 5.0 g of lactide (DL), and stannous octoate with 0.2% of lactide were melt-polymerized at 125° C., and the reaction time was 24 hours. The reaction vessel was repeatedly evacuated 3 times, and nitrogen was protected during the reaction. After the reaction, the product was dissolved with an appropriate amount of tetrahydrofuran, precipitated in glacial ether, and the white precipitate was vacuum-dried for 24 hours.

Embodiment 2

[0047] Example 2: MPEG2000 5.0g was used as an initiator, lactide (DL) 4.0g, lactide 0.2% stannous octoate catalyzed melt polymerization at 125°C, and the reaction time was 24h. The reaction vessel was repeatedly evacuated 3 times, and nitrogen was protected during the reaction. After the reaction, the product was dissolved with an appropriate amount of tetrahydrofuran, precipitated in glacial ether, and the white precipitate was vacuum-dried for 24 hours.

Embodiment 3

[0048] Example 3: MPEG2000 5.0g was used as an initiator, lactide (DL) 2.5g, lactide 0.2% stannous octoate catalyzed melt polymerization at 125°C, and the reaction time was 24h. The reaction vessel was repeatedly evacuated 3 times, and nitrogen was protected during the reaction. After the reaction, the product was dissolved with an appropriate amount of tetrahydrofuran, precipitated in glacial ether, and the white precipitate was vacuum-dried for 24 hours.

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Abstract

The invention relates to medicine preparation which is characterized by having a special physical shape, and further relates to a pro-medicine of curcumin micelle with high medicine loading and a preparation method of the pro-medicine. The preparation method comprises the following steps of: bonding the curcumin modified by flutaric anhydride and MPEG-PLA (Methoxy poly(ethylene glycol)-poly(lactic acid)) with polyhydroxy distal end in an ester bond manner to form a curcumin micelle monomer with high grafting percent; and preparing medicine-loading micelle of the curcumin through a dialysis method. The pro-medicine of the curcumin micelle with the high medicine loading, obtained by the method disclosed by the invention breaks through a medicine administration mode of a traditional carrier-coating medicine so that a medicine is a part of a carrier; in addition, by controlling the usage of inert carrier materials, the medicine loading, the grain diameter and the stability of a micelle system are remarkably modified, and an EPR (Electron Paramagnetic Resonance) effect is reinforced.

Description

technical field [0001] The invention relates to a pharmaceutical preparation characterized by a special physical shape, and further relates to a high drug-loading curcumin micelle prodrug and a preparation method thereof. Background technique [0002] At present, malignant tumors have become a common disease that endangers human health, and the mortality rate of advanced cancer is increasing year by year. The mechanism of tumorigenesis is very complex, and most tumors are caused by abnormalities of more than 500 genes. Therefore, the effect and application of single-target anticancer drugs are greatly limited, and new multi-target anticancer drugs have become a new trend for the prevention and treatment of cancer. Curcumin (curcumin) is a phenolic compound extracted from turmeric, a plant of the ginger family, and is considered to be the main active ingredient of the traditional Chinese medicine turmeric. It has significant anti-inflammatory, anti-oxidation, hypolipidemic,...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/48C08G63/91C08G63/664A61P35/00
Inventor 王征杨汝磊高续丽朱俊东宋立超
Owner TIANJIN UNIV
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