Preparation method of pH value-sensitive curcumin-loading micelle (single chain) precursor

A technology of drug-loaded micelles and curcumin, which is applied in the direction of pharmaceutical formulas, medical preparations of non-active ingredients, anti-tumor drugs, etc., can solve the problems of sudden release phenomenon and the lack of selectivity of tumor cells, and achieve improved Affinity, increased solubility, increased drug release effects

Inactive Publication Date: 2014-04-23
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, both micelles and liposomes have limitations. For example, they are thermodynamically unstable systems, prone to burst release in the human environment, and have no selectivity for normal cells and tumor cells.

Method used

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  • Preparation method of pH value-sensitive curcumin-loading micelle (single chain) precursor
  • Preparation method of pH value-sensitive curcumin-loading micelle (single chain) precursor
  • Preparation method of pH value-sensitive curcumin-loading micelle (single chain) precursor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0050] Example 1-1: Weigh 5g of polyethylene glycol monomethyl ether (MPEG) into a round bottom flask, melt at 80°C, then weigh 5g of lactide and add it to the flask, heat up to 100°C to melt, and wait until it is completely melted After that, the vacuum was repeatedly pumped three times, under nitrogen protection, the temperature was raised to 125° C., and 1 mL of stannous octoate was slowly added dropwise to the above solution and stirred for 24 hours. The product was dissolved in 50mL of THF, then rotary evaporated to 5-10mL, slowly dropped into glacial ether, a large amount of white powder precipitate was formed, and the white powder was obtained by suction filtration under reduced pressure. After repeated precipitation three times, the product was redissolved in THF, added In a dialysis bag with a molecular weight of 3500, distilled water was used as the medium for dialysis for 24 hours, the solution in the dialysis bag was centrifuged, and the supernatant was freeze-dried...

Embodiment 1-2

[0051] Example 1-2: Weigh 5g of polyethylene glycol monomethyl ether (MPEG) into a round bottom flask, melt at 80°C, then weigh 5g of lactide and add it to the flask, heat up to 100°C to melt, and wait until it is completely melted Afterwards, vacuuming was repeated three times, under nitrogen protection, the temperature was raised to 125° C., 0.8 mL of stannous octoate was slowly added dropwise to the above solution and stirred for 24 hours. The product was dissolved in 50mL of THF, then rotary evaporated to 5-10mL, slowly dropped into glacial ether, a large amount of white powder precipitate was formed, and the white powder was obtained by suction filtration under reduced pressure. After repeated precipitation three times, the product was redissolved in THF, added In a dialysis bag with a molecular weight of 3500, distilled water was used as the medium for dialysis for 24 hours, the solution in the dialysis bag was centrifuged, and the supernatant was freeze-dried.

Embodiment 1-3

[0052] Example 1-3: Weigh 5g of polyethylene glycol monomethyl ether (MPEG) into a round bottom flask, melt at 80°C, then weigh 5g of lactide and add it to the flask, heat up to 100°C to melt, and wait until it is completely melted Afterwards, the vacuum was repeated three times, under nitrogen protection, the temperature was raised to 125°C, and 1.2 mL of stannous octoate was slowly added dropwise to the above solution and stirred for 24 hours. The product was dissolved in 50mL of THF, then rotary evaporated to 5-10mL, slowly dropped into glacial ether, a large amount of white powder precipitate was formed, and the white powder was obtained by suction filtration under reduced pressure. After repeated precipitation three times, the product was redissolved in THF, added In a dialysis bag with a molecular weight of 3500, distilled water was used as the medium for dialysis for 24 hours, the solution in the dialysis bag was centrifuged, and the supernatant was freeze-dried.

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Abstract

The invention relates to a preparation method of a pH value-sensitive curcumin-loading micelle (single chain) precursor. The chemical formula of the pH avid-sensitive curcumin micelle (single chain) precursor is MPEG-PLA-N=Cur. The preparation method comprises the following steps: dissolving modified methoxy poly(ethylene glycol)-poly(lactic acid) of which the terminal contains hydrazino and single-terminal phenolic hydroxyl carbonylated curcumin serving as reaction raw materials in a proper feeding ratio under the action of a certain solvent; carrying out a bonding reaction to form a pH avid-sensitive curcumin micelle monomer. Compared with the prior art, the preparation method has the advantages that a hydrazone bond is introduced into the conventional diblock copolymer (MPEG-PLA) structure and is bonded with curcumin which is a hydrophobic medicament, and a formed amphiphilic polymer is self-assembled into a micelle in an aqueous solution.

Description

Technical field: [0001] The invention relates to the preparation of a drug-loaded micelle (single chain) and a precursor thereof, and further relates to a preparation method of a pH-sensitive drug-loaded curcumin micelle (single chain) and a precursor. Background technique: [0002] Curcumin is a hydrophobic polyphenolic compound extracted from the rhizome of the herb turmeric. It has been proven to have a wide range of pharmacological activities such as anti-inflammatory, anti-oxidation, hypolipidemic, and anti-tumor. At the same time, clinical studies have found that high doses Oral administration of curcumin at 8 g / day has no toxic side effects, so its effectiveness and safety make curcumin a potential drug for the treatment and prevention of various diseases. Especially in the research of anti-tumor, because tumor has become a common disease that seriously threatens and endangers human life, and in the process of tumor treatment, it usually faces various problems such as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/19A61K31/12A61P35/00
Inventor 赵燕军王征张琪曹延武陈超高敏
Owner TIANJIN UNIV
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