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A kind of amphiphilic block polymer and preparation method thereof

A technology of amphiphilic block and polymer, which is applied in the direction of pharmaceutical formulations, medical preparations of non-effective ingredients, emulsion delivery, etc. Soluble in supercritical carbon dioxide and other issues, to achieve the effect of complete morphology, good drug encapsulation rate, and no organic solvent residue

Active Publication Date: 2018-05-15
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But on the one hand, this method cannot completely remove the organic solvent in the micelles, which may cause additional side effects in the clinical use of the prepared drug-loaded micelles; on the other hand, this method will produce volatile organic compounds during the preparation process Pollution
In order to overcome this shortcoming, patent 200810235050.2 proposes a method for preparing amphiphilic block polymer drug-loaded micelles using water-supercritical carbon dioxide system induction method, but due to the existing amphiphilic block polymer (one end hydrophilic , hydrophobic at one end) are difficult to dissolve in supercritical carbon dioxide. Therefore, it is difficult for the existing amphiphilic block polymers to obtain a complete morphology, high drug loading, and drug encapsulation efficiency by using the water-supercritical carbon dioxide induction method. Good drug-loaded micelles, so the development of an amphiphilic block polymer with both a hydrophilic end and a supercritical carbon dioxide end is necessary

Method used

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  • A kind of amphiphilic block polymer and preparation method thereof
  • A kind of amphiphilic block polymer and preparation method thereof
  • A kind of amphiphilic block polymer and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Example 1: Preparation of an amphiphilic block polymer with one end hydrophilic and one end hydrophilic supercritical carbon dioxide:

[0026] Step 1, the preparation of vinyl acetate monomer polymerized segment:

[0027] Dissolve 25g of vinyl acetate, 2.3g of chain transfer agent O-ethyl xanthate ethyl propionate and 0.7g of azobisisobutyronitrile in 100ml of ethanol solution, stir and react at 50°C for 10 hours, after reaction, the ethanol solution is obtained Polymerized segments of vinyl acetate with double bonds at the end;

[0028] Step 2, preparation of amphiphilic block polymer:

[0029] Add 25 g of n-butyl methacrylate and 0.7 g of azobisisobutyronitrile to the ethanol solution containing vinyl acetate polymer segments in step 1, stir and react at 70° C. for 16 hours, and remove the organic solvent ethanol by rotary evaporation after the reaction. Obtain the crude product of the polymer with amphiphilic properties, dissolve the crude product of the polymer in...

Embodiment 2

[0030] Example 2: Preparation of an amphiphilic block polymer with one end hydrophilic and one end hydrophilic supercritical carbon dioxide:

[0031] Step 1, the preparation of vinyl acetate monomer polymerized segment:

[0032] Dissolve 12.5g of vinyl acetate, 0.6g of O-ethyl xanthate ethyl propionate and 0.2g of azobisisobutyronitrile in 100ml of acetonitrile solution, and stir and react at 70°C for 5 hours. After the reaction, a terminal band is obtained in the acetonitrile solution. Double-bonded vinyl acetate polymer segment;

[0033] Step 2, preparation of amphiphilic block polymer:

[0034] Add 37.5 g of hydroxyethyl methacrylate and 0.2 g of azobisisobutyronitrile to the acetonitrile solution containing vinyl acetate polymer segments in step 1, stir and react at 90 ° C for 10 hours, and remove the organic solvent acetonitrile by rotary evaporation to obtain Polymer crude product with amphiphilic properties, the crude product is dissolved in 50ml of dichloromethane, a...

Embodiment 3

[0035] Example 3: Preparation of an amphiphilic block polymer with one end hydrophilic and one end hydrophilic supercritical carbon dioxide:

[0036] Step 1, the preparation of vinyl acetate monomer polymerized segment:

[0037] Dissolve 37.5g vinyl acetate, 0.1g O-ethyl xanthate ethyl propionate and 0.05g azobisisobutyronitrile in 100ml 1,4-dioxane solution, stir and react at 90°C for 6 hours, and react The final 1,4-dioxane solution obtains a vinyl acetate polymer segment with a double bond at the end;

[0038] Step 2, preparation of amphiphilic block polymer:

[0039] Add 12.5g polyethylene glycol dimethacrylate (wherein, the number of polyethylene glycol monomer segments is 3) and 0.05g Azobisisobutyronitrile, stirred and reacted at 90°C for 12 hours, and the organic solvent 1,4-dioxane was removed by rotary evaporation to obtain a crude amphiphilic polymer product, which was dissolved in 50ml of dichloromethane , using a dialysis bag with a molecular weight of 1000 for...

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Abstract

The invention discloses an amphiphilic block copolymer, which is copolymerized by a hydrophilic alpha-methyl unsaturated olefinic bond monomer polymer chain segment and a vinyl acetate monomer polymer chain segment of hydrophilic supercritical carbon dioxide, so as to obtain the amphiphilic block copolymer with the number-average molecular weight of 3,000-50,000, wherein the alpha-methyl unsaturated olefinic bond monomer polymer chain segment accounts for 20%-80% of weight of the amphiphilic block copolymer; and the alpha-methyl unsaturated olefinic bond monomer is any one of a methyl methacrylate monomer, an ethyl methacrylate monomer, a methacrylic acid normal propyl acetate monomer, a methacrylic isopropyl ester monomer, an n-butyl methacrylate monomer, an isobutyl methacrylate monomer, a tert-butyl methacrylate monomer, a glycidyl methacrylate monomer, a hydroxyethyl methylacrylate monomer or polyethylene glycol dimethacrylate. The invention further discloses a preparation method of the amphiphilic block copolymer.

Description

technical field [0001] The present invention relates to a block polymer with amphiphilic performance, and also relates to a preparation method of the above-mentioned amphiphilic block polymer. Background technique [0002] The amphiphilic block polymer is composed of a hydrophilic segment and a hydrophobic segment, and the drug-loaded micelles formed by it have a "core-shell" structure. Among them, the hydrophobic core of the micelle can effectively wrap the hydrophobic drug, and the hydrophilic shell makes the micelle soluble in water, so that the micelle obtains the effect of solubilizing the hydrophobic drug. The use of amphiphilic block polymer micelles as the drug delivery carrier has the advantages of prolonging the half-life of the drug, controlling the particle size of the drug-loaded micelles, and enhancing the targeting of tumor cells while solubilizing the drug. One of the most promising approaches for hydrophobic antitumor drug delivery systems. [0003] Amphip...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00A61K9/107A61K47/34A61K47/32
CPCY02P20/54
Inventor 焦真樊文景王梓屹王秀东
Owner SOUTHEAST UNIV
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