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Star-shaped amphiphilic redox response type polymer and preparation method and application thereof

An amphiphilic and responsive technology, which can be used in drug combinations, pharmaceutical formulations, and emulsion delivery. Compatibility and stability, low price, low steric hindrance

Inactive Publication Date: 2020-03-10
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the drug-loaded nanoparticles have no controlled release characteristics, and cannot control the release of drugs according to changes in the environment, and cannot meet the needs of the body.
Administration of drugs when the body does not need the drug will instead increase the burden on the body and have a negative impact, and in the second half of the sustained release, as the concentration of the drug decreases, the efficacy of the drug also decreases, which cannot meet the needs of the body. , there is an urgent need for a drug system that can control drug delivery according to the needs of the body environment

Method used

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  • Star-shaped amphiphilic redox response type polymer and preparation method and application thereof
  • Star-shaped amphiphilic redox response type polymer and preparation method and application thereof
  • Star-shaped amphiphilic redox response type polymer and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0065] A star-shaped amphiphilic redox-responsive polymer named PT-[P(LA X -co-GA Y )-SS-mPEG] 4 , and its molecular structure is shown in formula (I), wherein X is 39, Y is 13, and m is 32. PT-[P(LA 39 -co-GA 13 )-SS-32PEG] 4 The synthetic route of figure 1 shown.

[0066] PT-[P(LA 39 -co-GA 13 )-SS-32PEG] 4 A preparation method comprising the steps of:

[0067] S1. Take 0.055g (0.4mmol) of pentaerythritol PT, 4.320g (30mmol) of lactide DL-LA and 1.160g (10mmol) of glycolide GA in an anhydrous and oxygen-free bottle, and then add 40 μL of stannous octoate. The reaction system was frozen with liquid nitrogen, and the air was removed by circulating pump-filling with argon three times, and the reaction bottle was vacuum-sealed. The reaction flask was placed in an oil bath at 130° C., and the reaction was stirred for 15 h under vacuum. After the reaction, the crude product was dissolved with an appropriate amount of dichloromethane, then precipitated with excess petro...

Embodiment 2

[0075] A star-shaped amphiphilic redox-responsive polymer named PT-[P(LA X -co-GA Y )-SS-mPEG] 4 , whose molecular structure is shown in formula (I), wherein X is 15, Y is 5, and m is 15.

[0076] PT-[P(LA 15 -co-GA 5 )-SS-15PEG] 4 The preparation method is the same as in Example 1, the difference is that step S1 is 0.4mmol pentaerythritol, 4mmol glycolide and 12mmol lactide, and the yield is 70%; 0.90mmol 3'3-dithiodipropionic acid, 2.24mmol DCC and 0.224mmol DMAP, and 1.12mmol polyethylene glycol monomethyl ether was dissolved in 20mL anhydrous DMF, the yield was 52%; step S2 was 0.25mmol mPEG-SS-COOH, 0.8mmol DCC and 0.009mmol DMAP in the Water anaerobic bottle, then 0.05mmol PT-P(LA-co-GA) 4 Dissolved in 10 mL of anhydrous DMF, the yield was 49%.

Embodiment 3

[0078] A star-shaped amphiphilic redox-responsive polymer named PT-[P(LA X -co-GA Y )-SS-mPEG] 4 , whose molecular structure is shown in formula (I), wherein X is 45, Y is 15, and m is 67.

[0079] PT-[P(LA 45 -co-GA 15 )-SS-67PEG]4 The preparation method is the same as in Example 1, the difference is that step S1 is 0.4mmol pentaerythritol, 12mmol glycolide and 36mmol lactide, and the yield is 50%; 1.34mmol 3'3-dithiodipropionic acid, 2.24mmol DCC and 0.224mmol DMAP, and 1.12mmol polyethylene glycol monomethyl ether was dissolved in 20mL anhydrous DMF, and the yield was 51%; step S2 was 0.50mmol mPEG-SS-COOH, 0.8mmol DCC and 0.009mmol DMAP in In an anhydrous and oxygen-free bottle, then add 0.05mmol PT-P(LA-co-GA) 4 Dissolved in 10 mL of anhydrous DMF, the yield was 50%.

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Abstract

The invention relates to a star-shaped amphiphilic redox response type polymer and a preparation method and application thereof. The polymer has a molecular structure shown in the formula (I), whereinX is 15-45, Y is 5-15 and m is 15-67. The polymer disclosed by the invention takes pentaerythritol as a core, poly(lactic acid-co-glycolic acid) as a hydrophobic segment, methoxypolyethylene glycol as a hydrophilic segment and disulfide bonds on a main chain as oxidation-reduction response functional groups to be used for preparation of low-toxicity and stable star-shaped oxidation-reduction response type polymer micelles, and meanwhile the star-shaped oxidation-reduction response type polymer micelles have a good drug loading rate, a good encapsulation rate and good drug release performancesin a specific environment. Due to the fact that pentaerythritol is low in price and relatively small in steric hindrance, the reaction of each step is easier to carry out, good yield is achieved, andlarge-scale production can be achieved.

Description

technical field [0001] The present invention relates to the technical field of pharmaceutical polymer carriers, more specifically, to a star-shaped amphiphilic redox-responsive polymer and its preparation method and application. Background technique [0002] Amphiphilic polymer micelles are generally formed by self-assembly of amphiphilic polymers in aqueous solution, and the micelle inner shell composed of hydrophobic blocks can provide a place for hydrophobic drugs to improve the solubility of insoluble drugs; The micellar shell composed of water blocks can improve the solubility of the micelles in blood. Amphiphilic polymer micelles can improve the solubility of poorly soluble drugs in water, improve the utilization rate, and can also achieve sustained release and prolong the action time of drugs. [0003] Chinese patent CN107243002A discloses a kind of polytetracaprolactone-pentaerythritol administration nanoparticle and its preparation method, first makes polytetracapr...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/34A61P35/00
Inventor 郭建维邓建辉李盟冯静洁温伟球姜文钊
Owner GUANGDONG UNIV OF TECH
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