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Polymer drug carrier with redox response and AIE effect, drug-loaded micelle and preparation method thereof

A technology for polymers and drugs, applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of slow drug release, limited application, lack of intelligent release, etc., and achieve cycle time. The effect of improving and improving biosafety

Active Publication Date: 2019-06-21
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Conventional nano-drug carriers release drugs slowly in cancer cells and lack intelligent release, which limits the therapeutic effect of drugs
At the same time, traditional micellar drug carriers cannot track the distribution of drugs in vivo, and traditional fluorescent molecules limit their application in bioimaging due to the aggregation-induced quenching (ACQ) effect.

Method used

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  • Polymer drug carrier with redox response and AIE effect, drug-loaded micelle and preparation method thereof
  • Polymer drug carrier with redox response and AIE effect, drug-loaded micelle and preparation method thereof
  • Polymer drug carrier with redox response and AIE effect, drug-loaded micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] A polymer drug carrier with redox response and aggregation-induced luminescent effect, the preparation method of which comprises the following steps:

[0047] (1) Preparation of polyamino acid benzyl ester macromolecular initiator

[0048] Weigh 5g of L-glutamic acid-γ-benzyl ester-N-carboxylic acid anhydride monomer, dissolve it in 50mL of anhydrous N,N-dimethylformamide, then add 0.209g of N-(2-aminoethyl) -2-Bromoisobutyramide was used as an initiator, and under the protection of nitrogen, the reaction was stirred at room temperature for 72 hours. After the reaction was completed, the reaction product was concentrated by distillation under reduced pressure, and then precipitated in ether for 3 times, and finally dried in vacuum to obtain formula II. macromolecular initiator;

[0049]

[0050] Wherein, the degree of polymerization n of the polyamino acid block is 18;

[0051] (2) Preparation of two-block polymer precursors

[0052] Take the resultant of step (1)...

Embodiment 2

[0064] The method for preparing polymer drug-loaded micelles by using the polymer drug carrier with redox response and AIE effect prepared in Example 1 comprises the following steps:

[0065] Weigh 10 mg of the obtained product of Example 1, dissolve it in the mixed solution of N,N-dimethylformamide and methanol in a volume ratio of 1:1, then add 2 mg of doxorubicin hydrochloride and 50 μL of triethylamine, Stir at room temperature for 12 hours, slowly add it dropwise into rapidly stirred ultrapure water, stir for 6 hours, and then dialyze to remove the organic solvent to obtain polymer drug-loaded nanomicelles. The specific structural formula is shown in Formula I:

[0066]

[0067] Wherein, the R* group is doxorubicin.

[0068] Dynamic light scattering instrument (DLS) measures the particle size of blank polymer micelles and polymer drug-loaded nano micelles, and the results are shown in figure 2 , the transmission electron microscope (TEM) image is shown in image 3 ....

Embodiment 3

[0071] A polymer drug carrier with redox response and aggregation-induced luminescent effect, the preparation method of which comprises the following steps:

[0072] (1) Preparation of polyamino acid benzyl ester macromolecular initiator

[0073] Weigh 20mmol L-glutamic acid-γ-benzyl ester-N-carboxylic acid anhydride monomer, dissolve it in 70mL anhydrous N,N-dimethylformamide, then add 0.1mmol N-(2-aminoethyl) -2-Bromoisobutyramide was used as an initiator, and under the protection of nitrogen, the reaction was stirred at room temperature for 72 hours. After the reaction was completed, the reaction product was concentrated by distillation under reduced pressure, and then precipitated in ether for 3 times, and finally dried in vacuum to obtain formula II. macromolecular initiator;

[0074]

[0075] Wherein, the degree of polymerization of the polyamino acid benzyl ester block is 15;

[0076] (2) Preparation of two-block polymer precursors

[0077] Take 0.5 g of the resul...

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Abstract

The invention provides a polymer drug carrier with redox response and AIE effect, a drug-loaded micelle and a preparation method thereof. The polymer drug carrier includes a hydrophobic core and a hydrophilic shell, and the hydrophobic core is polyaspartic acid or Polyglutamic acid links tetraphenylethylene through disulfide bonds to link TPE blocks with polyamino acids, and the hydrophilic shell is polyphosphorylcholine blocks. The polymer drug carrier has a hydrophobic core of polyamino acid blocks grafted with tetraphenylethylene, and a hydrophilic shell of polyphosphorylcholine blocks. Its unique biomembrane structure provides excellent biological properties for nanocarriers. Compatibility, wrapping anti-cancer drugs in the hydrophobic core to prepare polymer drug-loaded micelles, which have redox response, and the AIE (aggregation-induced emission) imaging performance of tetraphenylethylene is realized Monitoring of drug traces in the body.

Description

technical field [0001] The invention belongs to the technical field of polymer drug carriers, and in particular relates to a polymer drug carrier with redox response and AIE (aggregation-induced emission) effect, drug-loaded micelles and a preparation method thereof. Background technique [0002] The delivery method of anticancer drugs used in conventional cancer treatment will cause great toxic and side effects to normal tissues of the human body. Therefore, research on safe and efficient anticancer drug carriers is of great significance for improving the therapeutic effect of drugs and reducing the toxic and side effects of drugs. Great significance. Nano-drug carriers with a certain size can be targeted and enriched in tumor tissue through the enhanced osmotic retention effect (EPR effect) in tumor tissue, which helps to reduce the side effects of anticancer drugs and improve the curative effect. [0003] Conventional nano-drug carriers release drugs slowly in cancer cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F230/02C08F8/32C08F8/00A61K9/107A61K31/704A61K47/34A61K49/00A61P35/00
CPCA61K9/1075A61K31/704A61K47/34A61K49/0013A61K49/0082A61P35/00C08F8/00C08F8/32C08F230/02C08F293/00
Inventor 王云兵胡军庄伟华胡艳飞
Owner SICHUAN UNIV
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