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a maa -co- daa -co- pegma copolymer and its preparation method and application

A technology of maa-co-daa-co-pegma and copolymer, applied in the field of MAA-co-DAA-co-PEGMA copolymer and its preparation, can solve the problem of low drug loading, no targeting ability and slow drug release and other problems, to achieve the effects of high degradability, high drug loading, and wide application prospects

Active Publication Date: 2022-07-29
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] For a long time, BTZ nanomedicines have disadvantages such as low drug loading, easy leakage of drugs in physiological environment, slow release of drugs in tumor cells, and no targeting ability.

Method used

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  • a maa <i>-co-</i> daa <i>-co-</i> pegma copolymer and its preparation method and application
  • a maa <i>-co-</i> daa <i>-co-</i> pegma copolymer and its preparation method and application
  • a maa <i>-co-</i> daa <i>-co-</i> pegma copolymer and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A MAA-co-DAA-co-PEGMA copolymer, the preparation process is as follows:

[0028] .

[0029] The preparation steps are:

[0030] (1) Dissolve 0.27 g TBDMS-DAA in 2 mL DMF to obtain a TBDMS-DAA solution; dissolve 0.085 g BACy in 1 mL DMF to obtain a BACy solution; dissolve 2 mmol TBAF in 10 mL THF to obtain 0.2 mol / LTBAF solution;

[0031] (2) Under nitrogen atmosphere, add 0.492 g MAA, 0.198 g PEGMA (average molecular weight 300), 0.0692 g SDS, and the TBDMS-DAA solution and BACy solution obtained in step (1) into 36 mL of water, mix, and heat to 80 °C with stirring , added 0.001 g APS, reacted for 8 h, washed by centrifugation, and freeze-dried at -40 °C;

[0032] (3) The product obtained in step (2) was added to 10 mL of TBAF solution, stirred, centrifuged to collect the precipitate, washed with THF, washed with water, and freeze-dried at -45 °C to obtain MAA-co-DAA-co-PEGMA copolymer.

[0033] figure 1 TEM image of MAA-co-DAA-co-PEGMA copolymer. Depend on fi...

Embodiment 2

[0038] The difference with Example 1 is: in step (2), the consumption of TBDMS-DAA is kept unchanged, and the consumption of MAA is adjusted according to the MAA:TBDMS-DAA molar equivalent ratio of 32:2, and the others are the same as in Example 1.

Embodiment 3

[0040] The difference with Example 1 is: in step (2), the consumption of TBDMS-DAA is kept constant, the MAA:TBDMS-DAA molar equivalent ratio is 8:2 to adjust the consumption of MAA, and the others are the same as in Example 1.

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Abstract

The invention belongs to the technical field of drug carriers and discloses an MAA ‑co‑ DAA ‑co‑ PEGMA copolymer and its preparation method and application. The structural formula is as follows: . Preparation method: respectively dissolve TBDMS-DAA and BACy in DMF to obtain TBDMS-DAA solution and BACy solution; dissolve TBAF in THF to obtain TBAF solution; under nitrogen atmosphere, mix MAA, TBDMS-DAA solution, PEGMA, BACy solution and SDS were added to water, mixed, heated to 40-100 °C with stirring, APS was added, reacted for 5-10 h, centrifuged, washed, and freeze-dried; the dried product was added to TBAF solution, stirred, and centrifuged to collect the precipitate. THF washing, water washing and freeze drying to obtain MAA ‑co‑ DAA ‑co‑ PEGMA copolymer. MAA of the present invention ‑co‑ DAA ‑co‑ As a drug carrier, PEGMA copolymer has a high drug loading and can solve the hydrophobicity problem of the drug itself.

Description

technical field [0001] The invention belongs to the technical field of drug carriers, and in particular relates to a MAA-co-DAA-co-PEGMA copolymer and a preparation method and application thereof. Background technique [0002] Cancer has always been an important disease threatening human life. A study reported by CNN showed that the number of cancer patients in the world is still increasing. In 2018 alone, there were nearly 18.1 million cancer diagnoses, of which 9.92 million people will die from cancer, more than half of the cancer mortality rate. According to a report released by the World Health Organization's International Agency for Research on Cancer on September 12, by the end of this century, cancer will become the world's number one killer and the biggest obstacle to increasing life expectancy. For better cancer treatment, this is not only based on the high efficiency of anticancer drugs, but also requires the synergy of antitumor drug delivery systems and the high...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F283/06C08F220/06C08F222/38C08F220/58A61K47/34
CPCC08F283/065A61K47/34C08F220/06C08F222/385C08F220/58
Inventor 赵旭波邱雨点刘仲毅
Owner ZHENGZHOU UNIV
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