A polymer anti-tumor drug combined with angioblocker and immunomodulator and preparation method thereof

A vascular blocker, immunomodulator technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of unsatisfactory clinical chemotherapy effect, drug resistance, tumor recurrence, metastasis and spread, etc., to improve the efficacy and Effectiveness of drug utilization, improving therapeutic effect, reducing cytotoxicity

Active Publication Date: 2022-06-24
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problems that traditional chemotherapy is prone to drug resistance, chemotherapy drugs cannot penetrate into the tumor, and tumors are prone to recurrence, metastasis and spread, resulting in low actual utilization of drugs by the human body and unsatisfactory clinical chemotherapy effects, etc.

Method used

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  • A polymer anti-tumor drug combined with angioblocker and immunomodulator and preparation method thereof
  • A polymer anti-tumor drug combined with angioblocker and immunomodulator and preparation method thereof
  • A polymer anti-tumor drug combined with angioblocker and immunomodulator and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] 1. Preparation of polyethylene glycol monomethyl ether-b-polylactide:

[0068] Weigh 1.0 g (4.9 mmol) of norbornenyl lactide and 0.8 g (0.16 mmol) of polyethylene glycol monomethyl ether (molecular weight 5000) into a dry anaerobic ampoule that has been baked three times, and then place it under argon. Under gas protection, a catalytic amount of 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and 5.0 mL of purified dichloromethane were added, and the reaction was carried out at room temperature for 48 hours. After the end, use anhydrous ether to settle for three times repeatedly, stand for centrifugation and then vacuum dry to obtain polyethylene glycol monomethyl ether-b-polylactide. Its structural characterization is shown in the H NMR spectrum figure 1 , molecular weight distribution Figure 7(B), indicating that the polymer has been successfully synthesized.

[0069] 2. Preparation of polyethylene glycol monomethyl ether-b-polylactide containing carboxyl side groups: ...

Embodiment 2

[0080] Other experimental steps and experimental conditions are as in Example 1, except that the molar ratio of main chain norbornenyl lactide and polyethylene glycol monomethyl ether (molecular weight is 5000) is adjusted to 10:1; 20:1; 40:1, Polyethylene glycol monomethyl ether-b-polylactide block polymers with different molecular weights were prepared. The polyethylene glycol monomethyl ether-b-polylactide block polymer was then used for subsequent grafting of compretin and imiquimod, and a drug similar to that of Example 1 was also obtained.

Embodiment 3

[0082] Other steps and experimental conditions are as in Example 1, except that the addition ratio of compretin containing diphenylcyclooctyne functional group and imiquimod containing diphenylcyclooctyne functional group in the preparation process of polymer-bonded drug Adjusted to 7:1; 7:2, to prepare the polymer-bonded drugs with different graft ratios of the two drugs.

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Abstract

The invention discloses a macromolecular antitumor drug combined with a blood vessel blocking agent and an immunomodulator and a preparation method thereof; Chemical reactions such as -ene photoclick reaction, esterification reaction and azide-alkyne cycloaddition reaction are grafted on the main chain to bond blood vessel blocking agent and immunomodulator drug molecules at the same time. Through the synergistic effect of tumor vascular blocking therapy and immunotherapy, the polymer anti-tumor drug improves the anti-cancer activity while reducing the drug dose, and avoids the defects of traditional chemotherapy drugs that are difficult to penetrate into tumor cells and drug resistance. At the same time, immunotherapy is used to activate the patient's own immune system to kill tumor cells for a long time, effectively preventing clinical tumor metastasis and recurrence. In addition, the synthesis method of anti-tumor polymer-bonded drugs has the characteristics of simplicity, high efficiency, and mild reaction conditions.

Description

technical field [0001] The invention relates to a polymer anti-tumor drug, in particular to an anti-tumor polymer-bonded drug that binds a blood vessel blocker and an immune regulator simultaneously, and a preparation method thereof; it belongs to the field of biomedical polymer materials. Background technique [0002] As a global public health problem, tumor has greatly endangered human health, and has become the main cause of human death in the new century. At present, the main methods of cancer treatment include chemotherapy, surgery, radiation therapy, etc. Although traditional chemotherapy has progressed for a long time, there are still problems such as difficulty in penetration of anticancer drugs into the tumor and drug resistance caused by long-term use, which makes the treatment effect ineffective. However, both radiotherapy and surgery have defects such as large toxic side effects and easy to cause tumor cell spread and metastasis. Therefore, how to prevent tumor s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/59A61K47/60A61K45/06A61K31/09A61K31/4745A61P35/00
Inventor 张雪飞佘攀
Owner XIANGTAN UNIV
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