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Application of polymer in cis-platinum detoxification

A technology of polymer and cisplatin, which is applied in the field of medicine, can solve the problems of reducing the effect of cisplatin chemotherapy, and achieve the effects of reducing damage, improving clearance efficiency, and improving selectivity

Pending Publication Date: 2022-06-21
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Detoxification of cisplatin with small-molecule antidotes leads to reduced chemotherapeutic efficacy of cisplatin

Method used

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  • Application of polymer in cis-platinum detoxification
  • Application of polymer in cis-platinum detoxification
  • Application of polymer in cis-platinum detoxification

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0111] The preparation method provided by the present invention can improve the product yield and purity through the control of reaction steps and reaction time, and the optimization of purification steps.

[0112] In the prior art, the above-mentioned polymers are usually used as drug carriers, however, in the present application, the polymer of formula (1) is used to prepare a nano antidote, and a new use of the substance is developed. The polymer of formula (1) provided by the present invention can be used as a nano antidote, can be circulated and enriched in the body and has responsive characteristics in the face of different physiological environments, improve the clearance efficiency of cisplatin in normal tissues, and can utilize tumor tissue and The different microenvironments of normal tissues can further improve the selectivity of the polymer nano-antidote of formula (1) combined with cisplatin, reduce the damage to the liver and kidney during cisplatin chemotherapy, ...

Embodiment 1

[0115] Example 1: Preparation of the polymer of formula (1)

[0116] 1. Synthesis of cystine-N-cyclic carboxylic acid anhydride (L-Cystine NCA) represented by formula (2):

[0117] The synthetic route is as follows:

[0118]

[0119] The synthesis process is as follows:

[0120] Select a three-necked flask of suitable size for water removal operation, and fill with nitrogen after the end to ensure anhydrous and anoxic conditions. Weigh 20 g of cystine (L-Cystine) and add it to vacuum for 30 min, add 200 mL of reaction solvent anhydrous tetrahydrofuran (THF), and stir in an oil bath at 54°C under nitrogen protection. A total of 24 g of triphosgene was added three times under protective conditions, and the reaction was carried out for 5 h under the flow of nitrogen. Wherein, the mass ratio of cystine:triphosgene can be in the range of 20:22. After the reaction was completed, the reaction solution was evaporated to 50 mL with a large nitrogen gas, slowly settled in 400 mL ...

Embodiment 2

[0127] Example 2: Characterization and Testing

[0128] 1. Structural characterization

[0129] After dissolving the three products obtained in Example 1 with deuterated trifluoroacetic acid (d-TFA) respectively, carry out a hydrogen nuclear magnetic resonance spectrum ( 1 H NMR), the results are shown in figure 1 , figure 1 For the product mPEG-PCys obtained in Example 1 2 3 , mPEG-PCys 2 5 , mPEG-PCys 2 10 The H NMR spectrum of , the resonance at 4.46 ppm is the characteristic signal of protons in the polypeptide backbone.

[0130] 2. Particle size analysis

[0131] The three products obtained in Example 1 were prepared as 0.1 mg / mL solutions in water, respectively, and the particle sizes of nanoparticles were characterized by dynamic light scattering (DLS) and scanning electron microscopy (TEM). The result is as Figures 2 to 4 shown, where, figure 2 For the product mPEG-PCys obtained in Example 1 2 5 The particle size analysis diagram of , image 3 For the ...

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Abstract

The invention provides an application of a polymer in cis-platinum detoxification. The polymer as shown in the formula (1) provided by the invention is used as a nano antidote, can circulate and enrich in vivo and has responsiveness to different physiological environments, the removal efficiency of cis-platinum in normal tissues is improved, and different microenvironments of tumor tissues and the normal tissues are utilized to improve the removal efficiency of cis-platinum in the normal tissues. The selectivity of the polymer nano antidote in the formula (1) combined with cis-platinum can be further improved, and the damage to the liver and the kidney in the cis-platinum chemotherapy process is reduced, so that the aim of improving the chemotherapy tolerance of tumor patients on the premise of ensuring the treatment effect is achieved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of a polymer in cisplatin detoxification. Background technique [0002] Cisplatin is a broad-spectrum and highly effective chemotherapeutic drug, which is widely used in clinical combination chemotherapy for malignant tumors. However, the use of cisplatin for chemotherapy often brings physical and psychological pain to patients. This is mainly due to the huge hepatotoxicity, nephrotoxicity, neurotoxicity, and ototoxicity of cisplatin, as well as severe gastrointestinal reactions. These side effects delay the continuation of chemotherapy, allowing patients to have longer treatment cycles. [0003] The traditional method to reduce the toxicity of cisplatin is to hydrate cisplatin, which can shorten the half-life of cisplatin in plasma concentration and increase the renal clearance of cisplatin. On this basis, the use of diuretics to increase the patient's urinary excretio...

Claims

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Application Information

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IPC IPC(8): A61K31/795A61K33/243A61P39/02A61P35/00C08G65/334B82Y5/00
CPCA61K31/795A61K33/243A61P39/02A61P35/00C08G65/3348B82Y5/00Y02A50/30
Inventor 丁建勋杨佳臻陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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