Nano-drug for tumor radiotherapy and chemotherapy synergistic treatment and preparation method and application thereof

A technology of drugs and compounds, applied in the field of medicine, can solve the problems of damage to adjacent normal tissues, limited bioavailability, toxic and side effects, etc., and achieve the effect of strengthening the synergistic effect of radiotherapy and chemotherapy, reducing systemic toxicity, and mild conditions

Pending Publication Date: 2021-12-17
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some inherent disadvantages of RT also limit its long-term application, which mainly includes the following three aspects: 1) The ionizing radiation used to kill tumors may damage adjacent normal tissues, resulting in severe toxic side effects
2) The hypoxic nature of the tumor microenvironment (TME) may render tumor cells resistant to radiation, ultimately leading to the failure of tumor eradication
However, due to limited bioavailability, especially in hypoxic regions of tumor tissue, the efficacy of radiotherapy still needs to be improved

Method used

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  • Nano-drug for tumor radiotherapy and chemotherapy synergistic treatment and preparation method and application thereof
  • Nano-drug for tumor radiotherapy and chemotherapy synergistic treatment and preparation method and application thereof
  • Nano-drug for tumor radiotherapy and chemotherapy synergistic treatment and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Block copolymers of PEG 5k Preparation and characterization of -b-PMN

[0081] The reaction procedure is as follows:

[0082]

[0083] Wherein, x ranges from 10-40;

[0084] (1) Synthesis of monomers

[0085] Three-neck flask was placed in an oven at 120 deg.] C drying. Three-necked flask was added 2g of metronidazole in 50mL of methylene chloride and stirred and dissolved in an ice bath, was added 3.24mL of triethylamine. 5 ~ 10mL dichloromethane and was added 1.08mL 2- methacryloyl chloride in the pressure-equalizing dropping funnel, under an ice bath, was slowly dropped into the three-necked flask. After the dropwise addition, stirred for 1h. Extracted with distilled water, rotary evaporated to remove organic solvent to give a crude product. N-hexane as the mobile phase, the product was purified over a silica gel column. The final product was dried under vacuum to give saved. Di 6 The product was dissolved 10mg -DMSO, 1 H NMR analysis of measurement results are figure ...

Embodiment 2

[0094] Synthesis and Characterization of prodrug molecules (GM) of

[0095] The reaction procedure is as follows:

[0096]

[0097] Previously 50mL round bottom flask was placed in a drying oven at 120 deg.] C, the water addition to the net. Of tetrahydrofuran was added sodium metal, benzophenone indicator, in addition to water distillation 2h, the solution is the blue color of anhydrous tetrahydrofuran. Weigh 125.75mg (0.2mmol) gambogic acid (GA), 342.3mg (2mmol) metronidazole (MN), 76.68mg (0.4mmol) 1- ethyl - (3-dimethylaminopropyl) carbonyl carbodiimide (EDC), 48.84mg (0.4mmol) 4- dimethylaminopyridine (DMAP) was dissolved in 5mL dry tetrahydrofuran (THF), at room temperature for 24h.

[0098] After completion of the reaction, the resulting reaction solution was transferred to a separatory funnel, was added 10mL of deionized water and extracted three times with 10mL of ethyl acetate, organic phase was collected. Anhydrous sodium sulfate was added with stirring the crude prod...

Embodiment 3

[0100] Preparation and characterization of nanoparticles loaded prodrugs

[0101] PEG polymers were weighed 10mg 5k -b-PMN, 5mg gambogic acid prodrugs GM to 1.5mL centrifuge tube, then added 1mLN, N'- dimethylformamide (DMF) sufficiently dissolved. The syringe configured 2.5mL solution was aspirated from the centrifuge tube, using a syringe pump constant solution was poured into rapidly stirred 5mL ultrapure water in a state, a flow rate of 1.5mL / h. After stirring for 4 hours after injection, then the solution was dialyzed in dialysis bag was charged 3500KD ultrapure water, removing the organic solvent N, N'- dimethylformamide (DMF), ultra-pure water for once every 12h, 48h dialysis . After dialysis, a 0.45μm membrane filter, 4 ℃ refrigerator storage.

[0102] Micelle particle size measured by DLS. DLS test method: taking into polymeric micelles 1-1.5mL sample cuvette after selecting test items 2min preheated at a test temperature 25 ℃, then test, each sample was measured five t...

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Abstract

The invention relates to a nano-drug for tumor radioactive diagnosis and treatment and a preparation method and application thereof. The nano-drug is composed of a block copolymer shown as a general formula (I) and a prodrug, and the prodrug is preferably a gambogic acid derivative. The preparation method comprises the following steps of: preparing a macroinitiator and monomers required by polymerization, and initiating the monomers to carry out polymerization reaction by utilizing the macroinitiator to obtain a block copolymer; and connecting two drugs through esterification reaction to obtain a prodrug. After the copolymer is loaded with the prodrug, radiotherapy and chemotherapy combined treatment of tumors is realized. By preparing a polymer system with long circulation time and extremely low normal tissue uptake, the block copolymer can be effectively enriched in tumors. When the block copolymer is combined with the prodrug, effective release of drugs and radiotherapy sensitization are realized in a tumor hypoxic microenvironment, and tumor growth is effectively inhibited.

Description

Technical field [0001] The present invention relates to the field of medicine, particularly cancer chemotherapy, to a synergistic therapeutic nanoparticles and its preparation method and application, and more particularly relates to a method of modifying drug modified block copolymer, for drugs and gambogic acid and so its use. Background technique [0002] Cancer is a disease of mutant cells, immortalized cells with such mutations and evasion of apoptosis, eventually, tumor formation and invade surrounding tissues (also called metastasis). In today's society, despite massive financial and intellectual investment into the prevention and treatment of cancer, cancer remains a threat to human health of the world's disease. Therefore, finding better cancer treatments to complement and improve current cancer treatments is significant. [0003] Chemotherapy is the use of chemical drugs to prevent cancer cell proliferation, invasion, metastasis, is a systemic treatment. Existing on the ...

Claims

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Application Information

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IPC IPC(8): C08F293/00A61K31/352A61K31/4164A61K47/60A61K47/69A61P35/00
CPCC08F293/005A61K47/60A61K47/6929A61K31/352A61K31/4164A61P35/00C08F2438/01A61K2300/00Y02A50/30
Inventor 喻青松甘志华罗珂筠
Owner BEIJING UNIV OF CHEM TECH
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