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Preparation method of double-response nano prodrug for cancer synergistic treatment

A double-response, nano-technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., to achieve good application prospects, inhibit DNA transcription, and simple methods

Active Publication Date: 2020-03-24
FUZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these methods only use cisplatin to achieve anti-cancer purposes, which will inevitably increase the dosage of cisplatin

Method used

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  • Preparation method of double-response nano prodrug for cancer synergistic treatment
  • Preparation method of double-response nano prodrug for cancer synergistic treatment
  • Preparation method of double-response nano prodrug for cancer synergistic treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0025] (1) Ultrasonic dispersion of 100 mg cisplatin (CDDP) in 5 mL of 30% H 2 o 2 In an aqueous solution, react at 50°C for 1 h, then stand still for 24 h, then centrifuge and dry in vacuum to obtain a hydroxylated cisplatin compound (CDDP-OH);

[0026] (2) Dissolve 100 mg of the obtained hydroxylated cisplatin compound and 70 mg of succinic anhydride in 10 mL of N,N-dimethylformamide, react at 75°C for 24 h, and then rotate the mixed solution at 90°C , remove the solvent N,N-dimethylformamide to obtain carboxylated cisplatin compound (CDDP-COOH);

[0027] (3) Disperse 100 mg of carboxylated cisplatin compound, 191 mg of NHS, and 325 mg of EDC in 5 mL of PBS, and react in the dark for 2 h to activate the carboxyl group;

[0028] (4) Mix 100 mg of activated carboxylated cisplatin and 120 mg of L-arginine, disperse them in 5 mL of PBS, stir and react at room temperature for 24 h, then dialyze the sample with a 5KDa dialysis bag, and then After freeze-drying, a cisplatin / argi...

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Abstract

The invention discloses a preparation method of a double-response nano prodrug for cancer synergistic treatment. The preparation method comprises the following steps: with cis-platinum as a precursor,performing carboxylation modification and then carboxyl activation on the cis-platinum; mixing the activated carboxyl cis-platinum with L-arginine; and forming a double-response nano prodrug with thecis-platinum / arginine composite structure through dehydration condensation of intermolecular carboxyl and amino. The method has advantages of being simple, green, and mild and being low in cost. Thecis-platinum can effectively inhibit DNA transcription to realize the effect of treating cancer; cis-platinum can promote H2O2 generation under the induction of NOX enzyme in vivo and the arginine serving as human amino acid can react with H2O2 to generate NO, so that tumor extinction is further induced. Therefore, the nano prodrug is expected to be developed into an efficient anticancer drug.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a method for preparing a double-response nano-prodrug for synergistic treatment of cancer. Background technique [0002] Cancer, as the disease with the highest fatality rate, has become a major threat to human life and health. Chemotherapy has remained the standard of clinical cancer treatment for the past few decades. However, the use of single free anticancer drugs is limited due to problems such as drug resistance, low accumulation in tumor areas, and side effects on normal tissues. Therefore, combining non-cross-resistant anticancer drugs to minimize the induction of drug resistance is an effective means to improve the therapeutic effect. [0003] Because of its unique anticancer effect, cisplatin has been widely used in clinical anticancer regimens alone or in combination. However, drug resistance and severe side effects reduce the treatment outcome. Resistance to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K33/243A61P35/00
CPCA61K47/542A61P35/00A61K33/243
Inventor 卢春华王海辉祝筱慧刘永飞杨黄浩
Owner FUZHOU UNIV
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