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A kind of platinum antitumor prodrug, its nano hydrogel drug and preparation method thereof

A prodrug, platinum drug technology, applied in the field of biomedicine, can solve the problems of fast metabolism, short circulation time, poor targeting, etc., and achieve the effect of clear and concise preparation process and reduced side effects

Inactive Publication Date: 2018-10-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, tetravalent platinum complex (Pt(IV)), as a small molecule drug, also has the characteristics of short circulation time, fast metabolism and poor targeting in the human body, and it is difficult to effectively enrich it in the tumor site. Delivery to tumor tissue sites remains a big challenge

Method used

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  • A kind of platinum antitumor prodrug, its nano hydrogel drug and preparation method thereof
  • A kind of platinum antitumor prodrug, its nano hydrogel drug and preparation method thereof

Examples

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Effect test

Embodiment 1

[0030] Example 1: Preparation of cisplatin antitumor prodrugs

[0031]Add 2g of cisplatin, 50ml of deionized water and 11.4ml of hydrogen peroxide (30%) into a 100ml three-neck round bottom flask, and react in a nitrogen atmosphere at 70°C in the dark for 6h, then cool down to room temperature for another 12h, and spin evaporate After part of the water, the product was cooled with ice water to precipitate the product, suction filtered, and the reaction product was washed with ice water, ethanol, and ether once and then vacuum-dried to obtain a Pt(IV) precursor modified with hydroxyl groups at both ends of the axial direction, which was recorded as Pt(IV)-( Oh) 2 -1.

[0032] Take the above 2g precursor Pt(IV)-(OH) 2 -1 into a 50ml three-neck round bottom flask, then add methacrylic anhydride and 10ml pre-dried dimethyl sulfoxide (DMSO) at a molar ratio of 1:2, and react for 24 hours under a nitrogen atmosphere and 60°C in the dark After the reaction, the solvent was removed...

Embodiment 2

[0033] Example 2: Preparation of Oxaliplatin Antitumor Prodrugs

[0034] Add 2 g of oxaliplatin, 50 ml of deionized water, and 11.4 ml of hydrogen peroxide (30%) into a 100 ml three-neck round bottom flask. Under a nitrogen atmosphere, react at 70 ° C for 6 h in the dark, then cool down to room temperature for another 12 h, spin After evaporating part of the water, cool and precipitate the product with ice water, filter it with suction, wash the reaction product once with ice water, ethanol, and ether, and then dry it in vacuum to obtain a Pt(IV) precursor modified with hydroxyl groups at both ends of the axial direction, denoted as Pt(IV) -(OH) 2 -2

[0035] Take the above 2g precursor Pt(IV)-(OH) 2 -1 into a 50ml three-neck round bottom flask, then add methacrylic anhydride and 10ml pre-dried dimethyl sulfoxide (DMSO) at a molar ratio of 1:2, and react for 24 hours under a nitrogen atmosphere and 60°C in the dark After the reaction, the solvent was removed by lyophilizati...

Embodiment 3

[0036] Example 3: Preparation of Oxaliplatin Antitumor Prodrug Nano Hydrogel Microspheres

[0037] MAA monomer 400 mg, ZDMA cross-linking agent 100 mg, AIBN initiator 16.7 mg, acetonitrile 40 mL, heated to 95 ° C, reflux solvent reaction for 2 hours, centrifuged to remove solvent and unreacted monomer, washed with ethanol and deionized water for 3 and dried in a vacuum oven for 24 h.

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Abstract

The invention belongs to the technical field of biological medicines and particularly provides an anti-tumor platinum pro-drug and a nanometer hydrogel drug and a preparation method thereof.The pro-drug is obtained by conducting hydrogen peroxide oxidation on an anti-tumor platinum drug to obtain a Pt(IV) sexadentate complex and then making the sexadentate complex react with anhydride or carboxylic acid containing double bonds.The pro-drug can be in self-polymerization or can be copolymerized with other hydrophilic monomers for the preparation of drug micro-spheres having high drug loading capacity.The micro-spheres are uniform in particle size and controllable in size and can keep long-term stability in an aqueous solution by using a stabilizer.The preparation method is simple, an obtained nanometer hydrogel drug carrier has glutathione stimulus responsibility, so that nanometer hydrogel is kept stable in a low-glutathione-concentration environment outside tumor cells, the drug is rarely leaked after long-time cycle, the nanometer hydrogel is rapidly degraded in the reducing environment within the tumor cells and converted into a linear chain of small molecular weight, the drug is quickly released, and the targeted killing effect on the target tumor cells is achieved.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a platinum-based antitumor prodrug, a nano hydrogel drug thereof and a preparation method thereof. Background technique [0002] Due to the great threat of cancer to human life and health, the research of anticancer drugs has been widely concerned. Cisplatin is also called cis-dichlorodiammine platinum (Cisplatin, Pt(NH 3 ) 2 Cl 2 ), is a non-cell cycle-specific anticancer drug with cytotoxicity, which can combine with the N7 nitrogen atom of guanine on the DNA double helix to form a stable cross-linked structure, thereby destroying the replication function of DNA and causing cell apoptosis. Since the anticancer activity of cisplatin was discovered in 1967, the research and application of platinum metal anticancer drugs have been greatly developed. In addition to cisplatin, there are a series of cisplatin derivatives with similar structures and functions, such...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/555A61K33/24A61K9/06A61K9/16A61K47/34A61P35/00A61K47/32
CPCA61K9/06A61K9/1641A61K47/22C07F15/0093
Inventor 张子豪汪长春
Owner FUDAN UNIV
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