Cellulose-based camptothecin prodrug and preparation method thereof

A camptothecin and cellulose technology, which is applied to the field of cellulose-based camptothecin prodrugs and their preparation, can solve the problems of difficulty in ensuring selective and controllable drug release, poor selectivity, and low drug loading, and achieves structural Controllable, increase upload capacity, enhance the effect of internalization

Inactive Publication Date: 2018-12-21
SOUTHWEST UNIVERSITY
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0005] Aiming at the disadvantages of existing unimolecular polymeric prodrugs, such as poor selectivity, low drug loading capacity, and difficulty in ensuring selective and controllable drug release, the present invention aims to provide a preparation of a class of cellulose-based camptothecin prodrugs Method and its application in the field of drug treatment of cancer

Method used

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  • Cellulose-based camptothecin prodrug and preparation method thereof
  • Cellulose-based camptothecin prodrug and preparation method thereof
  • Cellulose-based camptothecin prodrug and preparation method thereof

Examples

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Embodiment 1

[0029] Example 1 Preparation of a class of cellulose-based camptothecin prodrugs

[0030] The schematic diagram of the total synthesis of a class of cellulose-based camptothecin prodrugs is shown as figure 1 As shown, it mainly includes the following steps:

[0031] (1) The preparation of intermediate MABHD containing disulfide bonds includes the following steps: in an ice bath and argon atmosphere, dissolve BHD (5g, 32.4mmoL) in 50mL THF, and then TEA (2.6mL, 18.9mmoL) ) Slowly add the above BHD solution in THF; Dissolve methacryloyl chloride (1.8mL, 18.2mmoL) in 10mL anhydrous THF, then add the methacryloyl solution dissolved in anhydrous THF slowly with stirring to In the above reaction system, the reaction was carried out at 0° C. for 0.5 h, and then heated to room temperature for 24 h. The column was purified to obtain the intermediate MABHD containing disulfide bonds.

[0032] (2) Preparation of MABHD-CPT, a CPT precursor containing disulfide bonds, includes the following step...

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Abstract

The invention discloses a cellulose-based camptothecin prodrug and a preparation method thereof. The preparation method comprises the following steps: (1), preparing a drug initiator MCC-Br; (2), preparing a camptothecin monomer MABHD-CPT; (3), through an atom transfer radical polymerization (ATRP) reaction, polymerizing the hydrophobic camptothecin monomer MABHD-CPT and a hydrophilic polyethyleneglycol methacrylate OEGMA to obtain an amphiphilic polymer MCC-P(MABHD-CPT)-b-P(OEGMA), which is named as MCO. The obtained amphiphilic polymer prodrug can form a single molecular drug micelle in water, has the advantages of high micelle stability, a controllable micelle shape, high drug loading amount, low toxic and side effects, good controlled drug release and the like, effectively solves theproblem of low solubility of hydrophobic drug molecules, and provides an efficient drug delivery system.

Description

Technical field [0001] The invention relates to the field of polymer chemical medicines, in particular to a class of cellulose-based camptothecin prodrugs and a preparation method thereof. Background technique [0002] Cellulose (MCC for short) is a polysaccharide composed of glucose with the molecular formula, (C 6 H 10 O 5 )n) It has many excellent properties: good water solubility, stable chemical properties, biodegradability, non-toxic, non-irritating, etc. It is widely used in various pharmaceutical preparations and is a good drug carrier material. Camptothecin (Camptothecin, CPT, chemical structure: C 20 H 16 N 2 O 4 , CAS number: 7689-03-4, relative molecular weight: 348.43) is a plant anticancer drug extracted from Camptotheca acuminata distributed in central and southwestern China. It has good curative effect on gastrointestinal tract and head and neck cancer. Camptothecin is a cytotoxic quinoline alkaloid and can inhibit DNA topoisomerase (TOPO I). [0003] Due to the s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K47/69A61K31/4745A61P35/00
CPCA61K31/4745A61K47/61A61K47/6907A61P35/00
Inventor 许志刚白霜康跃军马晓倩
Owner SOUTHWEST UNIVERSITY
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