Preparation method of oxidation-reduction double-response type macromolecular camptothecin prodrug

A camptothecin and polymer technology, applied in the field of medicinal chemistry, can solve the problems of uncontrollable release, poor selectivity of anti-tumor drugs, low drug loading rate, etc., and achieve the effect of high micellar stability
CN109364262AInactive Publication Date: 2019-02-22SOUTHWEST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SOUTHWEST UNIV
Publication Date
2019-02-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of an oxidation-reduction double-response type macromolecular camptothecin prodrug. Beta-cyclodextrin-CD is used as a carrier to stimulate splitting decomposition of disulfide bonds and oxalate bonds in prodrug molecules respectively through high-concentration glutathione and hydrogen peroxide in tumor microenvironment and to release an anti-cancer drugcamptothecin CPT. The preparation method comprises the following steps of 1 preparation of camptothecin monomers CPTGSH and CPTROS containing functional bonds, 2 preparation of a drug initiator beta-CD-Br, 3 preparation of CD-b-P (CPTGSH-co-CPTROS-co-OEGMA named as CPGR. The obtained monomolecular micelles formed by the dual-response prodrug have the advantages of high drug loading capacity (40%or above by weight), high micelle stability, sensitive stimulus response, superior biocompatibility, low toxic side effects and the like.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of a redox double-responsive polymer camptothecin prodrug and its application in the field of cancer treatment. Background technique

[0002] Cyclodextrin (Cyclodextrin, referred to as CD, a polysaccharide, molecular formula (C6H10O5) n) is the general name of a series of cyclic oligosaccharides produced by amylose in Bacillus, usually containing 6-12 D-glucopyranose unit. Cyclodextrin is a cyclic macromolecular polysaccharide formed by the polymerization of several glucose molecules, which can effectively increase the solubility of some poorly water-soluble drugs in water, and is a good drug carrier. Camptothecin (CPT for short, molecular formula: C 20 h 16 N 2 O 4 , CAS No.: 7689-03-4, relative molecular weight: 348.43) is a cytotoxic quinoline alkaloid that can selectively inhibit topoisomerase Ⅰ (Topo Ⅰ), bind to the complex formed by T...

Claims

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