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Co-delivery system of photo-responsive chemotherapeutic drug and preparation method thereof

A chemotherapeutic drug and co-delivery technology, applied in the field of medicine, can solve the problems of inability to directly apply multi-drug co-delivery and low delivery efficiency, and achieve the effects of improving curative effect and targeting, good stability, and wide application value

Inactive Publication Date: 2017-07-14
SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, limited by the active site of the photosensitive carrier, a single photosensitive carrier molecule can only carry one drug molecule, the delivery efficiency is relatively low, and it cannot be directly applied to multi-drug synergistic delivery.

Method used

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  • Co-delivery system of photo-responsive chemotherapeutic drug and preparation method thereof
  • Co-delivery system of photo-responsive chemotherapeutic drug and preparation method thereof
  • Co-delivery system of photo-responsive chemotherapeutic drug and preparation method thereof

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preparation example Construction

[0051] 1. Preparation of double-branched photosensitive carrier:

[0052] The method reported in the reference (Tetrahedron Letters, 2016, 57, 959-963), the preparation route is as follows figure 1 As shown, the steps are as follows:

[0053] (1) Take 20mL of concentrated nitric acid, stir in an ice bath to 0°C, add 25mL of concentrated sulfuric acid into the pipette, stir for 20min in an ice bath, and then add 10g of m-bromobenzaldehyde. Stir at room temperature for 4 h, add a small amount of water, and adjust the pH to 3-4 with NaOH. Then it was extracted three times with ethyl acetate, and the organic phase was concentrated by rotary evaporation to obtain product 1; the product 1 was dissolved in 25 mL of methanol, and 2 g of sodium borohydride was added in batches under an ice bath, and stirred at room temperature for 2 h. 20 mL of water was added to the reaction solution, and then extracted three times with 20 mL of ethyl acetate, the organic phases were combined, dried...

preparation Embodiment 1

[0060] The preparation route of chlorambucil-bexarotene co-delivery system [OEG(1)-Cb-Bex] is as follows figure 2 shown, including the following steps:

[0061] (1) Weigh 0.4 g of double-branched photosensitive carrier 6 (1) and dissolve it in 15 mL of dichloromethane, add 0.24 g of chlorambucil, 0.2 g of dicyclohexylcarbodiimide and a small amount of 4- Dimethylaminopyridine was reacted with stirring at room temperature for 4 h; 10 mL of water was added, extracted three times with ethyl acetate, the organic phase was concentrated and then purified by column to obtain 0.29 g of yellow product 7(1), with a yield of 50%;

[0062] (2) Weigh 0.2 g of product 7 (1) and dissolve it in 15 mL of dichloromethane, add 0.1 g of bexarotene, 70 mg of dicyclohexylcarbodiimide and a small amount of 4-dimethylaminopyridine, and The reaction was stirred for 4 h; 10 ml of water was added, extracted three times with ethyl acetate, the organic phase was concentrated, and the residue was purifie...

preparation Embodiment 2

[0064] The preparation route of chlorambucil-compretin A4 co-delivery system [OEG(1)-Cb-A4] is as follows image 3 shown, including the following steps:

[0065] (1) Weigh 0.8 g of double-branched photosensitive carrier 6 (1) and dissolve it in 30 mL of dichloromethane, add 0.48 g of chlorambucil, 0.4 g of dicyclohexylcarbodiimide and a small amount of 4- Dimethylaminopyridine was reacted with stirring at room temperature for 4 h; 20 mL of water was added, extracted three times with ethyl acetate, the organic phase was concentrated and then purified by column to obtain 0.58 g of yellow product 7(1), with a yield of 50%;

[0066] (2) Weigh 0.4 g of the product 7 (1) and dissolve it in 15 mL of chloroform, add 0.13 g of p-nitrophenyl chloroformate and 0.2 mL of triethylamine, and stir at room temperature for 3 h. 20 mL of water was added to the reaction solution, extracted three times with 15 mL of ethyl acetate, the organic phases were combined and concentrated, and the residu...

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Abstract

The invention discloses a co-delivery system of a photo-responsive chemotherapeutic drug and a preparation method thereof. A prodrug is prepared through covalent linkage of a double branched type photosensitive carrier with o-nitrobenzyl as a structural unit and an antineoplastic drug with different mechanism of action to form the co-delivery system of the photo-responsive chemotherapeutic drug. The co-delivery system of the photo-responsive chemotherapeutic drug has the beneficial effects that the advantages of excellent controllability of exogenous excitation photons and multidrug resistance (MDR) effect of combined chemotherapy capable of effectively inhibiting tumors in tumor therapy are combined; and the controllable release of different drugs is realized by changing parameters of excitation light so as to solve the technical problem of intelligent drug release in the co-delivery systems of traditional drugs; and the co-delivery system can be applied to tumor treatment.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a light-responsive chemotherapeutic drug co-delivery system and a preparation method thereof. Background technique [0002] In cancer chemotherapy, single drug therapy often cannot achieve the best effect, and combination chemotherapy based on simultaneous administration of multiple drugs has become one of the effective solutions. A major reason for the failure of tumor chemotherapy is the multidrug resistance (MDR) effect of tumor cells, and combined chemotherapy is currently a common method to overcome MDR. Combination chemotherapy usually refers to the simultaneous administration of two or more drugs, which produce synergistic effects to obtain a therapeutic effect of 1+1>2. Compared with single drug therapy, drug combination can regulate different signaling pathways in cells, effectively improve anticancer activity while reducing the dosage of single drug and reduce side...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K45/06A61K31/192A61K31/196A61K31/09A61K31/704A61P35/00
Inventor 孙晓华苟小军刘嵬颜军梁立杨晨秦其辉
Owner SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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