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
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[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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