Injection Cu(DDC)2 protein nano-particle preparation used for treating tumor, and preparation method thereof

Abstract

A compound Cu(DDC)2 with relatively high tumor-inhibiting activity can be used for treating cancers such as melanoma, breast cancer, lung cancer, liver cancer, and the like. The treatment effect is broad, and the compound has certain selective killing effect against tumor cells. The invention relates to an Cu(DDC)2 injection protein nano-particle preparation used for treating tumor, and a preparation method thereof. Therefore, problems of poor water-solubility and difficulty in intravenous administration of Cu(DDC)2 are solved. According to the invention, with an ultrasonic method, a high-pressure homogenization method, and a micro-jet method, the Cu(DDC)2 injection protein nano-particles are prepared. The Cu(DDC)2 protein nano-particles are prepared from the components that (Cu(DDC)2 + organic solvent) :(protein + water) = 1:2-1:30, wherein the specification of Cu(DDC)2 is 0.01-5mg/mL, the specification of protein is 0.05-25% (w/v), and a ratio of organic solvent to water is 1:2-1:30. Proteins such as human serum albumin (HSA), bovine serum albumin (BSA), hydrophobic protein, glycoprotein, and lipoprotein or polypeptide is adopted as a carrier and a stabilizer for coating medicine particles, such that the particles have good biocompatibility and high security. Cu(DDC)2 tumor-inhibiting treatment effect is improved, and adverse reaction is reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular provides a Cu(DDC) injection for treating tumors 2 Protein nanoparticle preparation and preparation method thereof. Background technique [0002] Cu(DDC) 2 (Copper Diethyldithiocarbamate), the Chinese full name is N,N-diethyldithiocarbamate copper, which is chelated by two molecules of DDC (N,N-diethyldithiocarbamate) and one molecule of copper (structure Such as formula I). DDC is the metabolite of the anti-alcoholic drug disulfiram (disulfiram, also known as disulfide tetraethylthiuram, disulfiram, structure such as formula II) in the body through the reduction of glutathione reductase system in red blood cells, and Both disulfiram and DDC are easily chelated with copper, eventually forming Cu(DDC) 2 . [0003] [0004] Formula Ⅰ [0005] [0006] Formula II [0007] The study found that Cu(DDC) 2 Positive anticancer efficacy: Nuclear transcription fact...

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to provide Cu (DDC) for injection for treating tumors 2 Nanoparticle preparation and preparation method thereof, the preparation solves Cu(DDC) 2 The problem of poor water solubility, nano-scale Cu(DDC) for intravenous injection with protein as drug carrier 2 Preparation, has the advantages of high efficacy, less toxic and side effects, long-lasting effect, good stability, etc.

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