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Nano-drug containing cis-platinum and arsenic trioxide and preparation method thereof

A nano-drug and nano-composite technology, applied in the directions of medical preparations, drug combinations, and pharmaceutical formulations containing active ingredients, can solve the problems of cisplatin's easy neurotoxicity, strong cisplatin resistance, and nephrotoxicity, etc. Achieving the effect of inhibiting the growth, enhancing the effect, enhancing the therapeutic effect

Inactive Publication Date: 2018-05-11
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cisplatin chemotherapy also faces the same problem as ATO. Cisplatin is prone to neurotoxicity and nephrotoxicity. In addition, many tumors are currently highly resistant to cisplatin.

Method used

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  • Nano-drug containing cis-platinum and arsenic trioxide and preparation method thereof
  • Nano-drug containing cis-platinum and arsenic trioxide and preparation method thereof
  • Nano-drug containing cis-platinum and arsenic trioxide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of cisplatin arsenite nanocomposite (PtAs)

[0027] (1) Preparation of diammine platinum acetate dihydrate

[0028] Add 150mg of cisplatin, 166mg of silver acetate, and 10ml of deionized water into a 25mL round bottom flask, heat at 55°C for 24h in the dark, centrifuge to remove the precipitate, and filter the supernatant with a 0.22μm filter membrane to obtain a concentration of about 0.05mol / L diammine platinum acetate dihydrate.

[0029] (2) Preparation of cisplatin arsenite nanocomposite (PtAs)

[0030] Add 5mL cyclohexane into a 25mL round bottom flask, add 2mL surfactant CO-520 at the same time, and successively add 0.05mol / L diammine platinum acetate solution 326μL, and the same volume of arsenic aqueous solution ( 0.1mol / LNaAsO 2 ). The mixed solution was stirred and mixed evenly (the rotation speed was 800r / min), and the reaction was kept at the rotation speed for 24h. After the reaction is finished, ethanol is used for preci...

Embodiment 2

[0031] Example 2: Preparation of nano-anticancer drug (PtAs@PAH-DXS) containing cisplatin and arsenic agent coated with polymer on the surface

[0032] In a 10mL round bottom flask, add 3mL of the aqueous solution of cisplatin arsenite nanocomposite in Example 1, then slowly add the PBS solution with an equal volume concentration of 0.5mg / mL polyallylamine (PAH) under constant stirring, and react After 3h, use an ultrafiltration tube for ultrafiltration, and wash the ultrafiltration several times with deionized water, then slowly add 5mL of dextran (DXS) aqueous solution with a concentration of 0.5mg / mL to the liquid on the intercepted ultrafiltration membrane, and react for 3h , and purified by ultrafiltration in the same way to obtain a nano-anticancer drug containing cisplatin and arsenic (PtAs@PAH-DXS).

Embodiment 3

[0033] Example 3: Scale up the preparation of nano-anticancer drugs containing cisplatin and arsenic (PtAs@PAH-DXS)

[0034] Add 25mL cyclohexane into a 50mL round bottom flask, add 10mL CO-520 at the same time, add 0.05mol / L diammine platinum acetate solution 1630μL, and the same volume of arsenic aqueous solution (0.1mol / L NaAsO 2 ). After reacting for 24 hours, precipitate with ethanol, centrifuge to remove the supernatant, wash the precipitate several times with ethanol and deionized water, and finally obtain the cisplatin arsenite nanocomposite (PtAs).

[0035] Take out 3 mL of cisplatin arsenite nanocomposite, slowly add PBS solution with an equal volume concentration of 0.5 mg / mL polyallylamine (PAH) under constant stirring, react for 3 h, then ultrafilter, and wash the ultrafiltration with deionized water. After several times of filtration, slowly add 5 mL of dextran (DXS) aqueous solution with a concentration of 0.5 mg / mL to the liquid on the intercepted ultrafiltrat...

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Abstract

The invention relates to a nano-drug containing cis-platinum and arsenic trioxide and a preparation method thereof, which relate to nano-drugs. The nano-drug containing the cis-platinum and the arsenic trioxide is a nanoscale cis-platinum arsenite compound ([Pt(NH3)2(H2O)2]HAsO3). The nano-drug containing the cis-platinum and the arsenic trioxide adopts a high polymer material as a surface coatedcarrier loading effective components ATO and the cis-platinum therein. The preparation method comprises the steps of preparing cis-diamminedihydrateplatinum acetate; preparing the cis-platinum arsenite nano compound; coating the surface of the cis-platinum arsenite nano compound with a high polymer material layer, and preparing to obtain the nano-drug (PtAs@PAN-DXS) containing the cis-platinum andthe arsenic trioxide. A reversed-phase microemulsion method and a high polymer layer by layer self-assembly method have the advantages of simple and easy steps, convenient operation, higher yield, controllable quality, and easy preparation in an amplification way. The nano-drug has a higher anticancer effect, can be more beneficial to effectively killing and inhibiting cancer cells, and achievesa better chemotherapeutic effect.

Description

technical field [0001] The invention relates to nanometer medicines, in particular to a nanometer medicine containing cisplatin and arsenic which can simultaneously load two kinds of medicines with high-efficiency anticancer effects and a preparation method thereof. Background technique [0002] Cancer has become one of the diseases that seriously endanger human health and quality of life. According to statistics, there were approximately 4.29 million new cancer cases and 2.81 million cancer deaths in China in 2015. Despite the continuous development of researchers, dozens of drugs have been put into clinical treatment, but the effect of treating cancer is far lower than expected. The main reason is that most traditional chemotherapy drugs are small molecule drugs, which have short blood circulation time, low effective concentration in tumor tissue, easy to produce toxic and side effects, and tumor cells will develop drug resistance mechanisms during treatment. Therefore, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/32A61K47/36A61K33/24A61K33/36A61P35/00
CPCA61K9/5138A61K9/5161A61K33/24A61K33/36A61K2300/00
Inventor 高锦豪辛靖宇
Owner XIAMEN UNIV
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