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Preparation and antitumor application of double-drug cisplatin/doxorubicin-polydopamine prodrug nanoparticles

A nanoparticle and polydopamine technology, applied in the field of biomedicine, has achieved great clinical application prospects and simple operation

Inactive Publication Date: 2018-11-23
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a double-drug cisplatin / doxorubicin-polydopamine prodrug nanoparticle for reversing tumor multidrug resistance and its drug resistance The photothermal therapy-cocktail therapy integrated technical solution for tumor scarless treatment to solve the multidrug resistance of tumors to anticancer drugs such as doxorubicin and cisplatin in the original technology, as well as local tissue overheating damage in tumor treatment, Clinical application problems such as scarring, incomplete tumor ablation and recurrence

Method used

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  • Preparation and antitumor application of double-drug cisplatin/doxorubicin-polydopamine prodrug nanoparticles
  • Preparation and antitumor application of double-drug cisplatin/doxorubicin-polydopamine prodrug nanoparticles
  • Preparation and antitumor application of double-drug cisplatin/doxorubicin-polydopamine prodrug nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1 Preparation of doxorubicin-dopamine conjugate molecule

[0054] Step 1, 455.5 mg of 3,4-dihydroxyphenylpropionic acid, 405.36 mg of 1-hydroxybenzotriazole, and 619.2 mg of dicyclohexylcarbodiimide were dissolved in 20 mL of anhydrous dimethylformamide, After reacting at 25° C. for 4 hours, a dimethylformamide solution of 396.5 mg tert-butyl carbazate was added dropwise into the reaction flask. After reacting at 25°C for 20 hours, centrifuge to remove dicyclohexylurea, and then evaporate with an oil pump at 60°C. The column was loaded with petroleum ether, and the eluent was a mixed solvent of ethyl acetate:petroleum ether (3:1), Rf=0.35. Vacuum oven dry. The product is white powdery solid tert-butyl-2-(3-(3,4-dihydroxyphenyl)propionyl)hydrazinecarboxylate. The yield is 47.3-61.0%.

[0055] Step 2: Dissolve tert-butyl-2-(3-(3,4-dihydroxyphenyl) propionyl) hydrazine carboxylate in 5 mL of dichloromethane, slowly add 2 mL of trifluoroacetic acid, and stir ...

Embodiment 2p

[0060] Example 2 Preparation of pH-responsive doxorubicin-polydopamine prodrug nanoparticles

[0061] Add 410mg of tris, 20mL of distilled water to a 50mL round bottom flask, stir at 30°C for 30 minutes, dissolve 12.5mg of dopamine hydrochloride and 2.74mg of the doxorubicin-dopamine conjugate molecules obtained in Example 1 in 1mL of distilled water was quickly injected into the above solution, and the reaction time was 24 hours, and the nanoparticle solution was black. Distilled water dialysis (dialysis bag molecular weight cut-off 3500) for two days, 1000mL distilled water × 8. Freeze dry for 48 hours. The yield is 38%~45%.

[0062] The dynamic light scattering pattern of the doxorubicin-polydopamine prodrug nanoparticles prepared in this embodiment is as follows: Figure 4 As shown, its number average particle diameter is 90±8nm, and PDI is 0.65±0.02.

Embodiment 3p

[0063] Example 3 Preparation of pH-responsive doxorubicin-polydopamine prodrug nanoparticles

[0064] The difference between this example and Example 2 is that the molecular weights of dopamine hydrochloride and doxorubicin-dopamine conjugate are 12.5 mg and 5 mg, respectively. The yield of the product obtained in this example is 34%-39%.

[0065] The dynamic light scattering pattern of the doxorubicin-polydopamine prodrug nanoparticles prepared in this embodiment is as follows: Figure 5 As shown, the number average particle diameter is 88±8nm, and the PDI is 0.46±0.08.

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Abstract

The invention relates to the preparation and antitumor application of double-drug cisplatin / doxorubicin-polydopamine prodrug nanoparticles. The nanoparticles provided by the invention are formed by the coordination of doxorubicin-polydopamine prodrug nanoparticles with cisplatin. The nanoparticles provided by the invention can be used to reverse tumor multidrug resistance. Compared with the priorart, the nanoparticles provided by the invention have strong absorption in the near-infrared region, and can effectively convert near-infrared light (NIR) having wavelength of 650 nm to 1000 nm into heat to kill cancer cells, thereby achieving photothermotherapy under mild illumination. Importantly, the nanoparticles can release two active drugs of doxorubicin and cisplatin in the cells, and realize the cocktail therapy of synergistic reversal of drug-resistant tumors, that is, the synergistic treatment of drug-resistant tumors by two chemotherapeutic drugs. In addition, a new integrated photothermotherapy-cocktail therapy technology for traceless treatment and complete ablation of drug-resistant tumors has been developed in combination with mild photothermotherapy.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the preparation of double-drug cisplatin / doxorubicin-polydopamine prodrug nanoparticles, photothermotherapy-cocktail therapy and anti-tumor application. Background technique [0002] In recent years, cancer has overtaken heart disease as the leading cause of death facing humans worldwide. Therefore, the development of simple and efficient anticancer strategies is a major technical problem that needs to be solved urgently. At present, clinical chemotherapy is one of the most convenient and widely used effective cancer treatment methods, and the most widely used anticancer drugs are doxorubicin and cisplatin active drugs. However, chemotherapy often has the risk of killing normal cells, destroying the immune system and increasing the incidence of secondary cancers, and doxorubicin and cisplatin anticancer drugs are prone to multidrug resistance, and even some tumors (such as b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/59A61K47/69A61K41/00A61K33/24A61K31/704A61P35/00
CPCA61K31/704A61K33/24A61K41/0052A61K47/59A61K47/6935A61P35/00A61K2300/00
Inventor 杜畅董常明
Owner SHANGHAI JIAO TONG UNIV