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Cinobufagin-loaded PDA nano-drug as well as preparation method and application thereof

A nano-drug, cinobufacin technology, applied in nano-drugs, drug combinations, nanotechnology, etc., can solve problems such as short circulation half-life, low bioavailability, poor water solubility of cinobufacin, and achieve good biocompatibility, The effect of uniform distribution, good colloidal stability and biocompatibility

Pending Publication Date: 2022-06-07
LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility, short circulation half-life and low bioavailability of cinobufacin, how to improve the anticancer efficacy of cinobufacin is a scientific problem that needs to be solved clinically.

Method used

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  • Cinobufagin-loaded PDA nano-drug as well as preparation method and application thereof
  • Cinobufagin-loaded PDA nano-drug as well as preparation method and application thereof
  • Cinobufagin-loaded PDA nano-drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1--Preparation method of ammonia water for PDA nanomedicine loaded with cinobufacini

[0030] (1) First, the blank PDA nanocarriers or the PDA nanomedicines loaded with cinobufagin were synthesized by using ammonia water in alcohol solution. First mix 290mL ultrapure water, 110mL ethanol and 1.5mL NH 4 OH was stirred at room temperature for 30 minutes. Then 50 mg of cinobufacini or 50 mg of doxorubicin (no blank nanocarrier added) was added to 10 ml of ethanol. Add 0.5 g of dopamine hydrochloride to 10 mL of ultrapure water, and stir overnight. Finally, the nano-drugs were collected by centrifugation, centrifuged at 10,000 rmp for 10 minutes, the unloaded drug was taken out, centrifuged at room temperature, washed twice with ultrapure water, and dried on a freeze dryer overnight.

[0031] (2) FA was then modified on the surface of nanoparticles with EDC\NHS. First, the above nanodrugs (100 mg) were dispersed in 10 ml of PBS buffer (10 mM, pH=6.0). Subsequen...

Embodiment 2

[0032] Embodiment 2--Tris-HCl preparation method of PDA nanomedicine loaded with cinobufacini

[0033] First, 72 mL of ethanol was added to 400 mL of Tris-HCl (10 mM, pH=8.5) buffer solution, and the mixture was stirred uniformly at 37°C. Then 50 mg of cinobufacini or 50 mg of doxorubicin (without the blank nanocarrier) was added to 10 ml of ethanol. Add 0.5 g of dopamine hydrochloride to 10 mL of ultrapure water, and stir overnight. During the reaction, the mixed solution rapidly changed from colorless to black, indicating the formation of PDA nanocarriers. Finally, the nano-drugs were collected by centrifugation, centrifuged at 10,000 rmp for 10 minutes, the supernatant was discarded, the unloaded drug was removed, centrifuged at room temperature, washed twice with ultrapure water, and dried on a freeze dryer overnight.

[0034] For the modification of targeting molecule FA, the above nanodrugs (100 mg) were first dispersed in 10 ml of PBS buffer (10 mM, pH=6.0). Subseque...

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Abstract

The invention relates to a preparation method of a cinobufagin-loaded PDA nano-drug, which comprises the following steps: (1) synthesizing a PDA nano-drug: preparing ammonia water or an alcohol-water solution of Tris-HCl, with the volume ratio of ethanol to water in the alcohol-water solution being 1: 1-1: 10; the preparation method comprises the following steps: adding cinobufagin and dopamine hydrochloride into an alcohol-water solution of ammonia water or Tris-HCl according to the molar ratio of cinobufagin to dopamine hydrochloride of 1: 1-1: 20 and the molar ratio of ammonia water or Tris-HCl to dopamine hydrochloride of 1: 1-1: 50, stirring, collecting the PDA nano-drug by using a centrifugal method, washing and drying; and (2) modification of the targeting molecule: dispersing the PDA nano-drug in a PBS buffer solution, using EDC / NHS to combine with targeting molecule folic acid with carboxyl through a coupling reaction of amino and carboxyl, with the molar ratio of EDC / NHS to dopamine hydrochloride being 1: 1-1: 10 and the molar ratio of folic acid to dopamine hydrochloride being 1: 1-1: 50, centrifugally collecting the targeting molecule modified nano-drug, washing and drying to obtain the targeting molecule modified nano-drug. And preparing the cinobufagin-loaded PDA nano-drug. The invention also discloses an application of the cinobufagin-loaded PDA nano-drug in preparation of anti-lung cancer drugs.

Description

technical field [0001] The invention relates to the preparation and application of anti-cancer nano-medicine, in particular to a polydopamine nano-medicine loaded with Chinese medicine monomer cinobufacini, which has targeted drug delivery and intelligent response, and its preparation and application. Background technique [0002] Malignant tumors have the characteristics of fast growth, strong metastasis and high recurrence rate. They have become the main killers that threaten human health, and their morbidity and mortality are still rising. At present, although many chemotherapeutic drugs in clinical use can inhibit tumor growth to a certain extent, they have disadvantages such as large toxic and side effects, low drug utilization rate, and large cumulative dose. However, nanoplatforms constructed by loading small-molecule anticancer drugs with nanomaterials have the advantages of targeted drug delivery and high drug release at the lesion site, which can reduce normal tiss...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61K47/34A61K41/00A61P35/00B82Y5/00B82Y40/00
CPCA61K31/585A61K47/34A61K41/0052A61P35/00B82Y5/00B82Y40/00A61K2300/00
Inventor 张占霞郑展李建文张军千
Owner LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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