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A kind of biomimetic dopamine polymerized drug-loaded nano-delivery system and its preparation method

A drug-loaded nanometer and dopamine technology, applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of shortened blood half-life, inability to achieve efficient drug delivery, accelerated blood clearance, etc. Capacitance, the effect of increasing the load capacity

Active Publication Date: 2022-05-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the existing methods of modifying polydopamine mainly use PEG modification. Studies have shown that after multiple applications of PEG, the immunogenicity of PEG will cause obvious humoral immune responses, and has the effect of accelerating blood clearance. PEG-modified carriers It will be recognized and cleared by phagocytes, and its blood half-life is significantly shortened, which cannot achieve efficient drug delivery

Method used

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  • A kind of biomimetic dopamine polymerized drug-loaded nano-delivery system and its preparation method
  • A kind of biomimetic dopamine polymerized drug-loaded nano-delivery system and its preparation method
  • A kind of biomimetic dopamine polymerized drug-loaded nano-delivery system and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Synthesis of dopamine polymeric drug-loaded nanoparticles loaded with doxorubicin

[0047] Prepare a 10 mg / mL dopamine solution with pure water, and a 20 mg / mL doxorubicin solution with DMSO. According to the mass ratio of dopamine and doxorubicin of 1:0.5, the dopamine solution and doxorubicin solution were added dropwise to the Tris-HCl buffer solution with pH=8.5, so that the final concentration of dopamine was 0.2 mg / mL. After stirring and reacting for 24 hours in the dark at room temperature under the condition of oxygen flow in the dark, put it in a 3500Da dialysis bag, place it in pure water, and dialyze in the dark to remove the unencapsulated doxorubicin, that is, to obtain the dopamine polymer loaded with doxorubicin. drug nanoparticles. The drug-loading capacity of the nanoparticles was measured by fluorescence spectrophotometry to be 32.3%, and the encapsulation efficiency was 95.7%.

Embodiment 2

[0049] Synthesis of dopamine polymeric drug-loaded nanoparticles loaded with doxorubicin

[0050] Prepare dopamine solution and doxorubicin solution according to Example 1, according to the mass ratio of dopamine and doxorubicin of 1:1, respectively add dopamine solution and doxorubicin solution dropwise to the Tris-HCl buffer solution with pH=8.5, Make the final concentration of dopamine 0.2 mg / mL. After stirring and reacting for 24 hours in the dark at room temperature under the condition of oxygen flow in the dark, put it in a 3500Da dialysis bag, place it in pure water, and dialyze in the dark to remove the unencapsulated doxorubicin, that is, to obtain the dopamine polymer loaded with doxorubicin. drug nanoparticles. The drug-loading capacity of the nanoparticles was measured by fluorescence spectrophotometry to be 47.6%, and the encapsulation efficiency was 90.9%.

Embodiment 3

[0057] Synthesis of dopamine-loaded polymer nanoparticles loaded with doxorubicin

[0058] Prepare dopamine solution and doxorubicin solution according to Example 1, according to the mass ratio of dopamine and doxorubicin of 1:2, respectively add dopamine solution and doxorubicin solution dropwise to the Tris-HCl buffer solution with pH=8.5, Make the final concentration of dopamine 0.2 mg / mL. After stirring and reacting for 24 hours in the dark at room temperature under the condition of oxygen flow in the dark, put it in a 3500Da dialysis bag, place it in pure water, and dialyze in the dark to remove the unencapsulated doxorubicin, that is, to obtain the dopamine polymer loaded with doxorubicin. drug nanoparticles. The drug-loading capacity of the nanoparticles was measured by fluorescence spectrophotometry to be 63.6%, and the encapsulation efficiency was 87.4%.

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Abstract

The invention belongs to the field of pharmacy, and discloses a bionic dopamine polymer-loaded drug-loaded nano-delivery system. The nano-delivery system includes dopamine polymer-loaded drug-loaded nanoparticles prepared from dopamine and anti-tumor drugs, and bionic dopamine grafted on the surface of polydopamine. Tumor targeting protein or polypeptide. The dopamine of the present invention encapsulates the drug inside the polydopamine in the form of polymerized drug loading, which significantly improves the encapsulation efficiency of the drug and has a higher drug loading capacity; subsequently, the biomimetic tumor targeting protein or polypeptide is covalently grafted to the polydopamine The surface endows the nano-delivery system with biomimetic properties and targeting functions. The nano-delivery system prepared by the present invention has triple-response rapid drug release characteristics of pH, ROS and photothermal, and can achieve the purpose of tumor chemotherapy-photothermal combined therapy through tumor targeting, and has a good application prospect in tumor targeted combined therapy .

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a nano-medicine and a preparation method thereof, in particular to a biomimetic dopamine polymerized drug-loaded nano-delivery system and a preparation method thereof. Background technique [0002] Traditional cancer treatment methods mainly include surgical resection, chemotherapy, immunotherapy, and radiation therapy. Among them, chemotherapy refers to the therapeutic effect of chemotherapy drugs by interfering or blocking the division and proliferation of tumor cells. Chemotherapy is the most commonly used treatment plan for clinical treatment of cancer patients, but there are still certain limitations. In the process of killing tumor cells by chemotherapy, due to its non-specificity, it is widely distributed in the body after administration, and it often causes toxicity to normal and rapidly proliferating cells in the body, such as digestive tract cells, bone marrow hematopoietic cells,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/64A61K41/00A61K45/06A61K31/704A61K31/4745A61K31/12A61P35/00
CPCA61K9/5146A61K47/64A61K47/643A61K41/0052A61K45/06A61K31/704A61K31/4745A61K31/12A61P35/00A61K2300/00
Inventor 丁杨张华清陈杰周建平
Owner CHINA PHARM UNIV
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