Biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing system and preparation method thereof

A drug-loading nanometer and dopamine technology, applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of accelerated blood clearance, shortened blood half-life, unable to achieve efficient drug delivery, etc., to increase the load capacity and reduce toxic side effects , Guarantee the effect of efficient release

Active Publication Date: 2020-12-25
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,

Method used

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  • Biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing system and preparation method thereof
  • Biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing system and preparation method thereof
  • Biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0045]Example 1

[0046]Synthesis of dopamine polymerized drug-loaded nanoparticles containing doxorubicin

[0047]Prepare a 10 mg / mL dopamine solution with pure water and a 20 mg / mL adriamycin solution with DMSO. According to the mass ratio of dopamine and adriamycin of 1:0.5, the dopamine solution and the adriamycin solution were added dropwise to the Tris-HCl buffer with pH=8.5, so that the final concentration of dopamine was 0.2 mg / mL. After the reaction was stirred for 24 hours in the dark under the condition of oxygen ventilation at room temperature, it was placed in a 3500Da dialysis bag, placed in pure water, and dialyzed against light to remove the unencapsulated doxorubicin, and the dopamine polymer carrier containing dopamine was obtained. Drug nanoparticles. Measured by fluorescence spectrophotometry, the drug loading of the nanoparticles was 32.3%, and the encapsulation efficiency was 95.7%.

Example Embodiment

[0048]Example 2

[0049]Synthesis of dopamine polymerized drug-loaded nanoparticles containing doxorubicin

[0050]Prepare the dopamine solution and doxorubicin solution according to Example 1. According to the mass ratio of dopamine and doxorubicin at 1:1, add the dopamine solution and doxorubicin solution dropwise to the Tris-HCl buffer with pH=8.5. Make the final concentration of dopamine 0.2mg / mL. After the reaction was stirred for 24 hours in the dark under the condition of oxygen ventilation at room temperature, it was placed in a 3500Da dialysis bag, placed in pure water, and dialyzed against light to remove the unencapsulated doxorubicin, and the dopamine polymer carrier containing dopamine was obtained. Drug nanoparticles. Measured by fluorescence spectrophotometry, the drug loading of the nanoparticles was 47.6%, and the encapsulation efficiency was 90.9%.

Example Embodiment

[0056]Example 3

[0057]Synthesis of dopamine polymerized drug-loaded nanoparticles containing doxorubicin

[0058]Prepare the dopamine solution and doxorubicin solution according to Example 1. According to the mass ratio of dopamine and doxorubicin at 1:2, add the dopamine solution and doxorubicin solution dropwise to the Tris-HCl buffer with pH=8.5. Make the final concentration of dopamine 0.2mg / mL. After the reaction was stirred for 24 hours in the dark under the condition of oxygen ventilation at room temperature, it was placed in a 3500Da dialysis bag, placed in pure water, and dialyzed against light to remove the unencapsulated doxorubicin, and the dopamine polymer carrier containing dopamine was obtained. Drug nanoparticles. Measured by fluorescence spectrophotometry, the drug loading of the nanoparticles was 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 biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing system. The nanometer transmitting and releasing system comprises dopamine polymerization drug-loading nanoparticles prepared from dopamine and anti-tumor drugs, and biomimetic tumor targeted protein or polypeptide grafted to the surface of polydopamine. The dopamine disclosed by the invention coats drugs in the polydopamine through a polymerization drug-loading way, drug encapsulation efficiency is obviously improved, and drug loading capacity ishigh. Then, biomimetic tumor targeted protein or polypeptide is covalently grafted to the surface of the polydopamine, and the nanometer transmitting and releasing system is endowed with biomimetic characteristics and targeted functions. The nanometer transmitting and releasing system prepared by the invention has pH, ROS and optothermal triple response quick drug-releasing characteristics, through tumor targeting, a purpose of tumor chemotherapy-optothermal combined treatment can be realized, and the biomimetic dopamine polymerization drug-loading nanometer transmitting and releasing systemhas a good application prospect on an aspect of tumor targeting combined treatment.

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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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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