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Application of fluorescence arborization nanometer macromolecule in preparing drug carrier

A technology for preparing drugs and dendrites, which is applied in the field of drug carriers, can solve the problems of not having fluorescence characteristics, limiting the scope of application, and hindering entry into cells, so as to achieve the effects of reducing cytotoxicity, expanding the scope of insecticide, and enhancing drug efficacy

Active Publication Date: 2014-08-27
CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, most insecticides are hydrophobic and have poor water solubility in physiological environment, which hinders their entry into cells, resulting in low insecticidal efficiency
Usually some organic solvents (such as dimethyl sulfoxide, DMSO) are used to dissolve insecticides to improve their water solubility, but these organic solvents often have high cytotoxicity
In addition, although the dendritic drug carriers studied in the past have good water solubility and biocompatibility, they do not have fluorescent properties, which limits their application to a certain extent.

Method used

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  • Application of fluorescence arborization nanometer macromolecule in preparing drug carrier
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  • Application of fluorescence arborization nanometer macromolecule in preparing drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Preparation of Fluorescent Functional Dendritic Nanomacromolecule (G1-G3) Drug Carrier

[0048] The fluorescent functional dendritic nano-macromolecule (G1-G3) drug carrier was synthesized based on the literature reported by our research group. Specific experimental steps refer to the literature:

[0049] 1. Xu Z, He B, Shen J, et al. Fluorescent water-soluble perylenediimide-cored cationic dendrimers: synthesis, optical properties, and cell uptake[J].Chem.Commun.,2013,49(35):3646- 3648;

[0050] 2. Synthesis method and application of water-soluble fluorescent dendrimers, patent publication number: 103204999A.

[0051] Fluorescent functional dendritic nano-macromolecular structural formula G1-G3 prepared by the above method, see Figure 1-3 .

[0052] There are many structures of PDI and fluorescent nuclear analogs that can replace PDI, see Figure 4 .

Embodiment 2

[0053] Example 2 Construction and Characterization of Fluorescent Functional Dendritic Nanomacromolecule Delivery Particles

[0054]Fluorescent functional dendritic nano-macromolecules (G1-G3) and thiamethoxam of different generations prepared in Example 1 (chemical structural formula see Figure 5 ) to prepare compound drugs, see Image 6 ,Specific steps are as follows:

[0055] 1. The loading capacity of fluorescent functional dendritic nano-macromolecules (G1-G3) of different generations on thiamethoxam

[0056] 1) Ultraviolet absorption spectrum test: The fluorescent functional dendritic nano-macromolecules (G1-G3) of different generations prepared in Example 1 were respectively prepared into solutions with a concentration of 5 μM with deionized water, and thiamethoxam (concentration of 0 -400μM), the sample was tested by UV absorption spectrum. see Figure 7 , the UV absorption peak did not change significantly.

[0057] 2) Fluorescence emission spectrum test: The sa...

Embodiment 3

[0067] Example 3 Application of Fluorescent Functional Dendritic Nanomacromolecule as Drug Carrier

[0068] The fluorescent functional dendritic nano-macromolecules G1-G3 are mixed with the drug thiamethoxam, and then co-incubated with the cells, and the drug-encapsulated dendrimer carrier enters the living culture cells through the endocytosis of the cells, or by feeding insects The method is to make the drug-coated dendrimer carrier enter the insect body cells.

[0069] Specifically, fluorescent functional dendritic nanomacromolecules are used as drug carriers and applied to living cultured cells and living insects:

[0070] 1. Toxicity of dendritic nano-macromolecules combined with drugs on living cultured cells

[0071] The drug thiamethoxam was mixed with the fluorescent functional dendritic nano-macromolecule G1-G3 compound prepared in Example 1 at different concentrations, the molar ratio of the fluorescent dendritic nano-macromolecule to the drug was 1:1-80, and then ...

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Abstract

The invention provides application of fluorescence arborization nanometer macromolecule in preparing a drug carrier, application of the fluorescence arborization nanometer macromolecule in preparing a compound drug and the compound drug made of the drug carrier and a hydrophobic drug in a mixing mode, and further provides application of the compound drug in pest control. Pests are fed with the compound drug in a feeding or injecting mode, the arborization compound can serve as the drug carrier to package the drug to enter the cells of the pests quickly, the drug can play a role in the pests, the pesticide effect is enhanced, and non-target pests are effectively killed. The new strategy that the fluorescence arborization nanometer macromolecule serves as the pesticide carrier to be applied in the field of pest control is achieved successfully. The pesticide effect of the pesticide is enhanced through the application, the pest killing range is enlarged, and a new approach for avoiding overusing of chemical pesticide is provided. The fluorescence arborization nanometer macromolecule has very high application value in the fields of agricultural pest control and biology scientific research.

Description

technical field [0001] The invention relates to the field of drug carriers, in particular to the application of a water-soluble fluorescent dendritic nano-macromolecule as a drug carrier in the field of pest control. Background technique [0002] In recent decades, the excessive use of pesticides has led to the resistance of pests, and the residues of pesticides have caused a series of environmental problems, posing a great threat to the health and safety of humans and animals. Therefore, exploring a new method in the field of pest control, using drug carriers to deliver insecticides to pests, enhancing the cytotoxicity of insecticides, improving insecticidal efficiency, and expanding the scope of insecticide has attracted the attention of researchers. In recent years, some nanocarriers, such as polymeric nanoparticles, liposomes, and dendrimers, have begun to be used in the research field of drug delivery. Due to the precise and controllable nanostructure, low dispersion, ...

Claims

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Application Information

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IPC IPC(8): A01N25/10A01N51/00A01P7/04C09K11/06
Inventor 沈杰尹梅贞何碧程许泽军
Owner CHINA AGRI UNIV
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