Application of fluorescence arborization nanometer macromolecule in preparing drug carrier

A macromolecular and dendritic technology, applied in the field of drug carriers, can solve the problems of non-fluorescent properties, hindering entry into cells, and limiting the scope of application, etc., to achieve the effects of reducing cytotoxicity, enhancing drug efficacy, and expanding the scope of insecticide

Active Publication Date: 2015-07-22
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
  • Application of fluorescence arborization nanometer macromolecule in preparing drug carrier
  • 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 nano-macromolecule (G1-G3) drug carrier

[0048] Fluorescent functional dendritic nano-macromolecules (G1-G3) drug carriers are synthesized based on the literature reported by our group. Refer to the literature for specific experimental steps:

[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. The synthesis method and application of water-soluble fluorescent dendrimer, patent publication number: 103204999A.

[0051] The structural formula G1-G3 of fluorescent functional dendritic nano-macromolecules 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 Delivery Particles Based on Fluorescent Functional Dendritic Nano-macromolecules

[0054] The fluorescent functional dendritic nano-macromolecules of different generations (G1-G3) and thiamethoxam (see chemical structure) prepared in Example 1 were used respectively Figure 5 ) Preparation of compound drugs, see Image 6 ,Specific steps are as follows:

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

[0056] 1) Ultraviolet absorption spectrum test: The fluorescent functional dendritic nano-macromolecules (G1-G3) of different generations prepared in Example 1 were respectively prepared with deionized water to a concentration of 5μM solution, and thiamethoxam (concentration of 0 -400μM), the sample is subjected to UV absorption spectrum test. See Figure 7 , The UV absorption peak has no obvious change.

[0057] 2) Fluorescence emission spectrum te...

Embodiment 3

[0067] Example 3 Application of fluorescent functional dendritic nano-macromolecules as drug carriers

[0068] Mix the fluorescent functional dendritic nano-macromolecules G1-G3 with the drug thiamethoxam, and then co-incubate with the cells. Through the endocytosis of the cells, the drug-encapsulated dendritic compound carrier can enter the living cultured cells, or by feeding insects In this way, the dendritic compound carrier encapsulating the drug enters the insect cells.

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

[0070] 1. The toxicity of dendritic nano-macromolecules combined with drugs to cultured cells in vivo

[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 1:1-8...

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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 insecticides has led to insecticide resistance, and the residue of pesticides has 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 pesticides to pests, enhances the cytotoxicity of the pesticides, improves the insecticidal efficiency, and expands 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. Dendrimers have excellent structures such as precise and controllable nan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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