Preparation method and application of nano-pesticide dosage form using non-phospholipid liposome as carrier

A technology of nano-pesticides and liposomes, applied in botany equipment and methods, applications, fungicides, etc., can solve the problems of pesticide residues and environmental pollution, difficulty, and low effective utilization rate, and achieve saving of pesticide dosage, The effect of reducing the dosage and improving the sustained-release ability

Active Publication Date: 2021-09-24
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the above-mentioned known technical information exists in the prior art, how to apply non-phospholipid liposomes in the pesticide drug-carrying system remains to be developed. The effective utilization rate of the known traditional pesticide formulations is low, and the pesticide residues and environmental pollution are also serious. Very serious, water-based, dust-free, slow-controlled release, etc. have become the development direction of new pesticide formulations. As a nano-carrier, non-phospholipid liposomes have shown outstanding performance in environmental stability and slow-controlled release of drugs. Excellent performance, has been applied in the field of medicine
However, unlike the relatively controllable environment of the human body, in agricultural applications, facing an open and changeable environment, there are higher requirements for the environmental stability of the drug, and it is more difficult to deliver the drug to the target.

Method used

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  • Preparation method and application of nano-pesticide dosage form using non-phospholipid liposome as carrier
  • Preparation method and application of nano-pesticide dosage form using non-phospholipid liposome as carrier
  • Preparation method and application of nano-pesticide dosage form using non-phospholipid liposome as carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Preparation of cationic cholesterol stearylamine-loaded cyanamide liposomes. Penoxuron is an effective systemic fungicide used to control plant diseases such as cucumber downy mildew caused by fungal infections. It has poor stability and is easily degraded under alkaline and high temperature conditions. 100 mg of octadecylamine and 143.5 mg of cholesterol were weighed, dissolved in 6 mL of benzene / methanol (5.4 mL of benzene, 0.6 mL of methanol), and lyophilized overnight to remove the organic solvent. Add 20 mL of MES-Tris buffer pH=5.0 for hydration. The reaction conditions were freezing in liquid nitrogen for 1 minute, water bath at 70°C for 10 minutes, alternating cycles for 5 times, vortexing for 30 s during each cycle, and then placing in the ultrasonic breaker for 20 minutes, during the treatment period, the cycle was turned on for 20 s and closed for 5 s, and the amplitude was 40%. . Dissolve 20 mg of cyanamide cyanide in a trace amount of DMSO, add it to the ...

Embodiment 2

[0049] Preparation of cationic cholesterol-stearylamine-loaded thiamethoxam liposomes. Thiamethoxam is a highly effective neonicotinoid insecticide with good water solubility. Weigh 100 mg of octadecylamine and 143.5 mg of cholesterol, dissolve in 6 mL of benzene / methanol (5.4 mL of benzene, 0.6 mL of methanol), freeze-dry overnight for 16 hours to remove the organic solvent. The original drug of thiamethoxam was dissolved in 20 mL of MES-NaCl buffer solution with pH=7.4 at a concentration of 1 mg / mL, and lyophilized cholesterol stearylamine powder was added for hydration. The reaction conditions are liquid nitrogen freezing for 1 minute, 70°C water bath for 10 minutes, and alternating cycles of 5 times. During each cycle, vortex oscillation for 30 seconds, and then placed in an ultrasonic breaker for 20 minutes. , to obtain cationic cholesterol octadecylamine-loaded thiamethoxam liposomes. Its drug loading is 8.97%.

[0050] Figure 7 It is the SEM picture of the cationic...

Embodiment 3

[0056] Preparation of cationic cholesterol-stearylamine-loaded sulfoxaflor liposomes. Sulfoxaflor is a new sulfonylimide insecticide for the control of sap-sucking pests, with low water solubility. Weigh 100 mg of octadecylamine, 143.5 mg of cholesterol, and 20 mg of sulfoxaflor, dissolve in 6 mL of benzene / methanol (5.4 mL of benzene, 0.6 mL of methanol), and freeze-dry overnight to remove the organic solvent. Add 20 mL of MES-Tris buffer solution with pH=5.0 for hydration. The reaction conditions are liquid nitrogen freezing for 1 minute, 70°C water bath for 10 minutes, and alternating cycle 5 times. , 20s on and 5s off cycle during processing, amplitude 40%. The cationic cholesterol-stearylamine-loaded sulfoxaflor liposome is obtained, and the drug-loading amount is 7%-10%.

[0057] Figure 9 It is the SEM image of the cationic cholesterol octadecylamine-loaded sulfoxaflor liposome prepared in Example 3; the analysis shows that the powder obtained after the liposome solu...

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Abstract

The present invention provides a nanoscale non-phospholipid liposome as an ideal drug carrier, the preparation method and application in the application of pesticide nano dosage forms, the method utilizes sterol compounds and single-chain alkylated amphiphilic compounds The self-assembly behavior in the buffer solution forms a nanodispersant with uniform size and high stability, which can have different charge properties and pH response functions. According to the differences in hydrophilicity, hydrophobicity, molecular weight, and stability of pesticide molecules, drugs are loaded on liposomes in different drug-loading methods, so as to improve drug stability, improve drug release performance, and enhance drug effects. The present invention uses non-phospholipid liposomes combined with pesticide molecules to prepare pesticide nano dosage forms, which can not only improve drug sustained-release ability, but also have environmental response performance, which is suitable for controlled release in different environments and has good drug stability, The slow and controlled release effect and biological safety have broad application prospects.

Description

technical field [0001] The invention belongs to the technical field of pesticide preparation, and in particular relates to a preparation method and application of a nano-pesticide dosage form using non-phospholipid liposomes as a carrier. Background technique [0002] The liquid product synthesized from the pesticide raw material is crude oil, and the solid product is the original powder, which are collectively referred to as the original drug. Most pesticide technical drugs cannot be used directly due to their high physicochemical properties and high content of active ingredients. In practice, they need to be processed into different formulations. Traditional pesticide formulations include emulsions, emulsifiable concentrates, powders, wettable powders, water preparations, suspensions, etc., which have disadvantages such as high content of organic components, poor dispersibility, and dust drift. To 1% of pesticide residues on target crops, this inefficient way of drug acti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N25/08A01N25/22A01N47/34A01N51/00A01N47/40A01N57/16A01P3/00A01P1/00A01P7/04A01P13/00
CPCA01N25/08A01N25/22A01N47/34A01N47/40A01N51/00A01N57/16
Inventor 崔忠凯杨青杨君张正黄志勇
Owner DALIAN UNIV OF TECH
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