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A kind of camptothecin-abamectin silica nanoparticle and its preparation method and application

A technology of abamectin and silicon dioxide, applied in the direction of botany equipment and methods, applications, pesticides, etc., can solve the problems of fast release of active ingredients, short duration of drug effect, environmental pollution, etc.

Inactive Publication Date: 2017-09-29
LANZHOU JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the general utilization rate of conventional pesticide formulations is only 20% to 30%, and the loss rate in the process of releasing to the target is 50% to 60% (Yang Lei, et al. Pesticide Science and Management, 2009, 30: 36-39)
The conventional dosage forms of pesticides have the disadvantages of fast release of active ingredients, short duration of drug effect, and large dosage, which are not only economically wasteful, but also cause environmental pollution.

Method used

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  • A kind of camptothecin-abamectin silica nanoparticle and its preparation method and application
  • A kind of camptothecin-abamectin silica nanoparticle and its preparation method and application
  • A kind of camptothecin-abamectin silica nanoparticle and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: CPT-mPEG 500 and AVM-mPEG 500 Synthesis of Derivatives

[0018] 1) CPT-mPEG 500 Synthesis of Derivative (3)

[0019]

[0020] Formula 1

[0021] Under nitrogen protection, add 5 g of mPEG to a 100 mL round bottom flask 500 (Polyethylene glycol monomethyl ether) (10 mmol) was dissolved with stirring in 50 mL of dry dichloromethane, then 5 g of succinic anhydride (50 mmol) and 4 mL of dry pyridine (50 mmol) were added, heated to 40° C. and refluxed for three days. After the reflux is completed, cool to room temperature, spin dry under reduced pressure, add an appropriate amount of distilled water to dissolve, and wash with ethyl acetate / n-hexane (1:1) for several times. The aqueous phase was extracted three times with chloroform, and the extracts were combined, dried over anhydrous magnesium sulfate overnight, filtered, and concentrated by distillation under reduced pressure to obtain mPEG. 500 -COOH(2).

[0022] Add mPEG to 100mL round bottom flask ...

Embodiment 2

[0027] Embodiment 2: the silicon dioxide nanoparticle (CPT-mPEG of loading camptothecin and abamectin 500 / AVM-mPEG 500 / CTAB@MSN) preparation and characterization

[0028] 1) CPT-mPEG 500 / AVM-mPEG 500 Preparation of / CTAB@MSN

[0029] Add 50mg CPT-mPEG to a 100mL round bottom flask 500 and 50mg AVM-mPEG 500 , dissolved in 30mL of deionized water, and continued to stir for 1 hour after dissolution. Added 200mg of CTAB and 2mL of triethylamine to the mixed system, and continued to stir for 2 hours after dissolution. Then 600 mg of TEOS was added dropwise, and after the addition was completed, the mixture was stirred at room temperature for 24 h. A pale yellow precipitate formed. Centrifuge (9000r / min, 10min) and vacuum dry to obtain a yellow solid powder.

[0030] 2) Drug loading test

[0031] Collect CPT-mPEG 500 / AVM-mPEG 500 / CTAB@MSN solution after centrifugation, based on the characteristic absorption peaks of camptothecin and abamectin at 365 and 252nm UV, res...

Embodiment 3

[0052] Embodiment 3: biological activity test

[0053] 1) Test insects:

[0054] 1) Tetranychus cinnabarinus: collected from soybean seedlings in the field of Gansu Academy of Agricultural Sciences, cultivated in the laboratory under the condition of artificial climate chamber [(25±1)℃, H / D 12:12], and set aside.

[0055] 2) Diamondback moth (Plutella xyllostella): The tested insects were the 3rd instar larvae of diamondback moth. A strain of subculture of rock cabbage seedlings.

[0056] Two) test agent (Table 5)

[0057] Table 5 Test agents and control pesticides

[0058]

[0059] 3) Activity determination:

[0060] 1) Determination of poisonous activity against Tetranychus cinnabarinus:

[0061] Determination by slide dipping method (Wang Y.J., et al. Agrochemicals Research & Application, 2006, 10:20-23). Dissolve 10 mg of compound No. 1 (the actual content of CPT) and compound No. 3 in 10 mL of acetone, and 10 mg of compound No. 2 in 10 mL of DMSO (heating to aid ...

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Abstract

The invention discloses a novel camptothecin-abamectin silica nanoparticle inclusion drug, its preparation method and its use in the preparation of pesticides. The preparation method of Camptothecin-Avermectin silica nanoparticles of the present invention is: first prepare mPEG500-COOH (2), then prepare the crude product, then 350mg Abamectin, mPEG500-COOH and 4- Dimethylaminopyridine (DMAP) is dissolved and stirred with dichloromethane and then added dicyclohexylcarbodiimide (DCC), finally obtaining a light yellow oily matter-camptothecin-abamectin silica nanoparticles AVM ‑mPEG500. The camptothecin-abamectin silica nanoparticles prepared by the method of the present invention can be used in pesticides, such as for killing crop pests such as Tetranychus cinnabarinus or diamondback moth.

Description

technical field [0001] The invention relates to a novel camptothecin-avermectin silica nanoparticle inclusion medicine, as well as its preparation method and its use in the preparation of pesticides. Background technique [0002] The promotion of pesticides is of great significance to agricultural production, and is also an indispensable industry in my country's national economy. Pesticides can generally be divided into chemical pesticides and biological pesticides. At present, chemical pesticides are the most used in my country. However, chemical pesticides are highly toxic and increasingly pollute the environment, and due to long-term, single use or abuse of pesticides, it is easy for pests to develop drug resistance, and even develop cross-resistance and multi-resistance (Hilder V.A., et al. .Crop Protection, 1999, 18:177-191). According to statistics, in the 100 years from 1910 to 2010, the number of drug-resistant pests has increased from one species to more than 600 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N43/90A01N25/18A01N25/22A01P7/02A01P7/04
Inventor 杨柳
Owner LANZHOU JIAOTONG UNIV
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