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Camptothecin-avermectin silica nanoparticle, and preparation method and application thereof

A technology of abamectin and nano-particles, applied in the fields of botanical equipment and methods, applications, pesticides, etc., can solve the problems of environmental pollution, fast release of active ingredients, and short duration of drug effect.

Inactive Publication Date: 2016-02-24
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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  • Camptothecin-avermectin silica nanoparticle, and preparation method and application thereof
  • Camptothecin-avermectin silica nanoparticle, and preparation method and application thereof
  • Camptothecin-avermectin silica nanoparticle, and preparation method and application thereof

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 5gmPEG to a 100mL round bottom flask 500 (Polyethylene glycol monomethyl ether) (10mmol), stirred and dissolved with 50mL of dry dichloromethane, then added 5g of succinic anhydride (50mmol), 4mL of dry pyridine (50mmol), heated to 40°C, and refluxed for three days. After the reflux is completed, cool to room temperature, distill and spin dry under reduced pressure, add an appropriate amount of distilled water to dissolve, and wash several times with ethyl acetate / n-hexane (1:1). The aqueous phase was extracted 3 times with chloroform, and the extracts were combined, dried over anhydrous magnesium sulfate, filtered, concentrated by distillation under reduced pressure to obtain mPEG 500 -COOH(2).

[0022] Add mPEG to a 100mL round bottom flask 500-COOH (1 mmol), stirred and di...

Embodiment 2

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

[0028] 1) CPT-mPEG 500 / AVM-mPEG 500 Preparation of / CTABMSN

[0029] Add 50mg of CPT-mPEG to a 100mL round bottom flask 500 and 50mg AVM-mPEG 500 , dissolve in 30mL deionized water, continue to stir for 1h after dissolving, add 200mgCTAB and 2mL triethylamine to the mixed system, and continue stirring for 2h after dissolving. Then 600 mg of TEOS was added dropwise, and after the addition was completed, it 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 / CTABMSN solution after centrifugation, based on the characteristic absorption peaks of camptothecin and avermectin at 365 and 252nm UV, respectively, to make CPT-mPEG 500 and ...

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)°C, H / D12:12], and set aside.

[0055] 2) Plutella xylostella (Plutella xyllostella): The tested insects are the 3rd instar larvae of Plutella xylostella. Under the conditions of artificial climate chamber [(26±1)℃, RH(70±5)%, H / D14], the modified vermiculite A strain of subcultured cabbage seedlings.

[0056] Two) test agent (table 5)

[0057] Table 5 test agent and contrast pesticide

[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 No. 1 compound 10mg (the actual content of CPT) and...

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Abstract

The invention discloses a novel camptothecin-avermectin silica nanoparticle clathrate medicine and a preparation method thereof, and application of the medicine in preparation of pesticide. The preparation method for the camptothecin-avermectin silica nanoparticle comprises the following steps: preparing mPEG500-COOH(2); then preparing a crude product; and dissolving 350 mg of avermectin, mPEG500-COOH and 4-dimethylaminopyridine (DMAP) with dichloromethane, carrying out stirring and then adding dicyclohexylcarbodiimide (DCC) so as to eventually obtain a light yellow oily matter, i.e., the camptothecin-avermectin silica nanoparticle AVM-mPEG500. The camptothecin-avermectin silica nanoparticle prepared by using the method can be applied to pesticide for, e.g., killing crop insects like Tetranychus cinnabarinus or diamondback moth.

Description

technical field [0001] The invention relates to a novel camptothecin-abamectin silica nano particle inclusion drug, 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 it 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, the toxicity of chemical pesticides is high, and the environmental pollution is also becoming more and more serious. Moreover, due to long-term, single use or abuse of pesticides, it is very easy for pests to develop resistance to pesticides, and even develop cross-resistance and multiple resistance (HilderV.A., et al. Crop Protection, 1999, 18:177-191). According to statistics, during the century from 1910 to 2010, the number of drug-resistant pests...

Claims

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Application Information

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IPC IPC(8): A01N43/90A01N25/18A01N25/22A01P7/02A01P7/04
Inventor 杨柳
Owner LANZHOU JIAOTONG UNIV
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