Dual-modified chitosan drug-loaded nano-micelle as well as preparation method and application thereof

A drug-loaded nano-carboxymethyl chitosan technology, applied in the direction of botanical equipment and methods, applications, biocides, etc., can solve the problems of complicated experimental process and cumbersome steps, and achieve uniform particle size distribution and good insecticide The effect of activity and larval refusal rate reduction

Active Publication Date: 2022-08-09
SOUTH SUBTROPICAL CROPS RES INST CHINESE ACAD OF TROPICAL AGRI SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above technologies all use chitosan derivatives as wall materials to prepare controlled-release nano-drug-loaded particles, most of them use chemical cross-linking methods to prepare micro-nanocapsules, and the experimental process is complicated and the steps are cumbersome.

Method used

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  • Dual-modified chitosan drug-loaded nano-micelle as well as preparation method and application thereof
  • Dual-modified chitosan drug-loaded nano-micelle as well as preparation method and application thereof
  • Dual-modified chitosan drug-loaded nano-micelle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0056] 4. The present invention discloses a preparation method of a drug-loaded nanomicelle, comprising the following steps:

[0057] (1) Dissolve carboxymethyl chitosan vegetable oil-based derivative in deionized water, and obtain a transparent blank nanomicellar aqueous solution after ultrasonic treatment; the output power of ultrasonic treatment is 100W ~ 250W, and intermittent pulse working mode: pulse width 2.0~3s, intermittent time 2.0~5s;

[0058] (2) dissolving the original pesticide solution in an organic solvent to obtain a pesticide solution;

[0059] (3) adding the pesticide solution of step (2) to the blank nanomicellar aqueous solution of step (1) to form a mixed solution, then stirring at a rate of 100-300 r / min for 2-4 hours, and dialyzing for 10-24 hours to remove the organic solvent , the molecular weight cut-off of dialysis is 3000; ultrasonic treatment is 5 ~ 10min, ultrasonic treatment output power is 100 ~ 250W, intermittent pulse working mode: pulse wid...

Embodiment 1

[0064] Alpha-linolenic acid (ALA) was selected as the vegetable oleic acid with a molecular weight of 278, and the bisamino compound was selected as urea with a molecular weight of 46. Carboxymethyl chitosan (CMCS, viscosity average molecular weight is 3.0×10 3 ~2.0×10 5 , the degree of deacetylation ≥ 90%, the degree of carboxymethylation ≥ 80%), α-linolenic acid (ALA) were purchased from Shanghai McLean Biochemical Co., Ltd. 1-Ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC), N-hydroxysuccinimide (NHS) were purchased from Shanghai Aladdin Reagent Co., Ltd. Ethanol and urea were provided by Tianjin Fuyu Fine Chemical Co., Ltd.; clothianidin was purchased from Shanghai Yuanye Biotechnology Co., Ltd.

[0065] The synthetic process of carboxymethyl chitosan vegetable oil-based derivatives is as follows:

[0066]

[0067] 1. The preparation process of carboxymethyl chitosan vegetable oil-based derivative, comprising the following steps:

[0068] 1. Preparatio...

Embodiment 2

[0090] Example 2 is the relevant performance test of the drug-loaded nanomicelles prepared in Example 1

[0091] 1. Structure and performance characterization of the prepared copolymer CTD@U-CMCS-g-ALA:

[0092] (1) Structural characterization of the copolymer: The functional groups of the copolymer were characterized by Fourier transform infrared spectroscopy (FT-IR) on a Nexus 670 from Thermo Fisher Scientific, and the spectral scanning range was 400-4000 cm. -1 . The samples were analyzed by hydrogen spectrum using Bruker's AV600 nuclear magnetic resonance spectrometer. Tetramethylsilane (TMS) was used as the internal standard and heavy water was used as the sample solvent to identify the structure of the copolymer.

[0093] The result is as image 3 shown, in the spectrum of ALA(a), 3013 cm -1 is -CH=CH- stretching vibration absorption peak, 2926cm -1 , 2852cm -1 Linolenic acid linear medium methylene CH 2 Asymmetric stretching vibration and symmetric stretching vibr...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to a dual-modified chitosan drug-loaded nano-micelle as well as a preparation method and application thereof. According to the specific technical scheme, the carboxymethyl chitosan derivative is prepared by grafting a hydrophobic group vegetable oleic acid and a hydrophilic group diamino compound onto carboxymethyl chitosan through an acylation reaction. The dual-modified chitosan drug-loaded nano-micelle provided by the invention can effectively inhibit the growth and development of sugarcane borers, and has certain insecticidal performance.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a double-modified chitosan drug-loaded nanomicelle, a preparation method and an application. Background technique [0002] Sugarcane borers are the most widely distributed and most serious pests in sugarcane areas in my country. They all use larvae to bore into sugarcane seedlings and stem tissue, causing dead seedlings and stem borers to damage nodes, thereby reducing sugarcane sugar content and yield. In recent years, its occurrence has shown the characteristics of explosive and perennial occurrence, which poses a great threat to the sugarcane industry. In recent years, some progress has been made in the application of nanomaterials and technologies in the agricultural field. Using nanoscience and technology to develop efficient and safe new formulations of pesticides, improve the biological activity and target utilization of medicinal components, and extend...

Claims

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Application Information

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IPC IPC(8): C08B37/08A01N25/28A01N51/00A01N43/36A01P7/04
CPCC08B37/003A01N25/28A01N51/00A01N43/36Y02A50/30
Inventor 周闯张利李普旺杨子明屈云慧于丽娟何祖宇王超刘运浩宋书会
Owner SOUTH SUBTROPICAL CROPS RES INST CHINESE ACAD OF TROPICAL AGRI SCI
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