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Salbutamol modified guanidinated chitosan and preparation method and application thereof

A technology of albuterol and chitosan, which is applied in gene therapy, pharmaceutical formulations, respiratory diseases, etc., can solve the problems of low transfection efficiency of chitosan and poor cell targeting, so as to reduce the stimulation of tissues and cells, Overcoming insoluble and improving transfection efficiency

Inactive Publication Date: 2011-08-31
TIANJIN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, like other non-viral vectors, chitosan has low transfection efficiency and poor cell targeting, and needs to be modified to improve its transfection efficiency and specificity

Method used

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  • Salbutamol modified guanidinated chitosan and preparation method and application thereof
  • Salbutamol modified guanidinated chitosan and preparation method and application thereof
  • Salbutamol modified guanidinated chitosan and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 0.1M HCl (150ml) into the beaker, add chitosan (Mw=50kDa, 0.161g, 1mmol), then stir and heat to 80°C, stop heating after the chitosan is completely dissolved, and cool to room temperature. Add 2M NaOH solution (150ml, excess), immediately produce a large amount of white flocculent precipitate, centrifuge at 10000r / min for 5min, and pour off the supernatant. The chitosan white colloidal precipitate after lye treatment is obtained.

[0026] Dissolve albuterol sulfate (0.288g, 1mmol) in DMSO (20ml) into a three-neck flask, then add epichlorohydrin (78.3μl, 1mmol) dropwise and stir until uniform. 1M NaOH (20ml) was quickly added and reacted at room temperature for 4.5h.

[0027] Add chitosan treated with lye, and continue to react for 4.5h. The reaction solution was diluted with water and dialyzed in deionized water for 5 days (dialysis bag molecular weight cut-off 3500), changing the water every 8 hours, and then lyophilized to obtain albuterol-modified chitosan.

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Embodiment 2

[0031] Weigh thiourea dioxide (10.8g, 0.1mol), take a small amount and add it to a three-necked flask, measure hydrogen peroxide (30%, 0.15mol, 17ml) and concentrated sulfuric acid (98%, 34ml) and mix them in proportion in a small beaker first, and prepare into hydrogen peroxide acidic solution. After cooling to room temperature, the mixed solution was added to a constant pressure dropping funnel. Control the temperature in the reactor at 50-60°C, slowly add hydrogen peroxide acidic solution dropwise while stirring, and at the same time add thiourea dioxide in small amounts, finish feeding within 1 hour, continue to react for 40 minutes, stop heating, pour the reaction solution into a beaker, Cool at 4°C for 2h. Excessive ethanol was added to the reaction solution to generate granular white crystals. The precipitate was collected by filtration, dissolved in a small amount of water, and recrystallized by adding excess ethanol. Repeat this three times. Finally, wash with abs...

Embodiment 3

[0037] Weigh thiourea dioxide (10.8g, 0.1mol), take a small amount and add it to a three-necked flask, measure hydrogen peroxide (30%, 0.15mol, 17ml) and concentrated sulfuric acid (98%, 34ml) and mix them in proportion in a small beaker first, and prepare into hydrogen peroxide acidic solution. After cooling to room temperature, the mixed solution was added to a constant pressure dropping funnel. Control the temperature in the reactor at 50-60°C, slowly add hydrogen peroxide acidic solution dropwise while stirring, and at the same time add thiourea dioxide in small amounts, finish feeding within 1 hour, continue to react for 40 minutes, stop heating, pour the reaction solution into a beaker, Cool at 4°C for 2h. Excessive ethanol was added to the reaction solution to generate granular white crystals. The precipitate was collected by filtration, dissolved in a small amount of water, and recrystallized by adding excess ethanol. Repeat this three times. Finally, wash with abs...

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Abstract

The invention relates to salbutamol modified guanidinated chitosan and a preparation method and application thereof. A method for double modifying of the guanido for promoting carrier transmembrane and the salbutamol with the targeted property is adopted; the salbutamol is coupled to the chitosan molecule through epoxy chloropropane; and then guanidination is performed on chitosan amino by using thiourea trioxide. The original chitosan carrier is modified to improve the transfection efficiency and the targeted property to respiratory cells. A synthesizing method is simple and convenient and the condition is mild; the transfection efficiency of the modified chitosan serving as a gene vector is improved obviously than that of the unmodified chitosan; and the modified chitosan has the potential practical value of respiratory diseases, particularly gene therapy of asthma.

Description

technical field [0001] The invention relates to a salbutamol-modified guanidinylated chitosan, a preparation method and application thereof, which can be used as a high-efficiency targeting non-viral gene carrier in gene therapy. Background technique [0002] The choice of vector system directly affects the efficiency and safety of gene therapy. Commonly used gene delivery methods are mainly divided into two categories, namely viral vectors and non-viral vector introduction techniques. Viral vectors have high transfection efficiency and are currently the main tool for in vivo gene therapy. Although viral vectors have high transfection efficiency, they have safety risks such as low gene carrying capacity, immunogenicity and potential tumorigenicity. Non-viral vectors provide another way for gene delivery. At present, non-viral vectors mainly include liposomes and cationic polymers. However, due to the lack of the natural gene delivery mechanism of viral vectors, the effici...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/08A61K48/00A61P11/06
Inventor 刘文广孙鹏徐军罗永峰
Owner TIANJIN UNIV
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