Folic acid-chitosan-nanometer selenium tumor targeted drug delivery system and preparation method thereof

A tumor targeting and chitosan technology, applied in the field of targeted nanometers, can solve the problems of unstable properties of nanometer selenium

Inactive Publication Date: 2020-06-02
JIANGSU FOOD & PHARMA SCI COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the nature of nano-selenium is unstable, and it is easy to convert into gray or black elemental selenium that is thermally stable but active and passivated.

Method used

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  • Folic acid-chitosan-nanometer selenium tumor targeted drug delivery system and preparation method thereof
  • Folic acid-chitosan-nanometer selenium tumor targeted drug delivery system and preparation method thereof
  • Folic acid-chitosan-nanometer selenium tumor targeted drug delivery system and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: prepare folic acid-chitosan-nano selenium according to the following steps

[0021] (a) Activation of folic acid (FA): Accurately weigh 1.0 g of folic acid and dissolve in 60 mL of dimethyl sulfoxide, stir at room temperature to dissolve completely, add 0.28 g of N-hydroxysuccinimide (NHS) and 0.8 g of carbonized Mix diimine hydrochloride (EDC·HCl) evenly, then add 6.0 mL of triethylamine, place it at room temperature, and react in the dark for 24 hours to obtain activated folic acid;

[0022] (b) Construction of folic acid-chitosan (FA-CS) system: weigh chitosan and dissolve it in 1% acetic acid solution to prepare 10% chitosan stock solution; the prepared chitosan stock solution Slowly drop the solution into the activated folic acid prepared in step (a), place it in a water bath at 50°C for 24 hours, and adjust the pH of the system to 9.0 to terminate the reaction; wherein, the mass ratio of activated folic acid to chitosan is 1.5:1 , the above process ...

Embodiment 2

[0028] Embodiment 2: prepare folic acid-chitosan-nano selenium according to the following steps

[0029] (a) Activation of folic acid (FA): Accurately weigh 1.5 g of folic acid and dissolve in 100 mL of dimethyl sulfoxide, stir at room temperature to dissolve completely, add 0.3 g of N-hydroxysuccinimide (NHS) and 0.8 g of carbonized Mix diimine hydrochloride (EDC·HCl) evenly, then add 8 mL of triethylamine, place it at room temperature, and react in the dark for 48 hours to obtain activated folic acid;

[0030] (b) Construction of folic acid-chitosan (FA-CS) system: Chitosan was weighed and dissolved in 1% acetic acid solution to prepare a chitosan stock solution with a mass concentration of 5%; the prepared chitosan Slowly drip the stock solution into the activated folic acid prepared in step (a), place it in a 40°C water bath for 12 hours, adjust the pH of the system to 9.0 to terminate the reaction; wherein, the mass ratio of activated folic acid to chitosan is 1 : 1, the...

Embodiment 3

[0034] Embodiment 3: prepare folic acid-chitosan-nano selenium according to the following steps

[0035] (a) Activation of folic acid (FA): Accurately weigh 2.0 g of folic acid and dissolve in 120 mL of dimethyl sulfoxide, stir at room temperature to dissolve completely, add 0.4 g of N-hydroxysuccinimide (NHS) and 1.2 g of carbonized Mix diimine hydrochloride (EDC·HCl) evenly, then add 10 mL of triethylamine, place it at room temperature, and react in the dark for 48 hours to obtain activated folic acid;

[0036] (b) Construction of folic acid-chitosan (FA-CS) system: Chitosan was weighed and dissolved in 1% acetic acid solution to prepare a chitosan stock solution with a mass concentration of 15%; the prepared chitosan Slowly drip the stock solution into the activated folic acid prepared in step (a), place it in a 70°C water bath for 48 hours, and adjust the pH of the system to 9.0 to terminate the reaction; wherein, the mass ratio of activated folic acid to chitosan is 2: 1...

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Abstract

The invention discloses a folic acid-chitosan-nanometer selenium tumor targeted drug delivery system and a preparation method thereof. The targeted drug delivery system is composed of folic acid, chitosan and nanometer selenium. Through activation the folic acid, the folic acid and the chitosan are combined to serve as a stabilizer and a coating agent, and then combined with the nanometer seleniumto form the folic acid-chitosan-nanometer selenium tumor targeted drug delivery system with a tumor targeting effect. The targeted drug delivery system prepared by using the preparation method provided by the invention is small in average particle size, uniform in particle size distribution and stable in properties; and the method is easy to be implemented, easy to operate and high in repeatability.

Description

technical field [0001] The invention relates to the field of targeting nanotechnology, in particular to a folic acid-chitosan-nano selenium tumor targeting drug delivery system and a preparation method thereof. Background technique [0002] According to statistics from the National Cancer Center, there are more than 3.5 million new cases of malignant tumors in my country every year, and more than 2 million deaths. Among them, lung cancer, breast cancer, and gastric cancer are the most common malignant tumors. With the in-depth study of tumor molecular mechanisms, tumor receptors have attracted widespread attention. Folate receptors are highly conserved in normal cells, but highly expressed in most malignant tumor cells. Using folate receptors for tumor targeting therapy is an effective means. Under physiological conditions, the solubility of antitumor drugs in aqueous solution is low, and the direct coupling of folic acid to drug molecules will further reduce the solubility...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/22A61K33/04A61P35/00
CPCA61K9/5123A61K9/5161A61K33/04A61P35/00
Inventor 东方张玲李冉冯锋王伟伟李岱曦向琼严平平
Owner JIANGSU FOOD & PHARMA SCI COLLEGE
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