Folic acid functionalized drug-loaded mesoporous silica and preparation method thereof

A mesoporous silicon oxide and mesoporous technology, which is applied in the direction of silicon oxide, silicon dioxide, pharmaceutical formulations, etc., can solve problems such as drug leakage, achieve short reaction time, easy operation, and avoid early leakage effects

Inactive Publication Date: 2012-12-05
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a common problem is that due to the opening at both ends of the pore, early leakage of the drug occurs before reaching the specific location

Method used

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  • Folic acid functionalized drug-loaded mesoporous silica and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0024] Example 1. Preparation of folic acid-functionalized drug-loaded mesoporous silica nano-drug carrier material

[0025] 1. Prepare mercapto-modified mesoporous silica by following methods of co-condensation and post-synthesis grafting:

[0026] a) Co-condensation method: put 1g of n-hexadecylammonium bromide (2.8mmol) in a round bottom flask, add deionized water (480mL, 26.7mol) and stir vigorously, add 2M sodium hydroxide (3.5mL, 0.175mmol) to adjust the pH to 11. A mixture of 5 mL tetraethylorthosilicate (22.4 mmol) and 0.97 mL mercaptopropyltrimethoxysilane (5.24 mmol) was added at a temperature of 80° C., and stirring was continued for 2 hours under nitrogen protection. After cooling, the reaction solution was centrifuged to obtain a white gel, which was washed several times with deionized water and ethanol, and dried in vacuum to obtain mercapto-modified mesoporous silica.

[0027] b) Post-synthesis grafting method: put 0.9 g of mercapto-modified mesoporous silica ...

Embodiment 2

[0032] Embodiment 2 drug release test in vitro:

[0033]At 37°C, 1.5 mg of F-MS-F obtained in Example 1 was dispersed in 3 mL of PBS buffer solution, 3.0 mg of DTT (6.5 mM) was added, and a F-2500 fluorescence spectrophotometer (HITACHI, Japan) was used to monitor 515 nm the fluorescence intensity at . Excitation wavelength: 504nm, slit: 2.5nm.

[0034] The reducing agent DTT was not added to the solution of the control group, and the reducing agent DTT of different concentrations was added to the solution of the experimental group. The release curve is drawn with time as the abscissa and cumulative release concentration as the ordinate. From figure 1 It can be seen that the control group did not add DTT, the disulfide bond did not break, the pores were blocked by folic acid, and the model drug was almost not released; while in the experimental group, the drug release rate was uniform due to the addition of DTT, the break of the disulfide bond Faster than the control group...

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Abstract

The invention discloses folic acid-functionalized drug-loaded mesoporous silica and a preparation method thereof. The folic acid-functionalized drug-loaded mesoporous silica of the present invention is prepared according to the following steps: 1) adopting orthosilicate as a silicon source, adopting an n-hexadecyl quaternary ammonium salt as a template agent, adopting mercaptopropyl trimethoxysilane as a functionalization reagent, and adopting a method of copolycondensation, synthesis and grafting to prepare thiol-functionalized mesoporous silica; 2) carrying out a reaction of the thiol-functionalized mesoporous silica and 2-(pyridindithio)ethyl ammonium chloride to obtain amino-functionalized mesoporous silica adopting a disulfide bond as a linker; 3) adopting a physical adsorption method to assemble a drug into pore channels of the mesoporous silica; and 4) linking folic acid to the mesoporous silica through the disulfide bond with a covalence effect to obtain the folic acid-functionalized drug-loaded mesoporous silica. The product of the present invention has characteristics of folic acid targeting effect, large specific surface area, high thermal stability, no toxicity, high drug loading rate, and effective prevention from drug leakage.

Description

technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a folic acid functionalized mesoporous silicon oxide and a preparation method thereof. Background technique [0002] The drug carrier is the main factor affecting the efficacy of the drug. Drug carriers with different properties have different drug release behaviors. An ideal drug carrier should have good biocompatibility, biodegradability, physical, chemical and biological stability, extremely low toxicity, and an appropriate drug loading. [0003] Mesoporous materials have uniform and adjustable mesoporous (2-50nm) channels, high specific surface area, stable skeleton structure, and easy functionalized surface. Mesoporous silicon oxide materials have been a research hotspot in the field of materials science since 1992 when scientists from Mobil Corporation of the United States first used nanostructure self-assembly technology to prepare mesoporous silicon oxi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/04A61K47/22C01B33/12
Inventor 房晨婕郭瑞张天蓝
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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