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Ph reversible response mesoporous silicon oxide composite medicament-carrying system, preparation method thereof and application thereof

A technology of mesoporous silica and silicon oxide, which is applied in pharmaceutical formulations, medical preparations of non-active ingredients, gene therapy, etc., to achieve the effects of high-efficiency drug release, excellent magnetic targeting effect, and excellent biocompatibility

Inactive Publication Date: 2011-10-12
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of the present invention is to provide a pH-reversible responsive mesoporous silica composite drug-loading system, which can realize high-activity loading and pH-responsive fixed-point reversible release of drugs / proteins and genes, and solve the "zero release" problem of traditional drug carriers At the same time, the drug can be released in a pulsed manner, and the composite drug-loading system has good magnetic targeting performance and biocompatibility

Method used

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  • Ph reversible response mesoporous silicon oxide composite medicament-carrying system, preparation method thereof and application thereof
  • Ph reversible response mesoporous silicon oxide composite medicament-carrying system, preparation method thereof and application thereof
  • Ph reversible response mesoporous silicon oxide composite medicament-carrying system, preparation method thereof and application thereof

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Embodiment 1 3

[0054] The synthesis of embodiment 1 triaminomethylethane-3 hydrochloric acid compound (TAE 3HCl)

[0055] Sodium azide (7 g) and 60 ml of DMF were added into the flask, stirred, then tribromoneopentyl alcohol (3.3 g) was added, the reaction system was heated to 90 degrees, and stirred for 28 hours under the protection of nitrogen. After the reaction was finished, the obtained product was poured into 500 ml of water, and extracted with ether (38 ml*4), the ether extracts obtained were combined together, dried with magnesium sulfate, filtered, and the volume of the solution was concentrated to 50ml. Then dioxane (125 ml), triphenylphosphine (13.3 g) and ammonia water (aq, 30%, 50 ml) were added to the solution, and stirred at room temperature for 19 hours. The solution of the product after stirring for 19 hours was sucked off, and the obtained product was dispersed in chloroform (200 ml), then extracted with HCl (aq, 2.5M, 38ml*5), and the obtained extracts were combined toget...

Embodiment 2 3

[0056] Synthesis of embodiment 2 triazadamantane compound (TAA)

[0057] Triethylamine (1.65ml) was added dropwise to the product in 0.8 gram of embodiment 1 dissolved in 10ml of methanol, stirred, and added benzaldehyde (1.05ml), the mixture was stirred and heated to reflux, and the reaction stopped after 20 minutes. Cool and evaporate the solvent, add 10 ml of water to the obtained product, stir and filter, so as to obtain the target product (triazaadamantane) protected by benzaldehyde, which can be used for the next reaction. Product liquid phase NMR results: 1 H NMR (400MHz, CDCl 3 )δ7.21-7.89 (m, 15H, Ar), 5.62 (s, 1H, PhCH eq ), 5.42 (s, 2H, PhCH ax ), 3.53 (d, J=13.2Hz, 2H, -CH 2 N-), 3.22 (d, J=12.9Hz, 2H, -CH 2 N-), 3.07(s, 1H, OH), 2.93(s, 4H, -CH 2 N-, -CH 2 O-).

Embodiment 34

[0058] The synthesis of embodiment 34-carboxybenzaldehyde-dimethoxy acetal (CBA-DMA)

[0059] 4 grams of 4-carboxybenzaldehyde were dispersed in 80 milliliters of methanol solution, 8 grams of ammonium chloride solid was added, and the reaction was heated under reflux for 20 hours. The solvent was removed by a rotary evaporator, and the white target product was obtained by recrystallization from n-hexane.

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Abstract

The invention discloses a pH reversible response mesoporous silicon oxide composite medicament-carrying system, a preparation method thereof and application thereof. The preparation method comprises the following steps of: preparing mesoporous silicon oxide nano particles by a sol-gel process; and modifying surfaces of mesoporous silicon oxide and nanometer magnetic particles respectively by using triaminomethyl ethane and 4-carboxybenzaldehyde, and reacting in alkalescent environment to generate pH sensitive triaza diamantane groups, so that the magnetic nano particles are covered on the surface of a mesoporous silicon oxide porous channel to obtain the pH reversible response mesoporous silicon oxide composite medicament-carrying system. The pH reversible response mesoporous silicon oxide composite medicament-carrying system has the excellent magnetic targeting and biocompatibility, and can realize pH response pulse release.

Description

technical field [0001] The present invention relates to a pH reversible responsive mesoporous silica composite drug-loading system and its preparation and application, in particular to a nano-magnetic particle / mesoporous silica material composite drug-loading system and its preparation method and application, in particular to a A pH-responsive nano-magnetic particle / mesoporous silica nano-composite drug-loading system and its preparation method and application. Background technique [0002] Due to their regular and adjustable pores, high specific surface area, easily modified surface, and good cell membrane penetration properties, nanometer mesoporous silica (MSNs) and its aqueous suspension are widely used in functional drugs, proteins and Gene carrier. In addition, due to the unique and regular through-hole structure with open ends, the orifices at both ends of MSNs can be closed by a kind of "lid", and then opened under physical and chemical stimuli outside the body, so ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/04A61K47/02A61K48/00
Inventor 刘昌胜甘琪袁媛施剑林
Owner EAST CHINA UNIV OF SCI & TECH
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