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Porous silica nano particle loaded with medicaments with slight solubility and preparation method and application of particle

A technology of porous silica and insoluble drugs, which is applied in the directions of non-active ingredients, such as medical preparations, drug combinations, and pharmaceutical formulations, can solve the problems of drug leakage and insufficient responsiveness, and achieves reduction of toxic side effects and broad application prospects. , the effect of improving water solubility

Inactive Publication Date: 2012-09-05
SHANGHAI INST OF CERAMIC CHEM & TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of today's nano-drug delivery systems can only achieve pH-responsive drug release in vitro at best, and the responsiveness is not high enough, or drug leakage is prone to occur under the condition of pH ≈ 7.4

Method used

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  • Porous silica nano particle loaded with medicaments with slight solubility and preparation method and application of particle
  • Porous silica nano particle loaded with medicaments with slight solubility and preparation method and application of particle
  • Porous silica nano particle loaded with medicaments with slight solubility and preparation method and application of particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Add 0.5mmol CTAB and 0.5mmol camptothecin to 50mL water together, stir at 80°C to dissolve completely, then add 4mmol ammonium fluoride to the system; add 4mmol tetraethyl orthosilicate after 30 minutes, and continue stirring for 1 Centrifuge after 1 hour and wash with water three times.

[0034] Use ultraviolet absorption spectrometer to detect the absorbance at 368nm of the mixed solution before and after the reaction, calculate the concentration of camptothecin in the solution according to the Beer-Lambert law, and calculate the drug loading capacity of porous silica nanoparticles in combination with the yield of porous silica nanoparticles .

[0035] The drug loading capacity of the obtained porous silica nanoparticles loaded with camptothecin is 1.5mg / g, and the average particle size is 100nm, with narrow particle size distribution and good dispersibility, such as figure 2 and image 3 Shown: figure 2 The porous structure and good monodispersity of the nanoparti...

Embodiment 2

[0039] Add 0.5mmol CTAB and 0.1mmol doxorubicin to 50mL water together, stir at 60°C to dissolve completely, then add 8mmol ammonium fluoride to the system; add 4mmol ethyl orthosilicate after 30 minutes, and continue stirring for 2 Centrifuge after 1 hour and wash with water three times.

[0040] After detection and analysis, it is known that the drug loading capacity of the porous silica nanoparticles loaded with doxorubicin prepared in this example is 80mg / g, the average particle size is 96nm, and has a narrow particle size distribution and good dispersibility. And it has a strong pH-sensitive drug release performance.

Embodiment 3

[0042] Add 0.17mmol P123 and 0.05mmol paclitaxel together into 80mL hydrochloric acid solution, stir at 35°C to dissolve completely, then add 2mmol zirconium oxychloride and 10mmol methyl orthosilicate to the system, continue stirring for 6 hours and then centrifuge , washed three times with water.

[0043] After detection and analysis, it is known that the drug loading capacity of paclitaxel-loaded porous silica nanoparticles prepared in this example is 32mg / g, the average particle size is 300nm, has a narrow particle size distribution and good dispersibility, and has Strong pH-sensitive drug release properties.

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Abstract

The invention discloses a porous silica nano particle loaded with medicaments with slight solubility. The nano particle has a nano composite structure of inorganic mesoporous silica / organic micelle / the medicaments with slight solubility, and the medicaments with slight solubility are wrapped in the organic micelle in porous channels of the inorganic mesoporous silica. According to the preparationmethod, the medicaments with slight solubility are loaded in situ and in a single step, and the carrier synthesis and medicament load are performed simultaneously, thereby remarkably improving the loading of the medicaments with slight solubility and simplifying the medicament loading way, wherein the total loading rate of the medicaments is higher than 80%, and the loading quantity of the medicaments is not lower than 1mg / g; the prepared nano particle has good dispersibility and high suspension stability, the size of the particle is less than 500nm and is adjustable, and the aperture of the nano particle ranges from 2nm to 30nm and is adjustable; the nano particle has the characteristics of pH-responsive releasing medicaments without subsequent modification; the preparation process is simple and can be implemented in a scale; and the nano particle can be applied to the preparation of anti-inflammation or anti-cancer medicinal preparations and has wide application prospect in the field of biomedicine.

Description

technical field [0001] The present invention relates to a kind of porous silicon dioxide nanoparticles loaded with insoluble drugs and its preparation method and application. The particle and its preparation method and application belong to the technical field of pharmaceutical nanomaterials. Background technique [0002] Due to their poor solubility, a large number of poorly soluble drugs often have disadvantages such as high toxicity and short circulation time in the body, which greatly restrict their application. Reducing the toxic and side effects of poorly soluble drugs and improving their bioavailability are of great significance for the development of new drugs. Improving the water solubility of poorly soluble drugs is an important strategy to improve their efficacy and reduce their side effects. At present, the commonly used method is to encapsulate poorly soluble drugs in organic micelles or liposomes. However, this technology has some important shortcomings, such...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/04A61K47/34A61P31/00A61P35/00
Inventor 何前军施剑林
Owner SHANGHAI INST OF CERAMIC CHEM & TECH CHINESE ACAD OF SCI
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