Method for improving solubility of poorly soluble drugs using silicon nanocarriers

A technology of insoluble drugs and silicon nanometers, which is applied in the directions of pharmaceutical formulations, organic active ingredients, and medical preparations of non-active ingredients, etc., can solve the problems of large particle size and difficult cellular uptake, etc., and achieves a simple preparation method and easy purification. Effect

Inactive Publication Date: 2018-05-25
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In view of the problem that the current mesoporous silicon drug carrier has a large particle size (greater than 200nm) and is not easily taken up by cells, the present invention provides a preparation method for small-diameter silicon nanoparticles capable of encapsulating insoluble drugs, which improves the efficiency of insoluble drugs. Solubility and Bioavailability

Method used

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  • Method for improving solubility of poorly soluble drugs using silicon nanocarriers
  • Method for improving solubility of poorly soluble drugs using silicon nanocarriers
  • Method for improving solubility of poorly soluble drugs using silicon nanocarriers

Examples

Experimental program
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Effect test

Embodiment 1

[0030] (1) Prepare 0.50% ((w / v)) aminopropyltriethoxysilane (APS) aqueous solution as the microemulsion water phase, prepare cetyltrimethylammonium bromide (CTAB), cyclohexane , Triton X-100 and n-octanol mixed solution are microemulsion oil phases, and the distribution ratio of each component is cetyltrimethylammonium bromide (CTAB) 0.15% (w / v), cyclohexane 65.5% (w / v), Triton X-100 18.15% (w / v), n-octanol 16.2% (w / v);

[0031] (2) The oil phase is added into the reactor and stirred at a stirring speed of 400rpm, and the water phase is slowly added to the oil phase to form a water-in-oil inverse microemulsion system, and the ratio of the water phase to the oil phase is 1:20, Continue to stir for 30min to form a stable microemulsion;

[0032] (3) Add tetraethyl orthosilicate (TEOS) and ammonia water to trigger the polymerization reaction, and the addition of tetraethyl orthosilicate (TEOS) and ammonia liquor is 0.45% (w / v) and 0.40% (w / v) of the total volume of the microemul...

Embodiment 2

[0038] (1) Prepare 1.00% (w / v) aminopropyltriethoxysilane (APS) aqueous solution as the microemulsion water phase, prepare cetyltrimethylammonium bromide (CTAB), cyclohexane, Triton The mixed solution of X-100 and n-octanol is the microemulsion oil phase, and the distribution ratio of each component is cetyltrimethylammonium bromide (CTAB) 0.3% (w / v), cyclohexane 60.00% (w / v) , Triton X-100 21.00% (w / v), n-octanol 18.70% (w / v);

[0039] (2) The oil phase is added into the reactor and stirred, the stirring speed is 300rpm, the water phase is slowly added to the oil phase to form a water-in-oil inverse microemulsion system, the ratio of the water phase to the oil phase is 1:15, Continue to stir for 60min to form a stable microemulsion;

[0040] (3) Add tetraethyl orthosilicate (TEOS) and ammonia water to trigger the polymerization reaction, and the addition of tetraethyl orthosilicate (TEOS) and ammonia liquor is 0.80% (w / v) and 0.70% (w / v) of the total volume of the microemuls...

Embodiment 3

[0046] (1) Prepare 0.40% (w / v) of 3-(methacryloyloxy)propyltrimethoxysilane (MEMO) (the aqueous solution is the microemulsion aqueous phase, prepare hexadecyltrimethylammonium bromide (CTAB), butane, Triton X-100 and n-heptanol mixed solution are the microemulsion oil phase, and the distribution ratio of each component is dodecyl dimethyl benzyl ammonium chloride (DDBAC) 0.2% (w / v), Butane 55.45% (w / v), Triton X-100 19.20% (w / v), n-heptanol 25.15% (w / v);

[0047] (2) The oil phase is added into the reactor and stirred at a stirring speed of 300rpm, and the water phase is slowly added to the oil phase to form a water-in-oil inverse microemulsion system, and the ratio of the water phase to the oil phase is 1:20, Continue to stir for 60min to form a stable microemulsion;

[0048] (3) add tetraethyl orthosilicate (TEOS) and ammoniacal liquor to trigger polymerization reaction, the addition of tetraethylorthosilicate (TEOS) and ammoniacal liquor is 0.40% (w / v) and 0.30% (w / v) of m...

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Abstract

The invention discloses a method for improving solubility of poorly soluble drugs using silicon nanocarriers. The technical points are as follows: an aqueous solution of silane is used as an aqueous phase, a mixed solvent of Triton X-100, alkanes, alcohols and pore-forming agents is used as an oil phase; under stirring conditions, the aqueous phase is added into the oil phase to form a water-in-oil reversed-phase microemulsion; after the microemulsion is stabilized, tetraethoxysilane (TEOS) and ammonia hydroxide are added to trigger polymerization reaction to form silicon nanoparticles at an emulsion interface; acetone is added to stop reaction, the silicon nanoparticles are added to an acetic acid solution to dissolve pore-forming agents after cleaning, and mesoporous silicon nanoparticles are obtained. The prepared mesoporous silica nanoparticle has a hollow structure with a particle size of 20 to 100 nm, a center cavity diameter is 5 to 20 nm, and a mesoporous diameter is 1 to 10 nm. The hollow mesoporous nanoparticles have the advantages that the poorly soluble drugs can be encapsulated, drug solubility and bioavailability are improved, and a new platform is provided for solubilization of the poorly soluble drugs.

Description

technical field [0001] The technology relates to the field of biopharmaceuticals, in particular to a method for preparing a silicon nanocarrier capable of improving the solubility of insoluble drugs, thereby increasing the solubility and bioavailability of insoluble drugs. Background technique [0002] Drug solubility is one of the important factors affecting drug bioavailability. Insoluble drugs have low solubility in water and are difficult to be absorbed by the body, resulting in low bioavailability and poor clinical efficacy. According to statistics, the proportion of poorly soluble drugs that have entered the development stage has increased from 40% to 70%. Due to the poor water solubility of these drugs, the preparation formulation and process are complicated, and there are many problems in bioavailability. Therefore, how to improve the solubility and bioavailability of poorly soluble drugs and diversify the dosage forms of poorly soluble drugs is a hot and difficult p...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/24A61K31/12A61K31/704
Inventor 孙广炜张英刘洋赵姗
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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