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Method for preparing water soluble hypocrellin silica nanometer particle and its application in preparing venous injection

A technology of oleocanthin and silicon dioxide, applied in the field of photosensitizers, can solve the problems of inconvenient preparation of medicaments, poor water solubility, etc., and achieve the effects of eliminating phototoxic side effects, high water solubility, and good dispersibility

Inactive Publication Date: 2007-12-12
CHANGSHU NANJING NORMAL UNIV DEV RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the shortcoming that hypocrellin is inconvenient to be made into medicament due to its poor water solubility, and at the same time, according to the requirements for phototherapy drugs in the clinical treatment process of photodynamic therapy, nano silicon dioxide with core-shell structure is introduced into bamboo In the research on the application of rhodomycin, water-soluble hypocretin silica nanoparticles with clinical application prospects were prepared, and the water-soluble hypocretin silica nanoparticles were applied to the preparation of intravenous injections of photodynamic drugs. That is, the application will provide the preparation method of water-soluble hypocretin silicon dioxide nanoparticles and its application in the preparation of intravenous injections

Method used

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  • Method for preparing water soluble hypocrellin silica nanometer particle and its application in preparing venous injection
  • Method for preparing water soluble hypocrellin silica nanometer particle and its application in preparing venous injection
  • Method for preparing water soluble hypocrellin silica nanometer particle and its application in preparing venous injection

Examples

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Embodiment 1

[0050] A single silane is used to prepare water-soluble hypocrellin silica nanoparticles, and the reaction system and conditions are as follows:

[0051] Add methanol 24mL, a certain amount of hypocrellin A methanol solution (0.4mM), N-(β-aminoethyl)-γ-aminopropyl-triethoxysilane 200ul, and ammonia water 200ul to the experimental system in sequence, The magnetic stirrer was used for 20 hours. After the reaction, the pH value of the solution was adjusted to 7.0 with hydrochloric acid, and the small molecular compounds generated during the hydrolysis of methanol were removed by dialysis, and finally, water-soluble hypocrellin A silica nanoparticles were obtained by freeze-drying.

[0052] The water-soluble hypocrellin A silicon dioxide nanoparticles were prepared into intravenous injections of photodynamic drugs. When used as an intravenous injection of photodynamic medicine, the range of the recommended injection amount of the present invention is: 2-8mg / kg, add 250ml of glucos...

Embodiment 2

[0054] Composite silane to prepare water-soluble hypocrellin A silica nanoparticles, the reaction system and conditions are as follows:

[0055] Add methanol 24mL, a certain amount of hypocretin A methanol solution (0.4mM), N-(β-aminoethyl)-γ-aminopropyl-triethoxysilane 200ul, tetramethoxy After 200ul of silane and 200ul of ammonia water, 20 hours on a magnetic stirrer, vacuum drying at 50°C, adding 50mL of double distilled water and 80uL of hydrochloric acid to adjust the pH to 7.0, dialyzing to remove methanol and small molecular compounds generated during hydrolysis, and finally freeze-drying to obtain water-soluble Hypocretin A silica nanoparticles.

Embodiment 3

[0057] The raw materials are basically the same as in Example 2; the composite silane is introduced into the surfactant AOT to prepare water-soluble hypocrellin A silica nanoparticles, and the reaction system and conditions are as follows:

[0058] Dissolve 0.44g AOT, 800ul n-butanol in 20ml double distilled water, stir until clarification with a magnetic stirrer, then add a certain amount of DMF solution (15mM) of hypocrellin A to the solution, stir with a magnetic stirrer until clarification, Add 200ul TEVS and stir for one hour, then add 10ul APTES and stir for 20 hours. Then the solution was dialyzed against water with a 12-14KD cellulose dialysis bag for 48 hours to remove surfactant AOT, n-butanol and small molecular compounds generated during hydrolysis. Finally, the solution is freeze-dried to obtain the water-soluble hypocrellin A silicon dioxide nanoparticles.

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Abstract

Preparation method of water-soluble hypocrelline silica nanoparticle comprises carrying out hydrolysis of single silicane or multiple silicanes to obtain nano-silica with core-shell structure, enveloping hypocrelline under the existence or inexistence of surfactant, dialysing to remove solvent and small moleculal chemical compound, and freeze drying to obtain water-soluble hypocrelline silica nanoparticle with particle diameter less than 150nm suitable for intravenous injection. The invention also provides thr application of the water soluble hypocrelline silica nanoparticle in preparing photodynamic medicinal intravenous injection. The inventive preparation method has simple and easy operation and high product stability. The nanoparticle has good water-solubility and dispersity, low dark toxicity, and high phototoxicity; can not liberate hypocrelline thereby eliminating its photo toxico-adverse side effect. Hypocrellines can gather in intrastitial mitochondrion, effectively improve phototherapy efficiency, and reduce pharmic consumption.

Description

technical field [0001] The invention belongs to the technical field of photosensitizers with photodynamic activity, and relates to a preparation method of water-soluble hypocretin silica nanoparticles, and the use of the water-soluble hypocretin silica nanoparticles in preparing photodynamic drugs Application in intravenous injection. Background technique [0002] Photodynamic therapy (PDT) is a new type of tumor clinical therapy developed in recent years. Compared with traditional tumor treatment techniques (such as chemotherapy, radiotherapy and surgery, etc.), it has specific killing tumor cells, It has unique advantages such as little damage to healthy tissues, low toxic and side effects, few postoperative complications, and economic convenience. Especially for those patients with advanced cancer and who are not suitable for traditional treatment techniques due to age, physical fitness and other reasons, photodynamic therapy is still an ideal treatment method, so this t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K47/04A61K31/122A61P35/00
Inventor 周家宏魏少华冯玉英周林董超沈健
Owner CHANGSHU NANJING NORMAL UNIV DEV RES INST
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