Demethylcantharidate-loaded mesoporous silica nanoparticle and preparation method thereof

A technology of mesoporous and mesoporous silica of cantharidinic acid, which is applied in medical formulations, active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, etc., can solve the problem that norcantharidinic acid cannot maintain drug concentration, etc. Achieve the effects of improving bioavailability, increasing synthesis yield, and prolonging the half-life in vivo

Active Publication Date: 2019-05-28
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a kind of mesoporous silica nanoparticles loaded with norcantharidic acid and its preparation

Method used

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  • Demethylcantharidate-loaded mesoporous silica nanoparticle and preparation method thereof
  • Demethylcantharidate-loaded mesoporous silica nanoparticle and preparation method thereof
  • Demethylcantharidate-loaded mesoporous silica nanoparticle and preparation method thereof

Examples

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Effect test

Embodiment 1

[0023] The preparation method of mesoporous silica nanoparticles containing norcantharidic acid includes:

[0024] (1)NH 2 -Preparation of MSNs: 0.5g CTAB is dissolved in 40g ultrapure water, and 2mol / L NaOH solution is added to adjust the pH to 11; after magnetic stirring at 80℃ for 1h, the mixture containing 1.5mL TEOS and 0.5mL APTES is added dropwise Add to CTAB aqueous solution, react for 2h, stand for 4h, centrifuge at 15000r / min for 45min, wash with acidic ethanol to remove the template CTAB, the volume ratio of absolute ethanol to hydrochloric acid in the acidic ethanol is 10:1; wash with water, centrifuge, and freeze Dry to get NH 2 -MSNs.

[0025] (2)DM-NCTD@NH 2 -Preparation of MSN: Weigh NH 2 -MSNs freeze-dried powder 50mg, add to 10mL of 1mg / mL DM-NCTD aqueous solution, stir for 24h; 15000r / min high-speed centrifugation for 60min, remove free DM-NCTD, wash with water, centrifuge and freeze-dry to obtain DM-NCTD @NH 2 -MSN.

[0026] Observe the prepared NH with a high-p...

Embodiment 2

[0042] H22 in vitro cytotoxicity test:

[0043] Take H22 in the logarithmic growth phase, collect the suspension cell liquid, adjust the cell concentration, and seed it in a 96-well plate with a seeding density of 1×10 4 / Well; after the 96-well plate is incubated in a constant temperature incubator for 24 hours, the original drug (DM-NCTD), DM-NCTD@NH 2 -MSN group was added at different concentrations (0.8, 4, 20, 100, 500μg / mL), and 3 multiple wells were set for each concentration to calculate the average value; sterilized PBS was added to the outermost wells of the 96-well plate Buffer 0.2mL to resist the edge effect; 96-well plates were incubated for 24 and 48 hours respectively. Take the 96-well plates according to the time point, add 20μL / well of 5mg / ml MTT solution, and incubate at 37°C for 4 hours; In addition to the liquid in the well, add DMSO, 100μL / well; detect the absorbance at 490nm by the microplate reader; calculate and count the tumor inhibition rate, among which,...

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Abstract

The invention discloses a demethylcantharidate-loaded mesoporous silica nanoparticle. A preparation method of the demethylcantharidate-supported mesoporous silica nanoparticle comprises the steps of preparing ammonia-modified mesoporous silica through a co-precipitation method and preparing DM-NCTD@NH2-MSN by electrostatic adsorption loading of demethylcantharidate. The prepared DM-NCTD@NH2-MSN has obvious slow-release effects and long-acting tumor suppression effects, and has a better application prospect as a DM-NCTD tumor target delivery system.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a mesoporous silica nanoparticle containing norcantharidic acid and a preparation method thereof. Background technique [0002] Norcantharidin (Norcantharidin, NCTD) is based on the chemical structure of cantharidin (CTD), an effective anti-cancer component of the cantharidin of the Coleoptera genus Cantharidin. It is synthetically synthesized after removing the 1 and 2 methyl groups. The first anti-cancer drug with the effect of increasing white blood cells in the world, and the first anti-cancer drug synthesized in my country. NCTD has strong anti-tumor activity and a broad spectrum of tumor inhibition. It is mainly used to treat digestive tract tumors, especially primary liver cancer. It exists stably in the form of ring-opening hydrolysis in vivo and in vitro, that is, Diacid metabolite of norcantharidin (DM-NCTD). Although DM-NCTD has great potential for therapeutic ef...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/34A61K47/04A61P35/00
Inventor 刘敏臣
Owner ZHEJIANG UNIV
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