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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

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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, to solve the technical problem that norcantharidic acid cannot maintain its drug concentration in the body under the condition of higher dosage

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

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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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