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Annonaceous acetogenins nanoparticles taking cyclodextrin and lecithin as vectors as well as preparation method and application of annonaceous acetogenins nanoparticles

A cyclodextrin and nanoparticle technology, which can be applied to non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. Low problems, to achieve significant anti-tumor efficacy, simple process, no toxic and side effects

Active Publication Date: 2017-02-15
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] ACGs have poor water solubility, less than 1ug / mL, and are difficult to administer, resulting in greatly limited in vivo research
Existing in vivo studies mostly adopt suspension gavage, or disperse in vegetable oil for oral administration, and its curative effect is difficult to maximize due to low bioavailability
Moreover, ACGs have large toxic and side effects, narrow therapeutic window, and have certain toxicity to the liver and kidney of rats.

Method used

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  • Annonaceous acetogenins nanoparticles taking cyclodextrin and lecithin as vectors as well as preparation method and application of annonaceous acetogenins nanoparticles
  • Annonaceous acetogenins nanoparticles taking cyclodextrin and lecithin as vectors as well as preparation method and application of annonaceous acetogenins nanoparticles
  • Annonaceous acetogenins nanoparticles taking cyclodextrin and lecithin as vectors as well as preparation method and application of annonaceous acetogenins nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048]Weigh 2 mg of soybean lecithin and dissolve it in 0.2 mL of methanol, slowly inject it into 4 mL of aqueous solution containing 4 mg of hydroxypropyl-β-cyclodextrin at 25°C and 500 rpm under stirring conditions, continue stirring for 10 minutes, and then rotary evaporate to remove methanol. Subsequently, 8 mg of ACGs was dissolved in 0.4 mL of methanol, injected into the above-obtained solution at room temperature and stirred at 500 rpm, and then the methanol was removed by rotary evaporation to obtain ACGs nanoparticles. The average particle size is 144.4nm ( figure 1 ), the polydispersity index (PDI) was 0.08, and the potential value was -22.9mV.

Embodiment 2

[0050] Prepare ACGs suspension at a concentration of 2 mg / mL, absorb 6 μL and drop it on a 300-mesh copper grid, let it dry naturally in the air, and then stain it with 0.1% uranyl acetate for 10 min, observe the morphology of the particles under a transmission electron microscope ( figure 2 ).

Embodiment 3

[0051] Example 3 Investigation of the Stability of ACGs Nanoparticles in Artificial Gastrointestinal Fluid

[0052] Preparation of artificial gastric juice: Take 16.4mL of dilute hydrochloric acid with a concentration of 1mol / L, add 800mL of distilled water, 10g of pepsin, mix well, add water to dilute to 1000mL.

[0053] Preparation of artificial intestinal juice: 6.8g potassium dihydrogen phosphate, add 500mL water, adjust pH to 6.8 with 0.1mol / L sodium hydroxide, take another 10g trypsin, add water to dissolve, mix the two liquids and add water to dilute to 1000mL.

[0054] Take 0.5mL of the prepared artificial gastrointestinal fluid after passing through the membrane, mix it with ACGs nanoparticles in equal volume, and measure the change of its particle size at a certain time point.

[0055] Results: In the artificial gastrointestinal fluid, the particle size of ACGs nanoparticles changed little within 12 hours ( image 3 ), indicating that ACGs nanoparticles are basicall...

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Abstract

The invention relates to annonaceous acetogenins nanoparticles, which are prepared by taking cyclodextrin and lecithin as vectors, as well as a preparation method and an application of annonaceous acetogenins nanoparticles. The annonaceous acetogenins (annonaceous acetogenins total lactone or monomer ingredients thereof) nanoparticles are prepared by virtue of a solvent precipitation method; the mass ratio of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 1 to (0.02-20) to (0.02-20); and in accordance with an optimal prescription, the combining proportion of the annonaceous acetogenins to the cyclodextrin to the lecithin is at 4 to 2 to 1 (in percentage by mass). The average grain size of the annonaceous acetogenins nanoparticles is 20-1000nm, and the annonaceous acetogenins nanoparticles are good in dispersity; the annonaceous acetogenins nanoparticles are stable in both gastrointestinal fluid and plasmid, and the annonaceous acetogenins nanoparticles are suitable for both oral administration and intravenous injection; with the application of the nanoparticles, the inhibitory effect of the annonaceous acetogenins on tumor cells can be significantly improved, and meanwhile, in vivo anti-tumor efficacy can be enhanced; and the annonaceous acetogenins nanoparticles have a broad development prospect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an annonacein nanoparticle prepared by using cyclodextrin and lecithin as carriers, a preparation method and application thereof. Background technique [0002] Annonacein includes annonacein lactones (ACGs for short) and its monomers bullatacin, squamostatin, annosquacin, etc. Annonacein is a series of long-chain fatty acids with 35 or 37 carbons extracted from the seeds of Annonaceae plants, and contains 0 to 3 tetrahydrofuran (THF) ring-like structures. Most of the total lactones and monomers of custard apple showed strong anti-tumor activity, and the most active monomer bullatacin was effective against lung cancer A549 cells, human liver cancer HepG2 cells, human cervical cancer HeLa cells, and human breast cancer MCF-7 cells. , human colon cancer Lovo cells, sarcoma S180 cells, etc. have significant curative effect. At the same time, ACGs also have good activity a...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/40A61K47/24A61K31/365A61P35/00
CPCA61K9/0019A61K9/0053A61K9/5123A61K9/5161A61K31/365
Inventor 王向涛洪靖怡刘营营
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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