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
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[0047] Example 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 under stirring at 25° C. and 500 rpm, continue stirring for 10 minutes, and remove the methanol by rotary evaporation. Subsequently, 8 mg of ACGs were dissolved in 0.4 mL of methanol, and injected into the above-obtained solution under normal temperature and 500 rpm stirring conditions, 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) is 0.08, and the potential value is -22.9mV.
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[0049] Example 2
[0050] Prepare ACGs suspension with a concentration of 2mg / mL, pipette 6μL onto a 300-mesh copper net, dry naturally in the air, and stain with 0.1% uranyl acetate for 10 minutes. Observe the shape of the particles under a transmission electron microscope ( figure 2 ).
Example Embodiment
[0051] Example 3 Investigation of the stability of ACGs nanoparticles in artificial gastrointestinal fluid
[0052] The configuration 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, and dilute to 1000mL with water.
[0053] The configuration of artificial intestinal juice: 6.8g potassium dihydrogen phosphate, add 500mL water, adjust pH 6.8 with 0.1mol / L sodium hydroxide, take another 10g trypsin, add water to dissolve, mix the two liquids and dilute with water to 1000mL.
[0054] Take 0.5 mL of the prepared artificial gastrointestinal fluid after passing the membrane and mix it with ACGs nanoparticles in equal volume, and measure the change of its particle size at a certain time.
[0055] Results: In the artificial gastrointestinal fluid, ACGs nanoparticles have little change in particle size within 12 hours ( image 3 ), indicating that ACGs nanoparticles are basically stable in...
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