Capsaicin-Vitamin E Prodrug Self-Assembled Nanoparticles and Its Preparation and Application
A technology of self-assembled nanoparticles and capsaicin, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, etc., can solve the problems that hinder the development and utilization of food-borne drugs, the great irritation of capsaicin, and the poor bioavailability To improve bioavailability, increase targeting effect, improve anti-oxidation and lower blood lipid
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Embodiment 1
[0037] Embodiment 1. the synthesis of capsaicin-vitamin E prodrug
[0038] Dissolve 1 g of dithiodiacetic acid in 10 mL of acetic anhydride, stir at room temperature for 3-4 hours, and evaporate to dryness at 60° C. after the reaction is complete. The crude product was dissolved in an appropriate amount of dichloromethane, 20 mg DMAP and 500 mg vitamin E were added, and stirred at room temperature for 2 hours. The reaction solution was purified with a silica gel column, and the eluent was petroleum ether-ethyl acetate-glacial acetic acid (95:5:0.1~80:20:0.1, V / V) to obtain about 800 mg of S-VE. Dissolve 500mg of S-VE in an appropriate amount of dichloromethane, add 200mg of DCC, 14mg of DMAP, stir at room temperature for 5 minutes, add 250mg of capsaicin, and stir for two hours at room temperature. The reaction solution was purified with a silica gel column, and the eluent was dichloromethane-methanol (100:0-90:10 V / V), and about 500 mg of light yellow viscous semi-solid was ...
Embodiment 2
[0044] Example 2. Preparation of capsaicin-vitamin E prodrug self-assembled nanoparticles
[0045] The preparation process is as follows: Take an appropriate amount of capsaicin-vitamin E prodrug in Example 1 and dissolve it in absolute ethanol, and slowly drop it into deionized water under the condition of magnetic stirring (600-800rpm). Make the final concentration of ethanol <5%. Under these conditions, the capsaicin-vitamin E prodrug self-assembled to form a liquid with blue shimmer, that is, the capsaicin-vitamin E prodrug self-assembled nanoparticle solution.
Embodiment 3
[0046] Example 3. Morphological observation of capsaicin-vitamin E prodrug self-assembled nanoparticles
[0047] Observe the morphology of capsaicin-vitamin E prodrug self-assembled nanoparticles in Example 2 through a transmission electron microscope, specifically: prepare capsaicin-vitamin E prodrug self-assembled nanoparticles, dilute with an appropriate amount of distilled water and drop it on a copper grid, and leave it at room temperature Let dry. Then add a drop of 2% phosphotungstic acid to stain the sample, leave it to dry at room temperature, and observe its morphological characteristics with a transmission electron microscope. Figure 4 It is in the form of capsaicin-vitamin E prodrug self-assembled nanoparticles, which is spherical.
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