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

Active Publication Date: 2021-12-28
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, capsaicin has poor bioavailability due to its low water solubility, and capsaicin has a large irritant, which seriously hinders its development and utilization as a food-derived drug.

Method used

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  • Capsaicin-Vitamin E Prodrug Self-Assembled Nanoparticles and Its Preparation and Application
  • Capsaicin-Vitamin E Prodrug Self-Assembled Nanoparticles and Its Preparation and Application
  • Capsaicin-Vitamin E Prodrug Self-Assembled Nanoparticles and Its Preparation and Application

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention relates to the preparation of a capsaicin-vitamin E prodrug self-assembled nano drug delivery system. Capsaicin‑tocopherol prodrug (Cap‑SVE) was prepared by linking capsaicin to vitamin E using dithioethylenediacetic acid. On this basis, capsaicin-vitamin E prodrug self-assembled nanoparticles (Cap-SVE NPs) were further prepared. The prodrug self-assembled nanoparticles have some characteristics: the average particle size is less than 200nm, the distribution is spherical and uniform, and the drug loading can reach 8mg·mL calculated by capsaicin ‑1 . It is relatively stable under acidic conditions and gradually hydrolyzes at pH 7.4. The self-assembled nanoparticles of the prodrug can reduce the gastrointestinal irritation of capsaicin, significantly improve the bioavailability of capsaicin, increase the targeting effect of capsaicin in the liver, and significantly improve the anti-oxidation and hypolipidemic properties of capsaicin. effect. Good stability, high security, and great market prospects.

Description

technical field [0001] The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, and includes the synthesis of capsaicin-vitamin E prodrug and the construction of capsaicin-vitamin E prodrug self-assembled nanoparticles, as well as its application in drug delivery. Background technique [0002] Capsaicin (Capsaicin, Cap) is the main spicy ingredient in pepper. Capsicum is a herbaceous plant of the genus Capsicum of the Solanaceae family (Solanaceae), native to South America. Pepper is pungent in taste, hot in nature, has the effect of warming the middle and dispelling cold, appetizing and eliminating food. It is widely used in the treatment of vomiting, diarrhea, frostbite, cold stagnation and abdominal pain and other diseases. In addition, chili also has the effects of digestion, insecticide, and detoxification. Modern pharmacological research shows that capsaicin is the main active ingredient of capsicum and has v...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/54A61K47/69A61K31/165A61P1/16A61P3/06C07D311/72
CPCA61K9/5123A61K31/165C07D311/72
Inventor 余江南冯颖淑徐希明张卫明
Owner JIANGSU UNIV
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