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Capsaicin-vitamin E prodrug self-assembly nanoparticles and preparation method and purpose thereof

A technology for self-assembling nanoparticles and capsaicin, which is applied in the directions of drug combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve problems such as hindering the development and utilization of food-derived drugs, large irritation of capsaicin, and poor bioavailability. And other issues

Active Publication Date: 2017-08-18
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-assembly nanoparticles and preparation method and purpose thereof
  • Capsaicin-vitamin E prodrug self-assembly nanoparticles and preparation method and purpose thereof
  • Capsaicin-vitamin E prodrug self-assembly nanoparticles and preparation method and purpose thereof

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 preparation of a capsaicin-vitamin E prodrug self-assembly nano drug delivery system. Thiodiglycolic acid is utilized for connecting capsaicin and vitanmin E so as to prepare capsaicin-vitamin E prodrug (Cap-SVE). On this basis, capsaicin-vitamin E prodrug self-assembly nanoparticles (Cap-SVE NPs) are prepared further. The prodrug self-assembly nanoparticles have features as following. The average particle size is smaller than 200 nm and the prodrug self-assembly nanoparticles are distributed uniformly in spherical shape. The drug carrying capacity reaches 8 mg*mL<-1> on the calculation base of capsaicin.The prodrug self-assembly nanoparticles are stable in acid environment and hydrolyzes gradually in PH 7.4. irritation to gastrointestinal tract of capsaicin can be reduced, biological utilization of capsaicin can be improved distinctively, targeting effects of capsaicin in livers can be enhanced and pesticide effect of capsaicin in oxidation resistance and blood fat reduction can be improved distinctively. The stability is good, the safety is high and the capsaicin-vitamin E prodrug self-assembly nanoparticles have good market prospect.

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 Applications(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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