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Capsaicin-vitamin e prodrug liposome, and preparation method therefor and use thereof

A technology of capsaicin and vitamins, which is applied in the field of capsaicin-vitamin E prodrug liposome and its preparation method and application, and can solve the problems of hindering the development and utilization of food-derived drugs, the great irritation of capsaicin, and poor bioavailability, etc. question

Inactive Publication Date: 2018-09-28
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 liposome, and preparation method therefor and use thereof
  • Capsaicin-vitamin e prodrug liposome, and preparation method therefor and use thereof
  • Capsaicin-vitamin e prodrug liposome, and preparation method therefor and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1. the synthesis of capsaicin-vitamin E prodrug

[0025] 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

[0031] Embodiment 2. the preparation of capsaicin-vitamin E prodrug liposome

[0032]The preparation process of capsaicin-vitamin E prodrug liposome is as follows: Weigh 90 mg of soybean lecithin for injection and place it in a round bottom flask, add absolute ethanol, sonicate until clarification, continue to add cholesterol 25 mg, sodium cholate 30 mg and nutmeg Acetate isopropyl ester 30mg, sonicate until clear, and remove most of absolute ethanol by rotary evaporation. Take 10 mg of capsaicin-vitamin E prodrug and dissolve it in absolute ethanol, add it into a round bottom flask, shake it evenly, and remove all the absolute ethanol by rotary evaporation until a thin film is formed at the bottom of the bottle wall. Add an appropriate amount of distilled water and shake slowly until a uniform, transparent solution with blue shimmer is formed to obtain the capsaicin-vitamin E prodrug liposome solution.

Embodiment 3

[0033] Embodiment 3. the preparation of capsaicin-vitamin E prodrug liposome

[0034] The preparation process of capsaicin-vitamin E prodrug liposome is as follows: Weigh 50 mg of soybean lecithin for injection and place it in a round bottom flask, add absolute ethanol, sonicate until clarification, continue to add cholesterol 12.5 mg, sodium cholate 22.5 mg and Isopropyl myristate 30 mg, sonicated until clarified, and most of absolute ethanol was removed by rotary evaporation. Take 10 mg of capsaicin-vitamin E prodrug and dissolve it in absolute ethanol, add it into a round bottom flask, shake it evenly, and remove all the absolute ethanol by rotary evaporation until a thin film is formed at the bottom of the bottle wall. Add an appropriate amount of distilled water and shake slowly until a uniform, transparent solution with blue shimmer is formed to obtain the capsaicin-vitamin E prodrug liposome solution.

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Abstract

Disclosed is a capsaicin-vitamin E prodrug liposome, which uses dithiodiglycolic acid to link capsaicin to vitamin E to prepare a capsaicin-vitamin E prodrug and uses the capsaicin-vitamin E prodrug as a model drug to prepare the capsaicin-vitamin E prodrug liposome. Excipients used include: phospholipid, cholesterol, sodium cholate and isopropyl myristate. The prodrug liposome has some characteristics: being near-spherical and uniformly distributed, with an average particle size of about 160 nm, and the drug loading capacity calculated with capsaicin of up to 8 mg*mL-1. The prodrug liposomescan reduce the irritation of capsaicin on the gastrointestinal tract and significantly increase the bioavailability of capsaicin. The invneiotn discloses a preparation method of the capsaicin-vitaminE prodrug liposome.

Description

technical field [0001] The invention relates to the construction of capsaicin-vitamin E prodrug liposome and its application in drug delivery system. Background technique [0002] Capsaicin is the main pungent component in capsicum, which has various pharmacological activities, such as anti-oxidation, anti-inflammation, analgesia, lowering blood fat, and anti-tumor, and has great development value. 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. [0003] Liposome is a nano-preparation formed by directional arrangement of phospholipid bimolecules, and has a single-layer or multilayer double-lipid membrane structure. When amphiphilic molecules are dispersed in the water phase, their hydrophobic tails gather together, and the hydrophilic head contacts with the water phase to form closed vesicles with a bilayer structure, and small lip...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/54A61K31/165A61P1/16A61P3/06
CPCA61K9/127A61K31/165A61K47/545A61P1/16A61P3/06A61K9/16A61K47/22A61P3/00
Inventor 余江南冯颖淑徐希明张卫明
Owner JIANGSU UNIV
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