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Novel acid response ionic liquid microcapsule as well as preparation method and application thereof

A technology of ionic liquid and microcapsule, which is applied in the field of new acid-responsive ionic liquid microcapsule and its preparation, to achieve the effect of improving drug efficacy, simple preparation method and reducing drug resistance

Active Publication Date: 2021-12-07
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no report on using MPN as a stabilizer of ionic liquid microemulsions to prepare ionic liquid microcapsules, and using its acid responsive properties to endow the ionic liquid system with the ability to release drugs in response to acid

Method used

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  • Novel acid response ionic liquid microcapsule as well as preparation method and application thereof
  • Novel acid response ionic liquid microcapsule as well as preparation method and application thereof
  • Novel acid response ionic liquid microcapsule as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] A method for preparing a novel acid-responsive ionic liquid microcapsule (IL@MPN), comprising the following steps:

[0047] Add 1.0 mg of quercetin to 2.0 mL of 1-ethyl-3-methylimidazolium bistrifluoromethanesulfonimide salt ionic liquid, stir to make it fully dissolve, and obtain a polyphenol-ionic liquid solution; take the above polyphenol - Add 40 μL of ionic liquid solution to 2.0 mL of water, sonicate for 1 min at a power of 260 W and an ultrasonic frequency of 25 kHz to disperse evenly, then add 20 μL of 10.0 mg / mL ferric chloride aqueous solution, vortex for 30 s, and then use 0.1 mol / mL The pH of the system was adjusted to 8.0 with L NaOH aqueous solution, and the dispersion of novel acid-responsive ionic liquid microcapsules (IL@MPN) was obtained; A novel acid-responsive ionic liquid microcapsule (IL@MPN) was obtained.

[0048] The SEM image, TEM image and optical microscope image of the ionic liquid microcapsule (IL@MPN) prepared in this example are as follow...

Embodiment 2

[0050] The preparation method of a novel acid-responsive ionic liquid microcapsule (IL@MPN) is as described in Example 1, the difference is that the volume ratio of water and polyphenol-ionic liquid is changed to 2000:1, 500:1, 200:1, 20:1.

[0051] The particle size of the microcapsules obtained in this embodiment varies with the volume ratio of water / polyphenol-ionic liquid. The histogram is as follows Figure 4 shown, from Figure 4 It can be seen that the particle size of the obtained ionic liquid microcapsules increases with the decrease of water / polyphenol-ionic liquid volume ratio.

Embodiment 3

[0053] A method for preparing a novel acid-responsive ionic liquid microcapsule (IL@MPN), comprising the following steps:

[0054] Add 1.0 mg of quercetin into 1.0 mL of fatty acid ethyl ester linoleate ionic liquid, stir to make it fully dissolve, and obtain a polyphenol-ionic liquid solution; take 80 μL of the above polyphenol-ionic liquid solution and add it to 8.0 mL In water, sonicate for 1min under the condition of 260W power and 25kHz ultrasonic frequency to disperse evenly, then add 40μL 10.0mg / mL ferric chloride aqueous solution, vortex for 30s, then adjust the pH of the system to 8.0 with 0.1mol / L NaOH aqueous solution, The novel acid-responsive ionic liquid microcapsules (IL@MPN) dispersion was obtained; the obtained novel acid-responsive ionic liquid microcapsules (IL@MPN) dispersion was centrifuged at 2000rpm for 3min to obtain the novel acid-responsive ionic liquid microcapsules. Capsules (IL@MPN).

[0055] The optical microscope images of the ionic liquid micro...

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Abstract

The invention provides a novel acid response ionic liquid microcapsule as well as a preparation method and application thereof. The ionic liquid microcapsule comprises an inner core and a shell layer, wherein the inner core is ionic liquid, and the shell layer is a metal-polyphenol network coating. The preparation method of the microcapsule comprises the following steps: adding polyphenol into the ionic liquid, and performing stirring to dissolve the polyphenol to obtain polyphenol-ionic liquid; adding the polyphenol-ionic liquid into water, and performing ultrasonic and uniform dispersing; and then adding a metal ion solution, performing whirling to uniformly mix the system, then adjusting the pH value of the system, and performing centrifuging to obtain the microcapsule. According to the ionic liquid microcapsule prepared by the method, the stability of ionic liquid droplets can be remarkably improved, and various drug molecules, especially indissolvable drugs, can be effectively loaded; and MPN of the prepared microcapsule is dissociated in an acidic microenvironment, so that the ionic liquid carries the medicines to permeate into a target tissue, and the utilization rate of the medicines is greatly improved and the efficacy of the medicines is enhanced due to the relatively strong medicine permeation effect of the ionic liquid.

Description

technical field [0001] The invention relates to a novel acid-responsive ionic liquid microcapsule and its preparation method and application, belonging to the technical field of drug delivery. Background technique [0002] Most drug molecules (approximately 60%-70%) have greatly reduced drug utilization efficiency due to low solubility and poor permeability. In the field of pharmacy, the problem of poor solubility and permeability is improved by using chemical penetration enhancers (CPE). In recent years, ionic liquids (ILs) have been introduced into drug delivery systems as a novel permeation enhancer for enhanced transdermal drug delivery to various drug molecules (small molecules, proteins, peptides, nucleic acids, etc.). [0003] Ionic liquid (IL) usually refers to an organic salt with a melting point lower than 100 °C, which has excellent properties such as low vapor pressure, strong ability to dissolve substances, good conductivity, wide electrochemical window, and de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/22A61K47/02A61K31/192A61K31/337A61K31/704A61K45/00
CPCA61K9/5089A61K9/5015A61K9/501A61K45/00A61K31/704A61K31/192A61K31/337
Inventor 李建华沈兰波杨晓茹张彦笛刘小艺张亚萍徐文秀
Owner SHANDONG UNIV
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