CN-117224481-B - Food-grade O/W quercetin microemulsion, and preparation method and application thereof

Abstract

The invention discloses a food-grade O/W quercetin microemulsion, and a preparation method and application thereof, wherein the food-grade O/W quercetin microemulsion comprises, by weight, 10% -42% of a surfactant, 2% -32% of an oil phase solution and the balance of a water phase, wherein the oil phase solution comprises isopropyl myristate and ethanol, and the weight ratio of the isopropyl myristate to the ethanol=1:1-4. The O/W microemulsion has simple preparation method, is an excellent carrier of active substances or functional substances with poor stability and water solubility represented by quercetin, and thus improves the stability of the active substances or functional substances in a pharmaceutical preparation and improves the slow release behavior of the active substances or functional substances.

Inventors

• YAN XIUHUA
• ZHANG JUN
• XU WEI
• SHAO RONG
• DING JIANFEI
• SHI WENYAN
• ZHANG YIDONG
• XU YAYING

Assignees

• 盐城工学院

Dates

Publication Date

20260508

Application Date

20231103

Claims (1)

1. 1. A food-grade O/W quercetin microemulsion is characterized in that the raw material formula is as follows: 0.151g of quercetin, which is prepared from the components of the total amount of quercetin, EL-35 30g, 13.5G of ethanol, and the weight of the ethanol, 6.5G of isopropyl myristate, 50G of water, and the water content is equal to or higher than the water content, The preparation method comprises the following steps: Mixing ethanol and isopropyl myristate to obtain an oil phase solution, adding EL-35 into a mixing kettle placed in a water bath at 55 ℃ under the condition of uninterrupted stirring by a magnetic stirrer at the rotating speed of 250 rpm, adding water into the oil phase solution, adjusting the pH of the solution to 7.4, adding excessive quercetin, stirring to dissolve, centrifuging and filtering to obtain a clear and transparent solution; the obtained quercetin microemulsion has the following characteristics: (1) Transparent or semitransparent, colorless or pale yellow liquid; (2) The average particle diameter is 232nm; (3) Drug release the cumulative release rate of the quercetin microemulsion over 24 hours was 47%.

Description

Food-grade O/W quercetin microemulsion, and preparation method and application thereof Technical Field The invention belongs to the field of pharmaceutics, and particularly relates to food-grade O/W quercetin microemulsion, and a preparation method and application thereof. Background A microemulsion is a dispersion of two immiscible liquids, one of which is dispersed in the other in the form of tiny droplets. Microemulsions have many advantages such as high bioavailability, high solubility, high stability, low toxicity, etc., and thus have wide application in the fields of pharmaceuticals, cosmetics, etc. The oil-in-water (O/W) microemulsion is a microemulsion which takes oil as a disperse phase and water as a continuous phase, can effectively wrap bioactive substances, protect the bioactive substances from the influence of external environment, and prolong the action time of the bioactive substances. Oil-in-water microemulsions generally require the addition of hydrophilic emulsifiers to reduce the surface tension of the water-oil interface, promoting the formation and stabilization of the microemulsion. Quercetin is a naturally occurring flavonoid compound and has various biological activities such as antioxidation, anti-inflammatory, antibacterial, anti-tumor and the like. Quercetin has low solubility in water, and its application in pharmaceuticals and cosmetics is limited. Therefore, the use of oil-in-water microemulsions to support quercetin is an effective method to increase the solubility and bioavailability of quercetin. At present, the quercetin is mainly modified or encapsulated by a preparation carrier at home and abroad to solve the problems that the quercetin Pi Suyi is oxidized and insoluble in water and the like. For example, in patent CN105534897a, flos Sophorae Immaturus is used as raw material to prepare quercetin, and the quercetin is modified, and then mixed with the prepared blank microemulsion to obtain high water-solubility quercetin microemulsion by ultrasonic vibration. Ma Juanjuan et al prepared quercetin composite colloidal particles and stabilized Pickering emulsion delivery systems based on interactions between zein and polysaccharides, phospholipids and polyphenols. The solubility and photo-thermal stability of the quercetin are obviously improved. (Ma Juanjuan; study of the biological Activity and bioavailability of quercetin delivery vehicles constructed based on zein, doctor's laboratory paper, university of North China, 2021, 4:1-179.). However, these methods have complicated preparation processes and high cost. Disclosure of Invention Aiming at the defects of the prior art, the invention provides the oil-in-water quercetin microemulsion and the preparation method thereof, and the problem of low solubility and poor bioavailability of the quercetin is solved by using a microemulsion technology to prepare the quercetin oil-in-water microemulsion, so that the stability and the drug effect of the quercetin oil-in-water microemulsion are improved. The emulsion has good stability and sustained release performance, and can effectively improve the solubility and bioavailability of quercetin. In order to achieve the above purpose, the technical scheme adopted by the invention is as follows: The food-grade O/W quercetin microemulsion comprises a blank microemulsion composed of a surfactant, an oil phase solution and an aqueous phase, and the blank microemulsion is a carrier encapsulated quercetin microemulsion, wherein the oil phase solution comprises oil and a cosurfactant; the quercetin microemulsion has the following characteristics: (1) Transparent or semitransparent, colorless or pale yellow liquid; (2) The average grain diameter is 200-300 nm; (3) The pH value is 6.0-8.0; (4) The medicine content is 0.4 mg/g-1.51 mg/g; (5) The drug release is that the accumulated release rate of the quercetin microemulsion is 25% -47% within 24 hours. Specifically, the quercetin is a flavonoid compound, and the chemical name of the quercetin is 3,3',4',5, 7-pentahydroxy flavonoid. Specifically, the surfactant is any one of an emulsifier EL-35, tween-80 and an emulsifier OP, and the emulsifier EL-35 is preferred. EL-35 is a nonionic surfactant, has the chemical name of polyoxyethylene-35 stearyl alcohol ether, has the characteristics of low toxicity, low irritation, low conductivity and the like, can effectively reduce the surface tension of the microemulsion and the repulsive force between micelles, and improves the stability and the solubilization capacity of the microemulsion. Specifically, the oil is selected from any one of peanut oil, isopropyl myristate, ethyl butyrate and ethyl n-octoate, preferably isopropyl myristate, and the chemical name of the oil is isopropyl myristate. Isopropyl myristate is a non-volatile or low-volatile oil, has good biocompatibility and safety, and can effectively avoid loss and deterioration of the drug caused by volatilization or oxidation of the oil during