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Phloretin liposome and preparation method thereof

A technology of phloretin and lipid, which is applied in the direction of liposome delivery, anti-toxic agent, digestive system, etc., to achieve good stability, promote the absorption of phloretin, and expand the scope of development and application

Inactive Publication Date: 2016-12-21
INT HEALTHCARE INNOVATION INST JIANGMEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The improvement of liposome preparation methods, the separation and enrichment methods and the development of application fields are in the ascendant at home and abroad.

Method used

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  • Phloretin liposome and preparation method thereof
  • Phloretin liposome and preparation method thereof
  • Phloretin liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The effect of the ratio of soybean lecithin to cholesterol, the ratio of drug to lipid and the ratio of oil to water on the encapsulation efficiency was studied. Get 4 clean test tubes, get respectively prescription amount soybean lecithin, cholesterol, phloretin, dichloromethane, sodium dodecylsulfonate and phosphate buffer, prepare liposome according to the method of above-mentioned embodiment 2, electron micrograph and The encapsulation rate is shown in the accompanying drawings (see Figure 1-4). It can be seen that the shape of the liposome is relatively round and nearly spherical. Table 1 shows the effects of different fat-to-biliary ratios on the investigated prescriptions, Table 2 shows the effects of different drug-to-lipid ratios on the investigated prescriptions, and Table 3 shows the effects of different oil-to-water ratios on the investigated prescriptions. Table 1 shows the effects of different fat-to-biliary ratios on the investigated prescriptions, Tab...

Embodiment 2

[0047] Weigh 1 g of phloretin, 30.0 g of soybean lecithin, 3.0 g of cholesterol, 10 mL of dichloromethane, and 0.25 g of tocopherol to dissolve to obtain an organic phase; another 250 mL of 0.5% sodium dodecylsulfonate phosphate buffer solution (pH6.8) , to be dissolved or dispersed to obtain the water phase; Pour the organic phase into the water phase, oscillate and disperse, and place it in a cell pulverizer for ultrasonic treatment for 30 minutes to obtain an O / W emulsifier. After exhaustion, a transparent white opalescent liposome solution can be obtained; phloretin liposomes with white opalescent light can be obtained by sterilizing through a 0.8 μm filter membrane. The prepared liposome phloretin has a concentration of 0.5 mg / mL and an encapsulation efficiency of 55%.

Embodiment 3

[0049] Weigh 20mg phloretin, 375mg soybean lecithin, 75mg cholesterol, add 10mL dichloromethane to dissolve to obtain an organic phase; take another 30mL 2% sodium dodecylsulfonate acetate buffer solution (pH 6.8), after dissolving or dispersing Obtain the water phase; pour the organic phase into the water phase, oscillate and disperse, place a cell pulverizer and ultrasonically treat for 30 minutes to obtain an O / W emulsifier, place it in a water bath at a temperature of 55°C, stir and evaporate to dryness, and after the organic phase is completely evaporated, a transparent The liposome solution with white opalescence; the phloretin liposome with white opalescence after sterilization through a 0.8 μm filter membrane. The concentration of the prepared liposome phloretin is 5 mg / mL, and the encapsulation efficiency is 90%.

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Abstract

The present invention relates to the field of chemical industry, particularly to a phloretin liposome and a preparation method thereof, wherein the phloretin liposome comprise 0.2-20 mg / mL of phloretin, 4-95% of phospholipid, 2-60% of cholesterol, and 0-90% of other auxiliary materials, wherein the phloretin liposome is prepared by using a stirring method, an ultrasonic dispersion method, a high-pressure homogenization method, a micro-jet dispersion method, a thin-film dispersion method, an injection method and a two-emulsification method. According to the preset invention, the prepared liposome has characteristics of high encapsulation efficiency, good stability, phloretin solubility improving, phloretin absorption promoting, targeting delivery, phloretin bioactivity improving, phloretin application scope expanding, and good social and economic values.

Description

technical field [0001] The invention relates to the field of chemical engineering, in particular to a phloretin liposome and a preparation method thereof. Background technique [0002] Phloretin (phloretin) is a natural plant compound containing dihydrochalcones. It is mainly distributed in the peels and root barks of juicy fruits such as apples and pears, as well as in various vegetable juices. Domestic and foreign studies have shown that phloretin has a wide range of pharmacological activities such as anti-inflammation, immunity, anti-oxidation, anti-cardiovascular disease, anti-diabetes, anti-tumor and liver protection, and is a potential active ingredient with broad application prospects. Phloretin is used in cosmetics such as facial masks, skin care creams, and essences because of its activities such as lightening spots, whitening, acne, anti-mutagenic, and anti-aging. Mizuma et al. found that phloretin can inhibit the effect of glucuronidation, promote the absorption...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/12A61P29/00A61P37/02A61P9/00A61P39/06A61P3/10A61P35/00A61P1/16
CPCA61K9/1277A61K31/12
Inventor 何燕陈晓珊杨健妮林惠琼江森韩雷武文敬程书朋张焜郑希杜志云
Owner INT HEALTHCARE INNOVATION INST JIANGMEN
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