Unlock instant, AI-driven research and patent intelligence for your innovation.

Beta-caryophyllene transdermal absorption enhancer and application of beta-caryophyllene transdermal absorption enhancer in external preparations and cosmetics

A technology of absorption enhancer and external preparation, applied in the field of biomedicine, can solve the problem of high cytotoxicity, achieve the effect of strong promoting ability, improving effect, and promoting the penetration of skin stratum corneum barrier

Active Publication Date: 2021-08-27
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Terpenoids are a large class of natural transdermal absorption accelerators, which have the characteristics of strong penetration-promoting ability, high safety and fragrant smell. Skin absorption enhancers, sesquiterpenes such as nerolidol have also been reported as transdermal absorption enhancers, but it is generally believed that sesquiterpenes have higher skin cytotoxicity than monoterpenes, so their applications are relatively seldom

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Beta-caryophyllene transdermal absorption enhancer and application of beta-caryophyllene transdermal absorption enhancer in external preparations and cosmetics
  • Beta-caryophyllene transdermal absorption enhancer and application of beta-caryophyllene transdermal absorption enhancer in external preparations and cosmetics
  • Beta-caryophyllene transdermal absorption enhancer and application of beta-caryophyllene transdermal absorption enhancer in external preparations and cosmetics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1 Fourier transform attenuated total reflection infrared spectrometry (ATR-FTIR) measures the effect on skin stratum corneum

[0015] Cut the rat skin to about 1 cm 2 The small pieces were placed in 5% 1,8-cineole, 5% β-caryophyllene or 5% azone solution, and the solvent was propylene glycol:isopropanol (3:7, v / v). The solvent-treated skin samples were used as the solvent group, and the untreated skin samples were used as the blank group. They were placed at 37°C for 36 hours, and then the treated skin samples were washed with distilled water and dried with filter paper. Infrared spectra of skin samples were obtained using an ATR-FTIR spectrometer. Infrared detection conditions: resolution 2cm -1 , an average of 64 scans, the scan range is 650-4000cm -1 . Table 1 shows the infrared spectrum parameters of rat skin treated with different transdermal absorption enhancers (PE).

[0016] Table 1 Infrared spectrum parameters of skin samples treated with β-cary...

Embodiment 2

[0021] Embodiment 2 skin resistance dynamics measurement

[0022] The rat skin was taken out and thawed naturally at room temperature, and hydrated in PBS solution for 1 h, and fixed on a 24-well nested plate with the cuticle facing upward. Add 650 μL of PBS solution to the receiving chamber, add 200 μL blank solvent to the supply chamber, and read the initial value of skin resistance after equilibrating at 37°C for 2 minutes, which is recorded as SER 0 . Remove the upper layer of the skin solution, add 200 μL of the test solution (containing 5% transdermal absorption enhancer), read the skin resistance value at different time points, and record it as SER t . All of the above solutions were maintained at the desired temperature.

[0023] The resistance reduction factor (RF), defined as the initial SER 0 with the resistor value SER at a predetermined time t Ratio. The calculation is as follows: RF=SER 0 / SER t . The value of RF is plotted against time t, and the slope ...

Embodiment 3

[0024] Embodiment 3 skin cytotoxicity assay

[0025] Human keratinocyte HaCaT was prepared in DMEM medium (containing 10% fetal bovine serum and 100 U·mL -1 penicillin-streptomycin solution) at 37°C in a concentration of 5% CO 2 in the incubator. MTT experiment procedure: Take HaCaT cells in the logarithmic growth phase to make a single cell suspension, adjust the cell concentration (5000 cells / well), inoculate in a 96-well culture plate, set 5 replicate wells in each group, and store in 5% CO 2 and cultured overnight at 37°C. The medium was aspirated and discarded, and 100 μL of transdermal penetration enhancer solutions with different concentrations were added, and the solvent was DMEM medium containing 1% dimethyl sulfoxide (DMSO). The culture was continued for 12 h at 37°C. Remove the medium, add 150 μL of DMSO solution, shake and dissolve for 10 minutes, detect the absorbance (A) of each well at 570 nm with a microplate reader, and calculate the cell survival rate, IC...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

In order to solve the technical problems that existing chemical synthetic transdermal penetration enhancers such as azone and oleic acid are not high in transdermal penetration enhancing performance, part of varieties have peculiar smell and the like, the invention provides a natural transdermal absorption enhancer-beta-caryophyllene (CAS: 87-44-5), which has the characteristics of being high in penetration enhancing capacity, high in safety, fragrant in smell and the like. The researches show that the interference effect of the beta-caryophyllene on the skin barrier is obviously better than that of a classical chemical transdermal absorption enhancer azone and the most common monoterpene transdermal absorption enhancer 1, 8-cineole, and particularly, the beta-caryophyllene can obviously promote macromolecular polar substances and micromolecular polar substances to penetrate through the skin cuticle barrier, The transdermal effect of active ingredients of cosmetics or external preparations is remarkably improved, so that the efficacy is remarkably improved; the optimal addition concentration during application is 0.5-10%; in addition, the skin cytotoxicity of the beta-caryophyllene is obviously lower than that of azone, the skin irritation is lower than that of azone, and the safety is superior to that of a chemical transdermal penetration enhancer. The results show that the beta-caryophyllene is the ideal natural transdermal penetration enhancer and can be used in external preparations and cosmetic formulas.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to β-caryophyllene as a transdermal absorption accelerator, and its application in cosmetics and external preparations to promote the absorption of active ingredients. Background technique [0002] The skin has a strong barrier function, especially its stratum corneum lipid, which constitutes the most important material basis of the skin barrier. Therefore, for most active ingredients in topical preparations or cosmetics, it is difficult to achieve therapeutically effective concentrations through the skin. The application of transdermal absorption enhancers is by far the most commonly used, the most economical and the easiest method to improve transdermal absorption of external preparations or cosmetics. A series of chemically synthesized transdermal absorption enhancers have been developed, such as azone, oleic acid, etc., but Its transdermal function needs to be further impr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/06A61K9/00A61K8/31A61Q19/00
CPCA61K47/06A61K9/0014A61K8/31A61Q19/00A61K2800/10Y02A50/30
Inventor 陈军顾薇顾琦苏曼
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE