CN116327635A - Natural permeation enhancer, preparation method, gel containing permeation enhancer and application of gel - Google Patents
Natural permeation enhancer, preparation method, gel containing permeation enhancer and application of gel Download PDFInfo
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- CN116327635A CN116327635A CN202310148513.6A CN202310148513A CN116327635A CN 116327635 A CN116327635 A CN 116327635A CN 202310148513 A CN202310148513 A CN 202310148513A CN 116327635 A CN116327635 A CN 116327635A
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- sodium alginate
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- -1 preparation method Substances 0.000 title claims abstract description 32
- 238000002360 preparation method Methods 0.000 title abstract description 10
- 235000010413 sodium alginate Nutrition 0.000 claims abstract description 68
- 239000000661 sodium alginate Substances 0.000 claims abstract description 68
- 229940005550 sodium alginate Drugs 0.000 claims abstract description 68
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims abstract description 39
- 239000002904 solvent Substances 0.000 claims abstract description 16
- 239000004480 active ingredient Substances 0.000 claims abstract description 10
- 150000004676 glycans Chemical class 0.000 claims abstract description 6
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 36
- JQWHASGSAFIOCM-UHFFFAOYSA-M sodium periodate Chemical compound [Na+].[O-]I(=O)(=O)=O JQWHASGSAFIOCM-UHFFFAOYSA-M 0.000 claims description 12
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 10
- 239000001110 calcium chloride Substances 0.000 claims description 10
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 10
- 239000008367 deionised water Substances 0.000 claims description 10
- 229910021641 deionized water Inorganic materials 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
- 239000002537 cosmetic Substances 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 7
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 4
- 238000006243 chemical reaction Methods 0.000 claims description 4
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- 229920001184 polypeptide Polymers 0.000 claims description 4
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- 238000000502 dialysis Methods 0.000 claims description 3
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- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 2
- 229910002651 NO3 Inorganic materials 0.000 claims description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims description 2
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- MHMNJMPURVTYEJ-UHFFFAOYSA-N fluorescein-5-isothiocyanate Chemical compound O1C(=O)C2=CC(N=C=S)=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 MHMNJMPURVTYEJ-UHFFFAOYSA-N 0.000 description 18
- 230000001186 cumulative effect Effects 0.000 description 10
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- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
- C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
- C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
- C08B37/0084—Guluromannuronans, e.g. alginic acid, i.e. D-mannuronic acid and D-guluronic acid units linked with alternating alpha- and beta-1,4-glycosidic bonds; Derivatives thereof, e.g. alginates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/042—Gels
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/20—Halogens; Compounds thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/733—Alginic acid; Salts thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Abstract
The invention discloses a natural permeation enhancer, a preparation method, gel containing the permeation enhancer and application of the gel. The permeation promoter is based on natural polysaccharide carbohydrate sodium alginate, and aldehyde sodium alginate is obtained through chemical modification; also provides a preparation method of the optimized aldehyde sodium alginate; finally, the gel of the natural permeation promoter is also disclosed, which comprises solution A and solution B, wherein the solution A comprises 1-3% of sodium alginate, 0.6-1.5% of aldehyde sodium alginate, 0.1-5% of functional active molecules and the balance of solvent; the solution B comprises 1-5% of calcium salt and the balance of solvent. The gel containing the penetration enhancer can promote the absorption of active ingredients, and the gel achieves remarkable skin care effect under extremely low dosage.
Description
Technical Field
The invention belongs to the technical field of preparation of cosmetic raw materials, and particularly relates to a natural permeation enhancer, a preparation method, gel containing the permeation enhancer and application of the gel.
Background
The application of active ingredients in cosmetics is becoming more and more popular, but because of the effect of skin barrier, many functional ingredients are difficult to penetrate through the stratum corneum of the skin and cannot have the effect on the effective parts, so that the skin barrier effect is overcome, the effective ingredients are promoted to enter the deep layer of the skin, and various physiological regulation effects are achieved on skin cells, so that the cosmetic is one of important means for improving the efficacy of the cosmetics. It is relatively common to increase the transdermal absorption rate of cosmetic polypeptides by means of physical permeation means of the apparatus and by adding certain permeation enhancers. However, the existing physical permeation-assisting method has the defects of high price, complicated use and the like, and the common chemical permeation-promoting agents such as azone, organic acid and the like are easy to cause skin allergy.
Therefore, developing a penetration enhancer which can be rapidly applied to skin care products and promote the absorption of functional components becomes a technical problem to be solved urgently.
In view of the above, the inventors have proposed a natural permeation enhancer, a preparation method, a gel containing the permeation enhancer and applications thereof, so as to solve the above technical problems.
Disclosure of Invention
The invention aims to solve the technical problem that the permeation promoting effect of chemical components is not obvious in the prior art, and provides a natural permeation promoting agent, a preparation method, gel containing the permeation promoting agent and application.
The technical problems to be solved by the invention are realized by the following technical scheme:
according to a first aspect of the invention, a novel natural permeation enhancer is provided, wherein the permeation enhancer is based on widely-available natural polysaccharide carbohydrate sodium alginate, and is subjected to chemical modification to obtain aldehyde sodium alginate; specifically, the aldehyde sodium alginate (SA-CHO) is obtained by oxidizing Sodium Alginate (SA) with sodium periodate.
In a second aspect of the present invention, there is provided an optimized process for preparing an aldehyde sodium alginate, comprising the steps of:
s1: dispersing 2 g of sodium alginate powder into 10ml of water-miscible organic solvent (one or more of methanol, ethanol, ethyl acetate, propanol and acetone), stirring for 30min, dissolving 1.08 g of sodium periodate in 10ml of water, dropwise adding into sodium alginate solution, and reacting for 8-24 h in dark place.
S2: after the reaction was completed, the obtained solution was transferred to a 3500 dalton dialysis bag and dialyzed in deionized water for 3 days.
S3: freeze drying to obtain aldehyde sodium alginate.
The invention also provides a gel containing the natural permeation enhancer, wherein the gel comprises A, B solutions, the solution A comprises 0.5-10% of sodium alginate, 0.25-2.5% of aldehyde sodium alginate, 0.1-2% of functional active ingredients and the balance of solvent deionized water according to weight percentage; the solution B comprises 1-5% of soluble salts such as chloride, nitrate, lactate, gluconate and the like of calcium and the balance of solvent deionized water; mixing the solution A and the solution B to form gel.
Further, the functional active ingredient (molecule) in the solution A is macromolecular polysaccharide, and one or a combination of a plurality of polypeptide substances;
preferably, in the solution A, the content of sodium alginate is preferably 2.0% by weight. Preferably, the content of the aldehyde sodium alginate is 1.0%, the active ingredient is 0.5%, and the balance is deionized water solvent;
further, in the solution A, the macromolecular polysaccharide is 0.5% of sodium hyaluronate, and the balance is deionized water solvent;
in a more preferred embodiment of the present invention, in the solution B of the gel formulation, the solution B specifically includes 4% by weight of calcium chloride, and the balance being deionized water solvent.
Furthermore, the gel containing the natural permeation enhancer is used as the permeation enhancer in cosmetics. Compared with the prior art, the invention has the beneficial effects that:
the natural permeation promoter, the preparation method, the gel containing the permeation promoter and the application provided by the invention have the following advantages:
1. the prepared aldehyde sodium alginate penetration enhancer can promote the absorption of active ingredients and does not cause damage to skin.
2. The aldehyde group in the aldehyde sodium alginate molecule in the gel prepared by the invention can react with amino residues of skin surface proteins to generate Schiff base, so that the gel is tightly attached to the skin, and an effective active molecule transmission channel between the gel and the skin is established.
3. The invention has the advantages of easily obtained raw materials, mild and safe formula, no stimulation to human body and accordance with industry standards; the process has strong practicability, can achieve remarkable skin care effect under extremely low dosage, and has wide application prospect in the field of cosmetics.
Drawings
The invention will be further described with reference to the drawings and the detailed description of the embodiments.
FIG. 1 shows infrared absorption peaks of the aldehyde sodium alginate generated at different reaction times in the invention;
FIG. 2 shows the method of using A, B of the invention to gel two solutions;
FIG. 3 is a graph showing the cumulative permeation of the novel permeation enhancers of the present invention for small fluorescent molecules at 15min,30 min time points; where A is a sample microscope photograph and B is a sample fluorescence intensity value.
FIG. 4 is a graph showing the cumulative permeation of the novel permeation enhancer of the present invention to fluorescent macromolecules at 15min and 30min time points; where A is a sample microscope photograph and B is a sample fluorescence intensity value.
Detailed Description
In order to make the technical problems, technical schemes and beneficial effects solved by the invention clearer, the invention is further described in detail below with reference to the accompanying drawings and embodiments. It is to be understood that the specific embodiments described herein are for purposes of illustration only and are not to be construed as limiting the invention, as described in detail below.
Example 1:
in the preparation process of the aldehyde sodium alginate, ethanol is selected as the organic solvent,selecting products with the reaction time of 30 minutes, 100 minutes and 300 minutes respectively, and comparing the positions of infrared absorption peak aldehyde groups of the products; FIG. 1 shows infrared absorption peaks of the sodium alginate aldehyde formed at different reaction times in the present invention, which is shown in FIG. 1 to be 1740cm compared with the spectrum of sodium alginate -1 The symmetrical vibration absorption peak of aldehyde carbonyl group which belongs to aldehyde group appears, and 3445cm in the figure -1 The change of the peaks indicates that the sodium alginate forms aldehyde groups after oxidation.
Example 2:
when the gel containing the natural permeation enhancer is prepared, the solution A comprises the following components in percentage by weight: sodium alginate 2.0%, aldehyde sodium alginate 0.5%, and the rest is solvent. And (3) uniformly smearing a proper amount of solution A on skin, spraying solution B, and immediately forming gel, wherein the solution B contains 4% of calcium chloride, and the balance is solvent.
The sodium alginate is from Qingdao sea forest company, and the solvent is deionized water.
Fig. 2 shows the method of using the two solutions A, B in the invention to gel, and as can be seen from fig. 2, the gel forming experiment test on human skin shows that the obtained solution A and solution B have gel forming effect.
Example 3:
when the gel containing the natural permeation enhancer is prepared, the solution A comprises the following components in percentage by weight: sodium alginate 2.0%, sodium alginate aldehyde 1%, sodium hyaluronate 0.5% and the balance of solvent. And (3) uniformly smearing a proper amount of solution A on skin, spraying solution B, and immediately forming gel, wherein the solution B contains 4% of calcium chloride, and the balance is solvent.
Example 4:
when the gel containing the natural permeation enhancer is prepared, the solution A comprises the following components in percentage by weight: sodium alginate 2.0%, aldehyde sodium alginate 0.5%, fluorescent active small molecule FITC0.5%, and water in balance; and (3) uniformly coating a proper amount of solution A on the skin, spraying solution B containing 3% of calcium chloride and 97% of water, and immediately forming gel.
And (3) permeability verification:
based on a milk pigskin-Franz cell system, the distribution of fluorescent marker substances in pigskin at different time points is observed through a fluorescence microscope, the change of the fluorescence intensity of a sample is counted, and the skin permeation behavior of the sample is evaluated.
The specific method for measuring the percutaneous absorption capacity comprises the following steps:
1) Firstly, fixing pigskin between a supply chamber and a receiving chamber of a Franz cell diffusion cell, wherein the skin cuticle of the pigskin faces the supply chamber and the dermis layer faces the receiving chamber;
2) Adding 7.0mL of receiving liquid into the receiving chamber, tightening and fixing pigskin, adding 1mL of receiving liquid (PBS) into the receiving chamber through a sampler, and exhausting air to enable the dermis layer of the skin to be in close contact with the receiving liquid;
3) Loading: the sample was applied to the skin surface in the supply chamber, with an effective penetration area S of about 3.14cm 2 . The sample was added to the surface of the pigskin and spread evenly from the center of the skin radially to the edge. 3 replicates and parallel (three replicates with individual donor specific sites of skin) per sample;
4) Penetration: starting an electromagnetic stirrer to stir at the speed of 300rpm, keeping a constant-temperature water bath at the temperature of (32+/-1) DEG C, and ensuring that a water bath interlayer is bubble-free;
5) Collecting skin samples at the time points of 15min and 30min, sucking PBS, cleaning the skin surface for 5 times, wiping off residual liquid on the surface with a cotton swab, cutting the skin with a blade ring, immersing in 4% paraformaldehyde solution for fixation (the fixation time is more than or equal to 24 h), and freezing for slicing for later use.
FIG. 3 shows the cumulative permeation quantity of the novel permeation enhancer to the fluorescent small molecule FITC at the time points of 15min and 30min, referring to FIG. 3, the control group is gel of SA+fluorescent active small molecule FITC, the solution A in the gel formula does not contain aldehyde sodium alginate, and the rest conditions are the same. From the results of fig. 3, it was demonstrated that the gel containing the aldehyde sodium alginate can more effectively promote the permeation of the active ingredient. Fluorescence microscopy observations of A in FIG. 3 show that permeation of sample SA+FITC fluorescent molecules, SA-CHO+FITC fluorescent molecules, and water+FITC fluorescent molecules occurs; the fluorescence intensity values at the time points of 15min and 30min in the B of the FIG. 3 show that the cumulative permeation amounts of SA+FITC fluorescent molecules, SA-CHO+FITC fluorescent molecules and water+FITC fluorescent molecules are all larger than the previous time point, namely, the sample permeation amount is continuously increased along with the time; the cumulative permeation quantity of the SA+FITC fluorescent molecules at the time points of 15min and 30min is obviously lower than that of the SA-CHO+FITC fluorescent molecules; the cumulative permeation of SA-CHO+FITC fluorescent molecules at 15min and 30min time points is significantly higher than that of water+FITC fluorescent molecules.
It is emphasized that: SA+FITC and SA-CHO+FITC are gels, which are different from each other in that (SA+FITC) gel does not contain the aldehyde sodium alginate penetrant component of the invention, and the gel component comprises: the solution A comprises 2.5% of sodium alginate, 0.5% of fluorescent active small molecule FITC and the balance of water; and (3) uniformly coating a proper amount of solution A on the skin, spraying solution B containing 3% of calcium chloride and 97% of water, and immediately forming gel. And (SA-CHO+FITC) gel comprising the aldehyde sodium alginate penetrant component of the invention; in the gel component, the solution A comprises 2.0% of sodium alginate, 0.5% of aldehyde sodium alginate, 0.5% of fluorescent active small molecule FITC and the balance of water; and (3) uniformly coating a proper amount of solution A on the skin, spraying solution B containing 3% of calcium chloride and 97% of water, and immediately forming gel.
Example 5:
a solution A of a highly-compatible skin smearing type self-crosslinking gel mask comprises the following components in percentage by weight: sodium alginate 2.0%, aldehyde sodium alginate 1%, fluorescent active macromolecular polypeptide-Cy 5.5%, and water in balance; and (3) uniformly coating a proper amount of solution A on pigskin, spraying solution B containing 1% of calcium chloride and 99% of water, and immediately forming gel.
And (3) permeability verification:
based on the milk pig skin-Franz cell system, the distribution of fluorescent marker substances in pig skin at different time points is observed through a fluorescence microscope, and the change of the fluorescence intensity of a sample is counted, so that the skin penetration behavior of the sample is evaluated, and the transdermal absorption capacity measurement method of the embodiment is the same as that of the embodiment 3.
FIG. 4 shows the cumulative permeation of the novel permeation enhancer of the present invention to the fluorescent macromolecular polypeptide-Cy 5 at 15min and 30min time points. The contrast group SA+fluorescent active macromolecules are that the solution A in the gel formula does not contain aldehyde sodium alginate, and the rest conditions are the same. The gel was left on the pigskin for 15min and rinsed off after 30 min. Fluorescence intensity was detected using a fluorescence microscope. As shown in FIG. 4A, the sample SA+polypeptide-Cy 5, SA-CHO+polypeptide-Cy 5, water+polypeptide-Cy 5 all underwent osmotic behavior; as shown in the B in FIG. 4, the fluorescence intensity values at the time points of 15min and 30min show that the cumulative permeation amounts of SA+polypeptide-Cy 5, SA-CHO+polypeptide-Cy 5 and water+polypeptide-Cy 5 are larger than that at the previous time point, namely, the sample permeation amount is continuously increased along with the time; importantly, the cumulative permeation of SA+polypeptide-Cy 5 at 15min and 30min time points is significantly lower than that of SA-CHO+polypeptide-Cy 5 and significantly higher than that of water+polypeptide-Cy 5; the cumulative permeation of SA-CHO+polypeptide-Cy 5 at 15min and 30min time points is significantly higher than that of water+polypeptide-Cy 5. Wherein the polypeptide is modified by myristoylation.
It is emphasized that: SA+ polypeptide-Cy 5, SA-CHO+ polypeptide-Cy 5, all represent gels.
Wherein, the SA+polypeptide-Cy 5 gel, the solution A comprises the following components: 3.0% of sodium alginate, 0.5% of fluorescent active macromolecular polypeptide-Cy, and the balance of water; and (3) uniformly coating a proper amount of solution A on pigskin, spraying solution B containing 1% of calcium chloride and 99% of water, and immediately forming gel.
SA-CHO+polypeptide-Cy 5 gel, solution A comprising the following components: sodium alginate 2.0%, aldehyde sodium alginate 1%, fluorescent active macromolecular polypeptide-Cy 5.5%, and water in balance; and (3) uniformly coating a proper amount of solution A on pigskin, spraying solution B containing 1% of calcium chloride and 99% of water, and immediately forming gel.
The foregoing is a further detailed description of the invention in connection with the preferred embodiments, and it is not intended that the invention be limited to the specific embodiments described. It will be apparent to those skilled in the art that several simple deductions or substitutions may be made without departing from the spirit of the invention, and these should be considered to be within the scope of the invention.
Claims (10)
1. The natural permeation enhancer is characterized by being aldehyde sodium alginate, and SA-CHO for short.
2. The natural permeation enhancer of claim 1, wherein said aldehyde sodium alginate is prepared by oxidizing sodium alginate with sodium periodate, said sodium alginate being abbreviated as SA.
3. The method for preparing the natural permeation enhancer according to claim 1-2, which is characterized by comprising the following steps:
s1: dispersing 2 g of sodium alginate powder into 10ml of water-miscible organic solvent, and stirring for 30 minutes to obtain sodium alginate solution;
then, 1.08 g of sodium periodate is dissolved in 10ml of water to obtain sodium periodate solution, the sodium periodate solution is added into sodium alginate solution drop by drop, and the reaction is carried out for 8 to 24 hours in a dark place;
s2: after the reaction is finished, transferring the solution obtained by the reaction into a 3500 Dalton dialysis bag, and dialyzing in deionized water for 3 days to obtain a dialysis product;
s3: freeze-drying the dialyzed product to obtain the aldehyde sodium alginate.
4. The method of claim 3, wherein in S2, the organic solvent comprises one or more of methanol, ethanol, ethyl acetate, propanol, and acetone.
5. The gel containing the natural permeation enhancer is characterized by comprising A, B two solutions, wherein the solution A comprises 0.5-10% of sodium alginate, 0.25-2.5% of aldehyde sodium alginate, 0.1-2% of functional active ingredient and the balance of solvent water according to weight percentage; the solution B comprises one or more of chloride, nitrate, lactate and gluconate of 1-5% of calcium, and the balance of solvent water; mixing the solution A and the solution B to form the gel.
6. The gel of claim 5, wherein the functional active ingredient in solution a is a macromolecular polysaccharide that is a combination of one or more polypeptides.
7. A natural permeation enhancer-containing gel according to claim 6, wherein in solution a, the sodium alginate is present in an amount of 2.0%, the aldehyde sodium alginate is present in an amount of 1.0%, the functional active ingredient is present in an amount of 0.5%, and the balance is water.
8. A natural permeation enhancer-containing gel according to claim 6, wherein in solution a, the macromolecular polysaccharide is 0.5% sodium hyaluronate, the remainder being deionized water solvent.
9. A natural permeation enhancer-containing gel according to claim 7, wherein the B solution comprises, by weight, 4% calcium chloride and the balance deionized water solvent.
10. Use of a gel comprising a natural penetration enhancer according to any one of claims 5 to 9 as a penetration enhancer in cosmetics.
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| CN202310148513.6A CN116327635A (en) | 2023-02-22 | 2023-02-22 | Natural permeation enhancer, preparation method, gel containing permeation enhancer and application of gel |
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| CN202310148513.6A CN116327635A (en) | 2023-02-22 | 2023-02-22 | Natural permeation enhancer, preparation method, gel containing permeation enhancer and application of gel |
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