A liposome-targeted delivery cream containing ectoine and ceramide and its application

By using new liposomes containing tetrahydromethylpyrimidine carboxylic acid and ceramide in the cream, the problem of poor transdermal absorption of tetrahydromethylpyrimidine carboxylic acid and ceramide in the prior art has been solved, and more efficient skin targeted delivery and long-term anti-inflammatory effects have been achieved.

CN119280146BActive Publication Date: 2025-07-01XINYAN BIOTECHNOLOGY (TAIZHOU) CO LTD
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Patent Information

Application Number
CN202411700231.3
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-11-26
Publication Date
2025-07-01
Estimated Expiration
2044-11-26

AI Technical Summary

Technical Problem

In the prior art, the transdermal absorption effect of tetrahydromethylpyrimidine carboxylic acid combined with ceramide needs to be further improved.

Method used

A new liposome targeted delivery cream containing tetrahydromethylpyrimidine carboxylic acid and ceramide was prepared by combining soy lecithin, cholesterol and polyethylene glycol-targeting ligands, and targeted liposomes that can encapsulate hydrophilic tetrahydromethylpyrimidine and hydrophobic ceramides were used to prepare and incorporate them into the cream matrix.

Benefits of technology

It significantly improves the transdermal absorption effect of tetrahydromethylpyrimidine carboxylic acid and ceramide, extends the action time of active ingredients, and enhances the treatment effect on skin sensitivity, dermatitis and eczema.

✦ Generated by Eureka AI based on patent content.

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Abstract

A novel liposome-targeted delivery cream containing ectoine and ceramide and its application, mainly used for relieving skin problems such as skin sensitivity, dermatitis, eczema, etc.; the novel liposome combines soybean lecithin, cholesterol, polyethylene glycol-targeting ligand, and the targeting ligand is ectoine to prepare a targeted liposome capable of simultaneously connecting and encapsulating hydrophilic ectoine and hydrophobic ceramide; further added to the cream matrix to develop a novel liposome-targeted delivery cream of compound ectoine combined with ceramide; it has a phospholipid bilayer and is self-closed in structure, can encapsulate ceramide inside the liposome, has good stability, and at the same time stably connects and modifies water-soluble ectoine to prevent its rapid degradation and reduce the drug release rate. Adding it to the cream matrix and directly applying it to the required skin area can achieve targeted transport of the drug in the skin tissue.
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Description

Technical Field

[0001] The present invention relates to the technical field of daily chemical products, in particular to a novel liposome-targeted delivery cream containing ectoine combined with ceramide and its application. Background Art

[0002] Ceramide is a biologically active sphingolipid composed of sphingosine and fatty acids. It is an important physiological lipid in the skin, widely present in all eukaryotic cells, and plays an important regulatory role in life activities such as cell differentiation, proliferation, apoptosis, and aging. As the main component of the intercellular lipid in the stratum corneum cells of the skin, ceramide plays a key role in the formation of the epidermal stratum corneum, and has multiple functions such as maintaining the skin barrier, soothing, moisturizing, anti-aging, whitening, and disease treatment. Ectoine is a cyclic amino acid derivative with good hydrophilicity, which can organize and bind the surrounding water molecules and amino acid derivatives. Ectoine not only has strong anti-stress and repair capabilities, but also can effectively repair the skin barrier, reduce the discomfort of sensitive and irritated skin, especially in the repair and soothing of sensitive skin, and can play a role in targeting inflammatory sites, with significant advantages. The combined use of ceramide and ectoine can give full play to the synergistic effect of the two, so as to achieve better results in the treatment of skin sensitivity, dermatitis, eczema, etc.

[0003] Liposome technology uses natural phospholipid compounds to prepare nanoscale vesicles with a bilayer molecular structure. Liposomes have good safety and biodegradability, have a structure similar to the cell membrane, can effectively encapsulate water-soluble and lipophilic active ingredients, and have protective, transporting, and sustained-release effects on active ingredients. The main component of liposomes is natural phospholipids, which are the basic scaffolds of biological cell membranes, have a strong affinity with cells, can enhance the fluidity and permeability of cells, promote the generation and recovery of epidermal cells, and promote cell metabolism.

[0004] At present, for the transdermal absorption effect of the combined use of ectoine and ceramide, the transdermal absorption effect still needs to be further improved. Summary of the Invention

[0005] In order to overcome the above-mentioned disadvantages of the prior art, the purpose of the present invention is to provide a novel liposome-targeted delivery cream containing ectoine combined with ceramide and its application.

[0006] The technical solution adopted by the present invention to solve its technical problems is: a novel liposome-targeted delivery cream containing ectoine combined with ceramide, characterized in that it includes an ectoine combined with ceramide liposome solution and a cream matrix, wherein the mass ratio of the ectoine combined with ceramide liposome solution to the cream matrix is (0.5 - 1):1.

[0007] As a further improvement of the present invention: the ectoine combined with ceramide liposome solution is prepared from the following raw materials: phospholipids, cholesterol, PEG3000-ectoine active ingredient, ceramide, absolute ethanol and liposome dispersion.

[0008] As a further improvement of the present invention: the PEG3000-ectoine active ingredient is PEG3000-ectoine.

[0009] As a further improvement of the present invention: the ectoine combined with ceramide liposome solution is prepared by the following method:

[0010] (1) Dissolve ectoine in PEG3000, and drop it into PBS buffer under stirring for activation reaction, and shake the reaction overnight to obtain PEG3000-ectoine active ingredient for standby;

[0011] (2) Dissolve soybean lecithin, cholesterol and ceramide in absolute ethanol solution, and stir ultrasonically until dissolved to obtain ceramide lipid precursor solution;

[0012] (3) Drop the ceramide lipid precursor solution into the PEG3000-ectoine active ingredient, and heat and stir on a magnetic stirrer until the ethanol evaporates completely to form a translucent suspension, namely the ectoine combined with ceramide liposome solution.

[0013] As a further improvement of the present invention: the liposome dispersion is PBS buffer.

[0014] As a further improvement of the present invention: the cream matrix contains the following components in parts by mass: 20-100 parts of emollient, 50-100 parts of emulsifier, 20-50 parts of humectant, 1-5 parts of thickener, 200-300 parts of auxiliary skin conditioner, 1-10 parts of chelating agent, 10-50 parts of antioxidant, and the balance is deionized water.

[0015] As a further improvement of the present invention: the emollient is one or a combination of lanolin, isononyl isononanoate, beeswax, caprylic / capric triglyceride, squalane, polydimethylsiloxane, shea butter and jojoba seed oil.

[0016] As a further improvement of the present invention: the emulsifier is one or a combination of C14-22 alcohol, C12-20 alkyl glucoside, behenyl alcohol, arachidyl alcohol, arachidyl glucoside and cetearyl glucoside.

[0017] As a further improvement of the present invention: the self-thickening emulsifier is a crosslinking of acrylic acid (ester) / C10-30 alkanol acrylate.

[0018] As a further improvement of the present invention: the humectant is one or a combination of glycerin, butanediol, 1,2-hexanediol, panthenol, and allantoin.

[0019] As a further improvement of the present invention: the thickener is xanthan gum.

[0020] As a further improvement of the present invention: the antioxidant is trehalose.

[0021] As a further improvement of the present invention: the chelating agent is disodium EDTA.

[0022] As a further improvement of the present invention: the auxiliary skin conditioner is one or a combination of a novel liposome of ectoine combined with ceramides, bisabolol, β-glucan, Artemisia argyi extract, Centella asiatica extract, Avena sativa extract, and menthol lactate.

[0023] The present invention also includes the application of a novel liposome-targeted delivery cream containing ectoine combined with ceramides in skin-sensitive, dermatitis, and eczema cosmetics.

[0024] The present invention also includes a preparation method of a novel liposome-targeted delivery cream containing ectoine combined with ceramides, comprising the following steps: heating and melting an emollient and an emulsifier as the oil phase, adding a humectant, a thickener, an auxiliary skin conditioner, a chelating agent, and an antioxidant to water, stirring evenly as the water phase, adding the oil phase to the water phase under rapid stirring, and subjecting to homogenization, heat-preserving stirring, and cooling stirring until condensation to prepare a novel liposome-targeted delivery cream containing ectoine combined with ceramides.

[0025] Compared with the prior art, the beneficial effects of the present invention are: the present invention provides a preparation method of a novel liposome-targeted delivery cream containing ectoine combined with ceramides, the liposome cream has a good transdermal absorption effect, can significantly inhibit and treat skin problems such as skin sensitivity, dermatitis, and eczema, and has a significantly improved effect compared with conventional ectoine or ceramide cream agents;

[0026] The present novel liposome is prepared by combining soybean lecithin, cholesterol, polyethylene glycol-targeting ligand, and the targeting ligand is ectoine, to prepare a targeting liposome that can simultaneously link and encapsulate hydrophilic ectoine and hydrophobic ceramide. On this basis, it is further added to the cream matrix, and finally a novel liposome-targeted delivery cream combining ectoine and ceramide is developed. The liposome has a phospholipid bilayer and is self-closed in structure, which can encapsulate ceramide inside the liposome, has good stability, and at the same time stably links and modifies water-soluble ectoine to prevent its rapid degradation and reduce the drug release rate. In addition, when it is added to the cream matrix and directly applied to the required skin area, it can achieve targeted transport of the drug in the skin tissue. Brief Description of the Drawings

[0027] In order to more clearly illustrate the technical solution, the drawings required for the embodiments will be briefly introduced below. Obviously, the drawings in the following description are only some embodiments of the present invention. For those of ordinary skill in the art, without creative efforts, other drawings can be obtained based on these drawings.

[0028] Figure 1 This is a HE staining picture of the neck and back tissue of the atopic dermatitis (AD) model in the embodiment of the present invention. Detailed Embodiments

[0029] To make the objectives, technical solutions, and advantages of the present invention clearer, the technical solutions of the present invention will be clearly and completely described below in conjunction with the specific embodiments and corresponding drawings of the present invention. Obviously, the described embodiments are only some embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative efforts belong to the scope of protection of the present invention.

[0030] It should be noted that the terms "first", "second", etc. in the description and claims of the present invention and the above drawings are used to distinguish similar objects, and do not necessarily need to describe a specific order or sequence. It should be understood that such data can be interchanged under appropriate circumstances so that the embodiments of the present invention described here can be implemented in an order other than those illustrated or described here. In addition, the terms "comprising" and "having" and any variations thereof are intended to cover non-exclusive inclusion. For example, a process, method, system, product, or device that includes a series of steps or units does not necessarily have to be limited to those steps or units clearly listed, but may include other steps or units not clearly listed or inherent to these processes, methods, products, or devices.

[0031] Ceramide is a bioactive sphingolipid composed of sphingosine and fatty acids. As an important component of the intercellular lipids in the stratum corneum of the skin, it has multiple functions such as maintaining the skin barrier, moisturizing, anti-aging, and whitening. Ectoine is a hydrophilic cyclic amino acid derivative, which has the effects of anti-stress and repairing the skin barrier, and is especially suitable for the repair of sensitive skin and the treatment of targeted inflammatory sites.

[0032] Combining the two can exert a synergistic effect and has more advantages in the treatment of skin sensitivity, dermatitis, and eczema. Using liposome technology, the active ingredients can be effectively encapsulated and slowly released through the bilayer nanovesicle structure, enhancing their stability and transdermal absorption effect. The cell affinity of liposomes helps to improve cell metabolism and skin barrier function. However, how to further enhance the transdermal absorption effect of the combined active ingredients remains a key issue in research.

[0033] The method of preparing liposomes by ethanol injection used in the implementation cases is conventional in this field.

[0034] Preparation Example 1:

[0035] Prepare an ectoine combined with ceramide liposome solution;

[0036] (1) Dissolve 4 g of ectoine in 3 ml of PEG3000, and drop it into 30 ml of PBS buffer solution with a pH of 7.4 during stirring for activation reaction. Shake the reaction overnight to obtain the PEG3000-ectoine active ingredient for later use;

[0037] (2) Dissolve 4 g of soybean lecithin, 1 g of cholesterol, and 1 g of ceramide in 14 ml of anhydrous ethanol solution, and stir ultrasonically until dissolved to obtain a ceramide lipid precursor solution;

[0038] (3) Drop 10 ml of the ceramide lipid precursor solution into 20 ml of the PEG3000-ectoine active ingredient, and heat and stir on a magnetic stirrer until the ethanol evaporates completely to form a translucent suspension, namely the ectoine combined with ceramide liposome solution.

[0039] Preparation Example 2:

[0040] The preparation method and raw materials are the same as those in Preparation Example 1. Add 3 g of ceramide to the preparation system, and the dosage of the remaining raw materials is the same as that in Preparation Example 1 to prepare an ectoine combined with ceramide liposome solution.

[0041] Preparation Example 3:

[0042] The preparation method and raw materials are the same as those in Preparation Example 1. Add 6 g of ceramide to the preparation system, and the dosage of the remaining raw materials is the same as that in Preparation Example 1 to prepare an ectoine combined with ceramide liposome solution.

[0043] Preparation of a novel liposome-targeted delivery cream of ectoine combined with ceramide according to the present invention:

[0044] Example 1:

[0045] The raw materials are as follows:

[0046]

[0047]

[0048] Preparation method: According to the weights shown in the above table, heat and melt C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, shea butter, jojoba seed oil, acrylate / C10-30 alkanol acrylate crosslinking, hydrogenated polyisobutene, and polydimethylsiloxane to form an oil phase. Add the humectants butylene glycol, glycerol, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, Artemisia argyi extract, Centella asiatica extract, and the liposome solution of Preparation Example 1 to water, stir evenly to form an aqueous phase, and add the oil phase to the aqueous phase under rapid stirring. After homogenization for 10 min, heat-preserving stirring for 30 min, and cooling stirring for 60 min until condensation, a novel liposome-targeted delivery cream of ectoine combined with ceramide is prepared.

[0049] Example 2:

[0050] The raw materials are as follows:

[0051]

[0052] Preparation method: According to the weights shown in the above table, heat and melt C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, shea butter, jojoba seed oil, acrylate / C10-30 alkanol acrylate crosslinking, hydrogenated polyisobutene, and polydimethylsiloxane to form an oil phase. Add the humectants butylene glycol, glycerol,, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, Artemisia argyi extract, Centella asiatica extract, and the liposome solution of Preparation Example 1 to water, stir evenly to form an aqueous phase, and add the oil phase to the aqueous phase under rapid stirring. After homogenization for 10 min, heat-preserving stirring for 30 min, and cooling stirring for 60 min until condensation, a novel liposome-targeted delivery cream of ectoine combined with ceramide is prepared.

[0053] Example 3:

[0054] The raw materials are as follows:

[0055]

[0056]

[0057] Preparation method: According to the weights shown in the above table, heat and melt C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, shea butter fruit extract, jojoba seed oil, acrylate / C10-30 alkanol acrylate cross-linked polymer, hydrogenated polyisobutene, and polydimethylsiloxane to form an oil phase. Add the humectants butanediol, glycerol, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, Artemisia argyi extract, and Centella asiatica extract, and the liposome solution of Preparation Example 1 to water, stir evenly to form an aqueous phase. Add the oil phase to the aqueous phase under rapid stirring, and after homogenization for 10 min, heat preservation and stirring for 30 min, and cooling and stirring for 60 min until condensation, to prepare a novel liposome-targeted delivery cream of ectoine combined with ceramide.

[0058] Comparative Example 1:

[0059] The raw materials are as follows:

[0060]

[0061]

[0062] Preparation method: According to the weights shown in the above table, heat and melt C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, shea butter fruit extract, ceramide, jojoba seed oil, acrylate / C10-30 alkanol acrylate cross-linked polymer, hydrogenated polyisobutene, and polydimethylsiloxane to form an oil phase. Add the humectants butanediol, glycerol, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, Artemisia argyi extract, and Centella asiatica extract, and ectoine to water, stir evenly to form an aqueous phase. Add the oil phase to the aqueous phase under rapid stirring, and after homogenization for 10 min, heat preservation and stirring for 30 min, and cooling and stirring for 60 min until condensation, to prepare a novel liposome-targeted delivery cream of ectoine combined with ceramide.

[0063] Comparative Example 2:

[0064] The raw materials are as follows:

[0065]

[0066]

[0067] Preparation method: According to the weights shown in the above table, heat and melt C14 - 22 alcohol, C12 - 20 alkyl glucoside, isononyl isononanoate, shea butter fruit extract, ceramide, jojoba seed oil, acrylate / C10 - 30 alkanol acrylate cross - linked polymer, hydrogenated polyisobutene, and polydimethylsiloxane as the oil phase. Add the humectants butylene glycol, glycerin, 1,2 - hexanediol, xanthan gum, allantoin, trehalose, β - glucan, disodium EDTA, Artemisia argyi extract, Centella asiatica extract, and ectoine into water, stir evenly as the water phase. Add the oil phase into the water phase under rapid stirring, and after homogenization for 10 min, heat - preservation stirring for 30 min, and cooling stirring for 60 min until condensation, a novel liposome - targeted delivery cream of ectoine combined with ceramide is prepared.

[0068] Comparative Example 3:

[0069] The raw materials are as follows:

[0070]

[0071]

[0072] Preparation method: According to the weights shown in the above table, heat and melt C14 - 22 alcohol, C12 - 20 alkyl glucoside, isononyl isononanoate, shea butter fruit extract, ceramide, jojoba seed oil, acrylate / C10 - 30 alkanol acrylate cross - linked polymer, hydrogenated polyisobutene, and polydimethylsiloxane as the oil phase. Add the humectants butylene glycol, glycerin, 1,2 - hexanediol, xanthan gum, allantoin, trehalose, β - glucan, disodium EDTA, Artemisia argyi extract, Centella asiatica extract, and ectoine into water, stir evenly as the water phase. Add the oil phase into the water phase under rapid stirring, and after homogenization for 10 min, heat - preservation stirring for 30 min, and cooling stirring for 60 min until condensation, a novel liposome - targeted delivery cream of ectoine combined with ceramide is prepared.

[0073] Perform efficacy determination on the novel liposome - targeted delivery cream of ectoine combined with ceramide prepared in the implementation cases of the present invention:

[0074] I. Sustained - release efficacy determination

[0075] Take the liposome skin care products prepared in Examples 1, 2, and 3 as the experimental groups, and the non - liposome skin care products prepared in Comparative Examples 1, 2, and 3 as the control groups. Use the Franz method to measure the in vitro transdermal rate, evaluate the sustained - release efficacy of the experimental groups and the control groups. Use the excised skin of rats as the experimental skin pieces, take samples 5 times within 24 h, and take the average value in parallel 3 times. The results are shown in Table 1.

[0076] Table 1 Sustained - release efficacy determination

[0077]

[0078] As can be seen from Table 1, from 2h to 24h, the release rate of the experimental group was high and continuous. After the release rate of the control group peaked at 8h - 16h, it decreased significantly, indicating that the liposome structure of the present invention can effectively help ectoine and ceramide penetrate the skin barrier, has a sustained-release and continuous effect on the active ingredients therein, can extend the action time of the active ingredients, and plays a role in long-term targeted positioning and anti-inflammation.

[0079] II. Observation of scratching behavior in mice

[0080] In this experiment, an atopic dermatitis (AD) model was established to observe the antipruritic effect of the test samples and provide certain pharmacological basis. There were 80 test model mice, which were randomly divided into eight groups, with 10 mice in each test group, half male and half female, including a control group, a model group, treatment groups of Examples 1 - 3, and treatment groups of Comparative Examples 1 - 3. The hair on the necks and backs of the mice was removed, with an area of 1.5 cm * 1.5 cm. A 0.15% DNFB solution prepared with acetone was evenly applied to the skin on the necks and backs of each mouse with a cotton swab, and the drug was administered continuously for 5 days, 0.2 ml each time. The successful modeling was based on symptoms such as erythema, edema, scratches, scale coverage, and epidermal exfoliation on the back skin of the mice. After the model was stable, except for the blank group and the AD model group, the remaining groups began to administer the corresponding test substances and continuously applied the drugs for 10 days. The recovery situation was observed and recorded every day. At the same time on the 0th, 5th, and 10th days of drug administration, 3 animals were randomly selected from the drug administration groups for a 15-minute observation of scratching behavior. The antipruritic rate (%) = (the number of scratching times in the model group - the number of scratching times in the sample group) / the number of scratching times in the model group * 100%. The experimental results are shown in Table 2.

[0081] Table 2 Determination of antipruritic rate

[0082]

[0083] As can be seen from Table 2, the AD mouse model had obvious itching symptoms. After the successful modeling of each group, the number of scratching times was very obvious. After each group was administered the drug, the antipruritic rate of the mice increased significantly, and the results were significantly better than those of Comparative Examples 1 - 3, indicating that the novel liposome of ectoine combined with ceramide in Examples 1 - 3 had a more significant inhibitory effect on the itching of AD mice, and the antipruritic effect of Examples 1 - 3 was positively correlated with the dose of the composition.

[0084] III. Observation of skin tissue morphology of each group of mice:

[0085] In this experiment, an atopic dermatitis (AD) model was established. The modeling process was the same as that of the scratching test. After the drugs were administered on the 10th day, samples were taken 2 hours later. After the mice were anesthetized and sacrificed, the tissue on the neck and back was taken and stored in 10% neutral formaldehyde at 4°C for HE staining. Staining process: The back skin of the mice placed in 4% paraformaldehyde was dehydrated, cleared, infiltrated with wax, embedded, sectioned, dewaxed, sectioned, dewaxed, and HE stained. Then, the pathological changes of the local skin of the mice were observed with a microscope imaging system. Five sections were selected from each tissue, and five fields of view were observed for each section. The epidermal necrosis and dermal inflammatory cell infiltration were observed under the microscope. The results are as Figure 1 shown.

[0086] Figure 1 .HE staining pictures

[0087] As Figure 1 can be seen, the morphological changes of the tissues observed by HE staining 10 days after drug administration. In the control group, the epidermal layer was intact with a moderate thickness, the collagen fibers in the dermal layer were arranged tightly, the hair follicles were evenly distributed and the structure was intact, and there was no obvious inflammatory cell infiltration. In the AD group, the epidermal layer was swollen and showed scars, there was a large infiltration of blood cells and inflammatory cells in the dermal layer, the hair follicles were atrophied, and the collagen fibers were loosely distributed. For the mice in Comparative Examples 1-3 of the present invention, the inflammatory cell infiltration in the stratum corneum, the lower epidermis and the dermal layer of the skin was improved compared with the control group. Although the dermal papillae were still visible, the number was relatively small. For Examples 1-3 of the present invention, the repair of the mice skin after modeling was particularly remarkable, and the thickness of the epidermal layer almost returned to the normal level.

[0088] The main functions of the present invention:

[0089] 1) By combining soybean lecithin, cholesterol and polyethylene glycol-targeting ligand (ectoine), a targeted liposome capable of encapsulating hydrophilic ectoine and hydrophobic ceramide simultaneously was prepared. The liposome adopts a phospholipid bilayer structure, can self-close, improve the stability of ceramide, and is stably connected with ectoine through surface modification to prevent its rapid degradation, further optimizing the drug release performance.

[0090] 2) After integrating the liposome into the cream matrix and directly applying it to the skin, targeted delivery of the drug in the skin tissue can be achieved. The slow-release property of the liposome reduces the rapid release rate of the drug, effectively prolongs the action time of ectoine and ceramide, and enhances the long-term anti-inflammatory and targeted positioning effects.

[0091] 3) Experimental data show that within the range from 2 hours to 24 hours, the release rate of the active ingredient in the experimental group is high and continuous. Compared with the control group where the release rate significantly decreases after 8 hours to 16 hours, the liposome structure of the present invention achieves stable release of the ingredients, significantly improves the efficiency of penetrating the skin barrier, and extends the effective action time of the active ingredient.

[0092] 4) The novel liposome cream of the present invention has good transdermal absorption effect and can significantly inhibit and treat skin problems such as skin sensitivity, dermatitis, and eczema. Compared with conventional ectoine or ceramide creams, the effect is significantly improved.

[0093] In summary, after reading the documents of the present invention, various other corresponding transformation schemes made by those of ordinary skill in the art without creative mental labor based on the technical solutions and technical concepts of the present invention all fall within the scope protected by the present invention.

Claims

1. A liposome targeted delivery cream containing ectoine and ceramide, characterized in that: The invention comprises an ectoine carboxylic acid combined with ceramide liposome solution and an ointment base, wherein the mass ratio of the ectoine carboxylic acid combined with ceramide liposome solution to the ointment base is (0.5-1):1; the ectoine carboxylic acid combined with ceramide liposome solution is prepared by using the following raw materials: phospholipid, cholesterol, PEG3000-ectoine carboxylic acid active ingredient, ceramide, anhydrous ethanol and liposome dispersion; the PEG3000-ectoine carboxylic acid active ingredient is PEG3000-ectoine carboxylic acid.

2. A liposome targeted delivery cream containing ectoine and ceramide according to claim 1, characterized in that: The ectoine carboxylic acid combined with ceramide liposome solution is prepared by the following method: (1) dissolving ectoine in PEG3000, adding dropwise to the liposome dispersion with stirring for activation reaction, shaking and reacting overnight to obtain PEG3000-ectoine active ingredient for standby use; (2) dissolving soybean lecithin, cholesterol and ceramide in an anhydrous ethanol solution, stirring by ultrasonication until dissolved, to obtain a ceramide lipid precursor solution; (3) The ceramide lipid precursor solution is added dropwise to the PEG3000-ectoine active ingredient and heated and stirred on a magnetic stirrer until the ethanol is completely evaporated to form a translucent suspension, thereby obtaining an ectoine combined with ceramide liposome solution.

3. A liposome targeted delivery cream containing ectoine and ceramide according to claim 1, characterized in that: The liposome dispersion liquid is PBS buffer.

4. The liposome targeted delivery cream containing ectoine and ceramide according to claim 1, characterized in that: The cream base comprises the following components in parts by weight: 20-100 parts of an emollient, 50-100 parts of an emulsifier, 20-50 parts of a moisturizer, 1-5 parts of a thickener, 200-300 parts of an auxiliary skin conditioning agent, 1-10 parts of a chelating agent, 10-50 parts of an antioxidant, and the balance is deionized water.

5. A liposome targeted delivery cream containing ectoine and ceramide according to claim 4, characterized in that: The emollient is one or a combination of more than one of lanolin, isononyl isononanoate, beeswax, caprylic / capric triglyceride, squalane, polydimethylsiloxane, shea butter and jojoba seed oil.

6. The liposome targeted delivery cream containing ectoine and ceramide according to claim 5, characterized in that: The moisturizing agent is one or a combination of multiple of glycerin, butylene glycol, 1,2-hexanediol, panthenol and allantoin.

7. The liposome targeted delivery cream containing ectoine and ceramide according to claim 4, characterized in that: The auxiliary skin conditioning agent is one or a combination of ectoine combined with ceramide liposome, bisabolol, β-glucan, wormwood leaf extract, Centella asiatica extract, oat extract and hydromenthol lactate.

8. Use of a liposome targeted delivery cream containing ectoine and ceramide as claimed in any one of claims 1 to 7 in the preparation of cosmetics.

Citation Information

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