Novel lipidosome targeted delivery cream containing tetrahydromethylpyrimidine carboxylic acid combined with ceramide and application of novel lipidosome targeted delivery cream

Abstract

The invention discloses novel liposome targeted delivery cream containing tetrahydromethylpyrimidine carboxylic acid and ceramide and application thereof. The novel liposome targeted delivery cream is mainly used for relieving skin problems such as skin sensitivity, dermatitis and eczema. According to the novel liposome, soybean lecithin, cholesterol and a polyethylene glycol-targeting ligand are combined, the targeting ligand is tetrahydromethylpyrimidine carboxylic acid, and the targeting liposome capable of simultaneously connecting and encapsulating hydrophilic tetrahydromethylpyrimidine carboxylic acid and hydrophobic ceramide is prepared. And further adding into a cream matrix to develop a novel liposome targeted delivery cream of compound hydromethylpyrimidine carboxylic acid combined with ceramide. The liposome has a phospholipid bilayer, is self-closed in structure, can entrap ceramide in the liposome, is good in stability, and is stably connected with water-soluble tetrahydromethylpyrimidine carboxylic acid for modification, so that the liposome is prevented from being quickly degraded, and the drug release speed is reduced. The nano-particles are added into a cream matrix and directly applied to a required skin part, so that targeted transportation of drugs in skin tissues can be realized.

Description

Technical Field

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

[0002] Ceramide is a biologically active sphingolipid composed of sphingosine and fatty acids. It is an important physiological lipid in the skin and is widely present in all eukaryotic cells. It plays an important regulatory role in life activities such as cell differentiation, proliferation, apoptosis, and aging. As the main component of intercellular lipids in the stratum corneum 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. Ectohydrogen methyl pyrimidine carboxylic acid is a cyclized amino acid derivative with good hydrophilicity. It can organize and bind to the surrounding water molecules and amino acid derivatives. Ectohydrogen methyl pyrimidine carboxylic acid not only has strong stress resistance and repair power, but also can effectively repair the skin barrier and reduce the discomfort of sensitive and irritated skin. Especially in terms of repairing and soothing sensitive skin, it can play a role in targeting inflammatory sites and has significant advantages. The combined use of ceramide and ectohydrogen methyl pyrimidine carboxylic acid can give full play to the synergistic effect of the two, thereby achieving better results in the treatment of skin sensitivity, dermatitis, eczema, etc.

[0003] Liposome technology uses natural phospholipid compounds to prepare nano-scale vesicles with a double-layer molecular structure. Liposomes have good safety and biodegradability, and have a similar cell membrane structure. They can effectively encapsulate water-soluble and fat-soluble 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. They have a strong affinity with cells, can enhance cell fluidity and permeability, promote the generation and recovery of epidermal cells, and promote cell metabolism.

[0004] Currently, the transdermal absorption effect of the combined use of ectoine and ceramide needs to be further improved. Summary of the invention

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

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

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

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

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

[0010] (1) dissolving ectoine in PEG3000, adding dropwise to PBS buffer solution with stirring for activation reaction, shaking and reacting overnight to obtain PEG3000-ectoine active ingredient for standby use;

[0011] (2) dissolving soybean lecithin, cholesterol and ceramide in an anhydrous ethanol solution, stirring by ultrasonication until dissolved, to obtain a ceramide lipid precursor solution;

[0012] (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.

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

[0014] As a further improvement of the present invention: the cream base comprises the following ingredients in parts by weight: 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 conditioning agent, 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 more than one of lanolin, isononyl isononanoate, beeswax, caprylic / capric triglyceride, squalane, polydimethylsiloxane, avocado butter and jojoba seed oil.

[0016] As a further improvement of the present invention: the emulsifier is one or a combination of more than one 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 acrylic acid (ester) / C10-30 alkyl acrylate crosslinked.

[0018] As a further improvement of the present invention: the moisturizing agent is one of glycerin, butylene glycol, 1,2-hexanediol, panthenol, and allantoin, or a combination of more than one of them.

[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 conditioning agent is one or a combination of multiple of a novel liposome of tetrahydromethylpyrimidine carboxylic acid combined with ceramide, bisabolol, β-glucan, wormwood leaf extract, Centella asiatica extract, oat extract and menthol lactate.

[0023] The present invention also includes the use of a novel liposome targeted delivery cream containing ectoine and ceramide in cosmetics for skin sensitivity, dermatitis and eczema.

[0024] The present invention also includes a method for preparing a novel liposome targeted delivery cream containing ectoine and ceramide, comprising the following steps: heating and melting an emollient and an emulsifier to form an oil phase, adding a moisturizer, a thickener, an auxiliary skin conditioning agent, a chelating agent, and an antioxidant into water, stirring the mixture evenly to form an aqueous phase, rapidly adding the oil phase into the aqueous phase under stirring, homogenizing, stirring at a constant temperature, and stirring at a reduced temperature until condensation occurs, thereby preparing a novel liposome targeted delivery cream containing ectoine and ceramide.

[0025] Compared with the prior art, the present invention has the following beneficial effects: the present invention provides a method for preparing a novel liposome targeted delivery cream containing ectoine carboxylic acid combined with ceramide, the liposome cream has good transdermal absorption effect, can significantly inhibit and treat skin problems such as skin sensitivity, dermatitis, eczema, and the like, and has significantly improved effects compared with conventional ectoine carboxylic acid or ceramide creams;

[0026] This new liposome is combined with soybean lecithin, cholesterol, polyethylene glycol-targeting ligand, and the targeting ligand is tetrahydromethylpyrimidine carboxylic acid to prepare a targeted liposome that can simultaneously connect and encapsulate hydrophilic tetrahydromethylpyrimidine carboxylic acid and hydrophobic ceramide. On this basis, it is further added to the cream matrix, and finally a new liposome targeted delivery cream of compound tetrahydromethylpyrimidine carboxylic acid combined with ceramide is developed. The liposome has a phospholipid bilayer and is self-enclosed in structure. Ceramide can be encapsulated inside the liposome, with good stability. At the same time, it can stably connect to water-soluble tetrahydromethylpyrimidine carboxylic acid for modification to prevent its rapid degradation and reduce the drug release rate. In addition, adding it to the cream matrix and applying it directly to the desired skin part can achieve targeted transportation of drugs in skin tissue. BRIEF DESCRIPTION OF THE DRAWINGS

[0027] In order to more clearly illustrate the technical solution, the drawings required for use in the implementation will be briefly introduced below. Obviously, the drawings described below are only some implementation methods of the present invention. For ordinary technicians in this field, other drawings can be obtained based on these drawings without paying creative labor.

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

[0029] In order to make the purpose, technical solution and advantages of the present invention clearer, the technical solution of the present invention will be clearly and completely described below in conjunction with the specific embodiments of the present invention and the corresponding drawings. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the present invention.

[0030] It should be noted that the terms "first", "second", etc. in the specification and claims of the present invention and the above-mentioned drawings are used to distinguish similar objects, and are not necessarily used to describe a specific order or sequence. It should be understood that the data used in this way can be interchanged where appropriate, so that the embodiments of the present invention described herein can be implemented in an order other than those illustrated or described herein. In addition, the terms "including" and "having" and any variations thereof are intended to cover non-exclusive inclusions, for example, a process, method, system, product or device that includes a series of steps or units is not necessarily limited to those steps or units that are clearly listed, but may include other steps or units that are 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 intercellular lipids in the stratum corneum of the skin, it has multiple functions such as maintaining the skin barrier, moisturizing, anti-aging, and whitening. Tetrahydromethylpyrimidine carboxylic acid is a hydrophilic cyclized amino acid derivative that has the effects of resisting stress and repairing the skin barrier. It is especially suitable for repairing sensitive skin and targeting inflammatory sites.

[0032] The combined use of the two can produce a synergistic effect and is more advantageous in treating skin sensitivity, dermatitis and eczema. Using liposome technology, the active ingredients can be effectively encapsulated and sustained-released through a double-layer nanovesicle structure, enhancing their stability and transdermal absorption effect. The cell affinity of liposomes helps improve cell metabolism and skin barrier function. However, how to further improve the transdermal absorption effect of the combined active ingredients remains a key research issue.

[0033] The ethanol injection method used in the embodiment to prepare liposomes is routine in the art.

[0034] Preparation Example 1:

[0035] preparing an ectoine carboxylic acid combined with ceramide liposome solution;

[0036] (1) 4 g of tetrahydromethylpyrimidine carboxylic acid was dissolved in 3 ml of PEG3000, and the mixture was added dropwise to 30 ml of PBS buffer having a pH of 7.4 under stirring for activation reaction. The mixture was shaken and reacted overnight to obtain PEG3000-tetrahydromethylpyrimidine carboxylic acid active ingredient for standby use;

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

[0038] (3) 10 ml of the ceramide lipid precursor solution was added dropwise to 20 ml of the PEG3000-ectoine active ingredient and heated and stirred on a magnetic stirrer until the ethanol was completely evaporated to form a translucent suspension, thereby obtaining an 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. 3 g of ceramide is added to the preparation system, and the amounts of other raw materials are the same as those in Preparation Example 1 to prepare an ectoine carboxylic acid 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. 6 g of ceramide is added to the preparation system, and the amounts of other raw materials are the same as those in Preparation Example 1 to prepare an ectoine carboxylic acid combined with ceramide liposome solution.

[0043] Preparation of the novel liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide of the present invention:

[0044] Implementation case 1:

[0045] The ingredients are as follows:

[0046]

[0047]

[0048] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, jojoba seed oil, acrylates / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutylene, and polydimethylsiloxane are heated and melted as the oil phase, and moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and the liposome solution of Preparation Example 1 are added to water and stirred evenly as the water phase, and the oil phase is added to the water phase under rapid stirring. After homogenization for 10 minutes, heat preservation and stirring for 30 minutes, and cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0049] Implementation case 2:

[0050] The ingredients are as follows:

[0051]

[0052] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, jojoba seed oil, acrylic acid (esters) / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutylene, and polydimethylsiloxane are heated and melted as the oil phase, moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and the liposome solution of Preparation Example 1 are added to water and stirred evenly as the water phase, and the oil phase is added to the water phase under rapid stirring. After homogenization for 10 minutes, heat-insulating and stirring for 30 minutes, and cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0053] Implementation case three:

[0054] The ingredients are as follows:

[0055]

[0056]

[0057] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, jojoba seed oil, acrylic acid (esters) / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutylene, and polydimethylsiloxane are heated and melted as the oil phase, moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and the liposome solution of Preparation Example 1 are added to water and stirred evenly as the water phase, and the oil phase is added to the water phase under rapid stirring. After homogenization for 10 minutes, heat-insulating and stirring for 30 minutes, and cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0058] Comparative Example 1:

[0059] The ingredients are as follows:

[0060]

[0061]

[0062] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, ceramide, jojoba seed oil, acrylates / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutene, and polydimethylsiloxane are heated and melted as the oil phase, moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and tetrahydromethylpyrimidine carboxylic acid are added to water and stirred evenly as the water phase, the oil phase is added to the water phase under rapid stirring, and after homogenization for 10 minutes, heat-insulating and stirring for 30 minutes, cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0063] Comparative Example 2:

[0064] The ingredients are as follows:

[0065]

[0066]

[0067] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, ceramide, jojoba seed oil, acrylates / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutene, and polydimethylsiloxane are heated and melted as the oil phase, moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and tetrahydromethylpyrimidine carboxylic acid are added to water and stirred evenly as the water phase, the oil phase is added to the water phase under rapid stirring, and after homogenization for 10 minutes, heat-insulating and stirring for 30 minutes, cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0068] Comparative Example 3:

[0069] The ingredients are as follows:

[0070]

[0071]

[0072] Preparation method: According to the weight shown in the above table, C14-22 alcohol, C12-20 alkyl glucoside, isononyl isononanoate, avocado esters, ceramide, jojoba seed oil, acrylates / C10-30 alkyl acrylate crosslinking, hydrogenated polyisobutene, and polydimethylsiloxane are heated and melted as the oil phase, moisturizers butylene glycol, glycerin, 1,2-hexanediol, xanthan gum, allantoin, trehalose, β-glucan, disodium EDTA, wormwood extract, Centella asiatica extract, and tetrahydromethylpyrimidine carboxylic acid are added to water and stirred evenly as the water phase, the oil phase is added to the water phase under rapid stirring, and after homogenization for 10 minutes, heat-insulating and stirring for 30 minutes, cooling and stirring for 60 minutes until condensation, a new liposome targeted delivery cream of tetrahydromethylpyrimidine carboxylic acid combined with ceramide is prepared.

[0073] The efficacy of the novel liposome targeted delivery cream of ectoine combined with ceramide prepared in the embodiment of the present invention was measured:

[0074] 1. Determination of sustained-release efficacy

[0075] The liposome skin care products prepared in Examples 1, 2, and 3 were used as the experimental group, and the non-liposome skin care products prepared in Comparative Examples 1, 2, and 3 were used as the control group. The Franz method was used to determine the in vitro transdermal rate, and the sustained-release efficacy of the experimental group and the control group was evaluated. The ex vivo skin of rats was used as the experimental skin sheet, and samples were taken 5 times within 24 hours, and the average value of 3 parallel times was taken. The results are shown in Table 1.

[0076] Table 1 Determination of sustained release efficacy

[0077]

[0078] As shown in Table 1, the release rate of the experimental group was efficient and sustained from 2h to 24h, and the release rate of the control group decreased significantly after the release peaked at 8h-16h, indicating that the liposome structure of the present invention can effectively help ectoine and ceramide to pass through the skin barrier, has a sustained release and sustained effect on the active ingredients therein, can prolong the action time of the active ingredients, and play a long-term targeting and anti-inflammatory role.

[0079] 2. Observation of Scratching Behavior of Mice

[0080] This experiment provides a certain pharmacological basis by establishing an atopic dermatitis (AD) model and observing the antipruritic effect of the test sample. There are 80 test model mice, which are randomly divided into eight groups, each test group has 10 mice, half male and half female, including a control group, a model group, an embodiment 1-3 treatment group, and a comparative example 1-3 treatment group. The neck and back of the mouse are depilated, with an area of ​​1.5cm*1.5cm. 100μL of 0.15% DNFB solution prepared with acetone is evenly applied to the skin of the neck and back of each mouse with a cotton swab. Continuous administration for 5d, 0.2ml / time, the back skin of the mouse forms erythema, edema, scratches, scales, epidermal exfoliation and other symptoms for successful modeling. After the model is stable, except for the blank group and the AD model group, the remaining groups begin to give the corresponding test substances, apply and administer for 10 days continuously, observe and record the recovery every day, and at the same time on the 0th, 5th, and 10th days of administration, 3 animals are randomly selected from the administration group for 15min scratching behavior observation. Antipruritic rate (%) = (number of scratching in the model group - number of scratching in the sample group) / number of scratching in the model group * 100%. The experimental results are shown in Table 2.

[0081] Table 2 Determination of itching rate

[0082]

[0083] As shown in Table 2, the AD mouse model has obvious itch symptoms. After the model was successfully established, the number of scratching in each group was very obvious. After administration of each group, the antipruritic rate of the mice was significantly increased, and the results were significantly better than those of Comparative Examples 1-3, indicating that the novel liposomes of tetrahydromethylpyrimidine carboxylic acid combined with ceramide in Examples 1-3 have a more significant inhibitory effect on the itch of AD mice, and the antipruritic effect of Examples 1-3 is positively correlated with the dose of the composition.

[0084] 3. Observation of skin tissue morphology of mice in each group:

[0085] In this experiment, an atopic dermatitis (AD) model was established. The modeling process was the same as the scratching test. Samples were collected 2 hours after the drug was given on the 10th day. After the mice were anesthetized and killed, the neck and back tissues were obtained 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 taken, and after dehydration, transparency, wax immersion, embedding, slicing, dewaxing, slicing, dewaxing, and HE staining, the pathological changes of the local skin of the mice were observed using a microscope imaging system. Five slices were selected for each tissue, and five fields of view were observed for each slice. Epidermal necrosis and dermal inflammatory cell infiltration were observed under a microscope. The results are as follows: Figure 1 shown.

[0086] Figure 1 .HE staining pictures

[0087] like Figure 1 It can be seen that the tissue morphological changes observed by HE staining 10 days after administration. The control group had a moderate intact epidermis thickness, the dermis collagen fibers were closely arranged, the hair follicles were evenly distributed and intact in structure, and there was no obvious inflammatory cell infiltration. The epidermis of the AD group was swollen and scarred, the dermis was heavily infiltrated with blood cells and inflammatory cells, the hair follicles were atrophied, and the collagen fibers were loosely distributed. For the comparative examples 1-3 groups of mice in the present invention, the inflammatory cell infiltration in the stratum corneum, subepidermis and dermis of the skin was improved compared with the control group. Although the dermal papillae were still visible, their number was relatively small. For Examples 1-3 of the present invention, the repair of the mouse skin after modeling was particularly significant, and the thickness of the epidermis was almost restored to normal levels.

[0088] The main functions of the present invention are:

[0089] 1) By combining soybean lecithin, cholesterol and polyethylene glycol-targeting ligand (ectoine), targeted liposomes that can simultaneously encapsulate hydrophilic ectoine and hydrophobic ceramide were prepared. The liposomes adopt a phospholipid bilayer structure, which can be self-enclosed, improve the stability of ceramide, and stably connect ectoine through surface modification to prevent its rapid degradation, further optimizing drug release performance.

[0090] 2) After the liposomes are incorporated into the cream matrix, they are directly applied to the skin to achieve targeted delivery of the drug in the skin tissue. The sustained-release properties of the liposomes reduce the rapid release rate of the drug, effectively prolong the action time of ectoine and ceramide, and enhance the long-term anti-inflammatory and targeted effects.

[0091] 3) Experimental data showed that the release rate of active ingredients in the experimental group was efficient and sustained from 2 hours to 24 hours. Compared with the control group, which showed a significant decrease in release rate after 8 to 16 hours, the liposome structure of the present invention achieved stable release of ingredients, significantly improved the efficiency of penetrating the skin barrier, and prolonged the effective action time of the active ingredients.

[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, eczema, etc. Compared with conventional ectoine or ceramide creams, the effect is significantly improved.

[0093] In summary, after reading the present invention document, ordinary technicians in this field can make various other corresponding transformation schemes based on the technical scheme and technical concept of the present invention without creative mental work, which all fall within the scope of protection of the present invention.

Claims

1. A novel liposome targeted delivery cream containing ectoine and ceramide, characterized in that: The invention comprises an ectoine carboxylic acid combined with a ceramide liposome solution and an ointment base, wherein the mass ratio of the ectoine carboxylic acid combined with a ceramide liposome solution to the ointment base is (0.5-1):

1.

2. A novel 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 from the following raw materials: phospholipid, cholesterol, PEG3000-ectoine carboxylic acid active ingredient, ceramide, anhydrous ethanol and liposome dispersion.

3. A novel liposome targeted delivery cream containing ectoine and ceramide according to claim 2, characterized in that: The PEG3000-tetrahydromethylpyrimidine carboxylic acid active ingredient is PEG3000-tetrahydromethylpyrimidine carboxylic acid.

4. A novel liposome targeted delivery cream containing ectoine and ceramide according to claim 3, 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 PBS buffer solution 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.

5. A novel liposome targeted delivery cream containing ectoine and ceramide according to claim 2, characterized in that: The liposome dispersion liquid is PBS buffer.

6. A novel 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.

7. A novel liposome targeted delivery cream containing ectoine and ceramide according to claim 6, 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.

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

9. The novel liposome targeted delivery cream containing ectoine and ceramide according to claim 6, characterized in that: The auxiliary skin conditioning agent is one or a combination of multiple of the novel liposomes of tetrahydromethylpyrimidine carboxylic acid combined with ceramide, bisabolol, beta-glucan, wormwood leaf extract, centella asiatica extract, oat extract and hydromenthol lactate.

10. Use of a novel liposome targeted delivery cream containing ectoine and ceramide as claimed in any one of claims 1 to 9 in cosmetics for skin sensitivity, dermatitis and eczema.

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