CN-122005337-A - Tranexamic acid ionic liquid, microcapsule, and preparation methods and applications thereof

Abstract

The application discloses an tranexamic acid ionic liquid, a microcapsule, a preparation method and application thereof, and relates to the field of daily chemical products. The ionic liquid comprises a tranexamic acid hydrogen bond donor and a hydrogen bond acceptor, wherein the hydrogen bond acceptor comprises at least one of citric acid, glycolic acid and malic acid, and the microcapsule is prepared by mixing grease, an emulsifying agent, tranexamic acid ionic liquid and water at a specific temperature and homogenizing. According to the application, the tranexamic acid is used as a hydrogen bond donor to prepare the ionic liquid, so that the solubility of the tranexamic acid is improved, meanwhile, the effect of the ionic liquid in water is realized by combining the emulsifying agent, the grease and the water, the efficient permeation of whitening components in skin can be promoted, the whitening effect is enhanced, meanwhile, the irritation is reduced, the prepared microcapsule has smaller particle size, the storage and the temperature resistance stability of the whitening active components are high, the encapsulation rate of the active components is obviously improved, the permeability, the stability and the safety of the tranexamic acid are comprehensively improved, and the whitening effect is good.

Inventors

• WANG XIAODONG
• WANG QI
• WU CHENGYU
• HAN HONGTAO

Assignees

• 上海优斐斯生物科技有限公司

Dates

Publication Date

20260512

Application Date

20260303

Claims (10)

1. 1. The tranexamic acid ionic liquid is characterized by comprising a hydrogen bond donor and a hydrogen bond acceptor in a molar ratio of (1-10): (1-10), wherein the hydrogen bond donor is tranexamic acid, and the hydrogen bond acceptor comprises at least one of citric acid, glycolic acid and malic acid.
2. 2. The tranexamic acid ionic liquid according to claim 1, wherein when the hydrogen bond acceptor is glycolic acid, the molar ratio of the hydrogen bond donor to the hydrogen bond acceptor is (1-3): 1-10; And/or, when the hydrogen bond acceptor is citric acid and/or malic acid, the molar ratio of the hydrogen bond donor to the hydrogen bond acceptor is (1-10): 1-10.
3. 3. The tranexamic acid ionic liquid according to claim 1, wherein the molar ratio of the hydrogen bond donor to the hydrogen bond acceptor is (1-2): 1-4.
4. 4. A method for preparing the tranexamic acid ionic liquid according to any one of claims 1 to 3, which is characterized by comprising the steps of mixing a hydrogen bond donor and a hydrogen bond acceptor, sealing, heating and stirring in a water bath device at 40-90 ℃ for 20-120 min, and cooling to room temperature to obtain the ionic liquid.
5. 5. A process for the preparation of tranexamic acid-containing microcapsules, characterized in that tranexamic acid ionic liquids according to any one of claims 1 to 3 are used, comprising the steps of: S1, mixing grease, an emulsifying agent and the tranexamic acid ionic liquid, uniformly stirring at the temperature of 70-75 ℃ to obtain a phase A, and uniformly stirring water to obtain a phase B; s2, dropwise adding the phase A into the phase B under the stirring condition, uniformly stirring to obtain a mixed solution, and homogenizing the mixed solution at the temperature of 70-75 ℃ to obtain the microcapsule.
6. 6. The method for preparing the tranexamic acid-containing microcapsule according to claim 5, wherein the oil accounts for 1-20% of the mass fraction of the microcapsule; and/or, the emulsifier accounts for 2-8% of the mass fraction of the microcapsule; and/or, the tranexamic acid ionic liquid accounts for 1-20% of the mass fraction of the microcapsule.
7. 7. The method for producing tranexamic acid-containing microcapsules according to claim 5, wherein in S1, the oil or fat comprises at least one of olive oil, grape seed oil, camellia oil, squalane, jojoba oil, shea butter, and lachryma-joba oil; And/or the emulsifier comprises at least one of soybean phospholipid, tween 80, tolocham, polyglycerol-3 methyl glucose distearate, PEG-40 hydrogenated castor oil, steareth-2, inulin lauryl carbamate, behenyl alcohol, polysorbate-60, PEG-15 glycerol laurate, glycerol stearate.
8. 8. A tranexamic acid-containing microcapsule prepared by the method for preparing a tranexamic acid-containing microcapsule according to any one of claims 5 to 7.
9. 9. Use of the tranexamic acid-containing microcapsule according to claim 8 in the field of whitening products.
10. 10. A whitening formulation comprising the tranexamic acid-containing microcapsule according to claim 8.

Description

Tranexamic acid ionic liquid, microcapsule, and preparation methods and applications thereof Technical Field The invention relates to the field of daily chemical products, in particular to an tranexamic acid ionic liquid, a microcapsule, a preparation method and application thereof. Background The cuticle, the water-soluble lipid protective layer and the cell membrane of the skin form natural barriers of the skin, and once the barrier functions are damaged, the skin is easy to lose moisture, and the problems of dryness, darkness and the like occur. Besides basic moisturizing, whitening and brightening have become important requirements in the field of skin care, and efficient, safe and stable whitening raw materials are receiving more and more market attention. The tranexamic acid is used as a common whitening active ingredient, has the effects of inhibiting melanin generation and improving darkness of skin color, but has low transdermal absorption efficiency, poor stability in illumination and high-temperature environment, and is easy to degrade, so that the whitening effect of the tranexamic acid is influenced. In addition, the tranexamic acid has high polarity and extremely strong water solubility, and can easily escape to an external water phase in the conventional emulsifying microcapsule system such as oil-in-water or water-in-oil, so that the encapsulation efficiency is low, the drug leakage is easy to occur, and the efficient slow release and targeted embedding are difficult to realize. Meanwhile, when tranexamic acid is singly used, certain irritation may exist on skin, and the wide application of tranexamic acid in cosmetics is limited. Therefore, how to improve the solubility, stability and transdermal absorption efficiency of tranexamic acid and reduce the irritation of tranexamic acid becomes a key to expand the application of tranexamic acid in whitening cosmetics. Ionic liquids are stable mixtures of two or more chemical species that form a liquid state at room temperature by physical interactions. It is formed mainly by the non-covalent action of functional groups between compounds, such as ionic bonds, intermolecular hydrogen bonds, van der Waals forces, etc. Ionic liquids do not change their chemical properties relative to the precursor, but some physical properties change, such as melting point, viscosity, state, vapor pressure, etc. Such non-covalently formed species are generally referred to as supramolecular species, and thus ionic liquids are also referred to as supramolecular solvents or supramolecular ionic liquids. The supermolecule ionic liquid has a plurality of excellent properties, has the advantages of low potential toxicity, high safety, proper price and the like by replacing an organic solvent in a plurality of fields, has the promotion effect on substance dissolution and efficacy, has the characteristics of enhancing the solubility of active substances, improving the efficacy of the active substances and the like, and has wide application in the fields of cosmetics, health care products, foods and the like. The ionic liquid can be used to the greatest/optimal extent by selecting the specific functional structural monomer, so that the selection of the proper monomer can produce a synergistic effect which is critical to the selection of the precursor monomer of the ionic liquid. The tranexamic acid generally has the effects of whitening, anti-inflammatory and the like, and the ligand monomer with a specific structure is selected to form the ionic liquid with the tranexamic acid, and the ionic liquid is applied to the fields of cosmetics, health-care foods and the like, so that the development of the tranexamic acid ionic liquid synergistic product has great significance. Disclosure of Invention The invention provides an ionic liquid of tranexamic acid, a microcapsule, a preparation method and application thereof, wherein tranexamic acid is used as a hydrogen bond donor to prepare the ionic liquid, so that the fat solubility of the tranexamic acid is improved, and simultaneously, the microcapsule with a nano structure is utilized to increase the transdermal rate and stability of the tranexamic acid, ensure the effective absorption of the tranexamic acid and the physical and chemical stability of the tranexamic acid, thereby prolonging the whitening effect and the service life of the product. In order to solve the technical problems, one of the purposes of the invention is to provide a tranexamic acid ionic liquid which comprises a hydrogen bond donor and a hydrogen bond acceptor in a molar ratio of (1-10): (1-10), wherein the hydrogen bond donor is tranexamic acid, and the hydrogen bond acceptor comprises at least one of citric acid, glycolic acid and malic acid. According to the application, the tranexamic acid is used as a hydrogen bond donor, a specific hydrogen bond acceptor is utilized, the specific molar ratio of the hydrogen bond donor to the hydrogen bond acceptor is c