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KR-20260064823-A - Galactose-coated exosomes with improved stability, antioxidant and anti-inflammatory effects and their uses

KR20260064823AKR 20260064823 AKR20260064823 AKR 20260064823AKR-20260064823-A

Abstract

The present invention relates to galactose-coated exosomes with improved stability and uses thereof. More specifically, the present invention relates to galactose-coated exosomes with improved dispersion stability and storage stability, comprising a first coating layer made of chitosan present on the exosomes and a second coating layer made of galactose present on the first coating layer, and uses thereof, for example, in antioxidants, anti-inflammatory agents, pharmaceutical compositions, quasi-drug compositions, cosmetic compositions or food compositions.

Inventors

  • 최원일
  • 오혜련
  • 손판모

Assignees

  • 한국세라믹기술원

Dates

Publication Date
20260508
Application Date
20241029

Claims (16)

  1. Exosome, A first coating layer existing on the exosome and composed of chitosan, and An exosome with improved stability comprising a second coating layer composed of galactose present on the first coating layer.
  2. In paragraph 1, An exosome with improved stability, characterized in that the weight ratio of the exosome to chitosan is 1:0.1 to 5.
  3. In paragraph 1, An exosome with improved stability, characterized in that the weight ratio of the exosome to galactose is 1:1 and the content is 100.
  4. In paragraph 1, An exosome with improved stability, characterized in that the weight ratio of the exosome, chitosan, and galactose is 1:2:2 to 20.
  5. An antioxidant comprising, as an active ingredient, an exosome with improved stability according to any one of paragraphs 1 to 4.
  6. An anti-inflammatory agent comprising, as an active ingredient, an exosome with improved water solubility according to any one of paragraphs 1 to 5.
  7. A pharmaceutical composition for the prevention or treatment of diseases caused by excessive production of reactive oxygen species, comprising as an active ingredient exosomes with improved water solubility according to any one of claims 1 to 4.
  8. In Paragraph 7, A pharmaceutical composition characterized in that the disease caused by the excessive generation of the above-mentioned reactive oxygen species is stroke, Parkinson's disease, Alzheimer's disease, aging, heart disease, eye disease, ischemia, arteriosclerosis, skin disease, asthma, inflammation, arthritis, autoimmune disease, hyperlipidemia, liver disease, diabetes, cancer, chronic ulcer, burn, or wound.
  9. A quasi-drug composition for the prevention or treatment of diseases caused by excessive production of reactive oxygen species, comprising as an active ingredient exosomes with improved water solubility according to any one of claims 1 to 4.
  10. In Paragraph 9, A quasi-drug composition characterized in that the above-mentioned quasi-drug composition is a disinfectant cleaner, shower foam, mouthwash, wet wipe, detergent soap, hand wash, humidifier filler, mask, ointment, or filter filler.
  11. A cosmetic composition for preventing or improving symptoms or diseases caused by excessive production of reactive oxygen species, comprising as an active ingredient exosomes with improved water solubility according to any one of claims 1 to 4.
  12. In Paragraph 11, A cosmetic composition characterized in that the symptoms or diseases caused by the above-mentioned active oxygen are skin aging, wrinkle formation, skin pigmentation, atopy, acne, psoriasis, or eczema.
  13. In Paragraph 11, A cosmetic composition characterized by the above cosmetic being manufactured in the form of an ampoule, cream, lotion, toner, essence, or pack.
  14. A topical skin composition for promoting wound healing or skin regeneration, comprising as an active ingredient an exosome with improved water solubility according to any one of claims 1 to 4.
  15. A food composition for the prevention or improvement of symptoms or diseases caused by reactive oxygen species, comprising as an active ingredient exosomes with improved water solubility according to any one of claims 1 to 4.
  16. In paragraph 15, A food composition characterized in that the symptoms or diseases caused by the above-mentioned active oxygen are skin aging, wrinkle formation, skin pigmentation, atopy, acne, psoriasis, or eczema.

Description

Galactose-coated exosomes with improved stability, antioxidant and anti-inflammatory effects and their uses The present invention relates to galactose-coated exosomes with improved stability, antioxidant and anti-inflammatory effects, and uses thereof. More specifically, the present invention relates to galactose-coated exosomes with improved stability, antioxidant and anti-inflammatory effects, a first coating layer present on the exosomes and composed of chitosan, and a second coating layer present on the first coating layer and composed of galactose, and uses thereof, for example, in antioxidants, anti-inflammatory agents, pharmaceutical compositions, quasi-drug compositions, cosmetic compositions, or food compositions. Exosomes refer to small membrane-bound vesicles secreted by various cells and are defined as a type of extracellular vesicle (EV). All cells exchange information with other cells or the external environment and secrete extracellular vesicles for this purpose. Exosomes range in size from approximately 50 to 200 nm and contain physiologically active substances such as proteins, lipids, and nucleic acids. Exosomes exist in various cells, including mammals, bacteria, and plants, and can be utilized in diagnosis and treatment as they reflect the state of the cells of origin. As double-phospholipid membrane structures, exosomes facilitate intracellular penetration and perform various physiological and pathological functions, such as immune responses and signal transduction. Recently, research on the various efficacies of exosomes has been conducted, and studies on their skin benefits, such as antioxidant and anti-inflammatory effects, are also beginning. Due to their various advantages and activities, exosomes are materials that can be utilized in fields such as pharmaceuticals, cosmetics, and food. However, despite these diverse advantages and applications, their use is limited due to their structural characteristics as phospholipid bilayers, which result in low dispersibility and a tendency to aggregate. Furthermore, they are unstable at high temperatures and can easily break during the manufacturing process of cosmetic formulations; these properties can reduce the stability of exosomes within the formulation and cause precipitation. Therefore, to maintain continuous activity, it is necessary to improve the stability within the formulation by increasing the dispersibility of exosomes in aqueous solutions. Prior art 1. 10-2022-0019228 A (2022.02.16) Figure 1 shows (A) size, (B) dispersion value, and (C) surface charge of galactose-coated exosomes (G-Exo) according to Example 1. Figure 2 shows the results of the stability evaluation of exosomes (Exo) and G-Exo by ratio according to Example 2, including (A) size and (B) variance values of exosomes (Exo) and G-Exo by ratio after storage in DIW for 4 weeks, and (C) size and (D) variance values of exosomes (Exo) and G-Exo by ratio after storage in PBS for 4 weeks. Figure 3 shows the results of the cytotoxicity evaluation of exosomes (Exo) and G-Exo according to the ratio in Example 3. Figure 4 shows the results of evaluating the reactive oxygen species scavenging ability according to the concentration of exosomes (Exo) and G-Exo according to the ratio in Example 4. Figure 5 shows the results of the anti-inflammatory evaluation of exosomes (Exo) and G-Exo5 at different concentrations according to Example 5. Figure 6 shows the results of cell wound healing of the control group and G-Exo5 according to Example 6, (A) a photograph of NIH 3T3 24 hours after G-Exo5 treatment and (B) the distance between cells. Hereinafter, galactose-coated exosomes with enhanced stability, antioxidant and anti-inflammatory effects according to specific embodiments of the invention and their uses will be described in detail. However, this is presented as merely one example of the invention and does not limit the scope of the invention; it is obvious to those skilled in the art that various modifications to the embodiments are possible within the scope of the invention. Throughout this specification, unless otherwise specifically stated, the terms "include" or "contain" refer to the inclusion of any component (or constituent) without any particular limitation and should not be interpreted as excluding the addition of other components (or constituents). As used in this specification, the term "antioxidant" refers to the action of inhibiting oxidation. Although the human body maintains a balance between prooxidants and antioxidants, various factors can cause this balance to become unbalanced and shift toward prooxidation. This leads to oxidative stress, which induces potential cell damage and pathological diseases. Reactive oxygen species (ROS), which are the direct cause of such oxidative stress, are unstable and highly reactive, easily reacting with various biomaterials. They attack macromolecules within the body, causing irreversible damage to cells and tissues, or resulti