KR-20260064617-A - Microneedle patch composition, Microneedle patch manufacturing method and Microneedle patch

Abstract

The present invention relates to a microneedle patch composition, a method for manufacturing a microneedle patch, and a microneedle patch; more specifically, it relates to a microneedle patch composition capable of stabilizing and maintaining the content of pure vitamin C (ascorbic acid), a method for manufacturing a microneedle patch, and a microneedle patch.

Inventors

• 정도현
• 나숙희
• 성창엽
• 최은실
• 이문수
• 김권우
• 최예람
• 박소빈

Assignees

• 주식회사 라파스

Dates

Publication Date

20260507

Application Date

20251030

Priority Date

20241030

Claims (9)

1. A microneedle patch composition characterized by comprising ascorbic acid, citric acid, sucrose, a biodegradable polymer compound, and purified water.
2. In paragraph 1, A microneedle patch composition characterized by containing 1 to 6 weight% of the citric acid and 2 to 8 weight% of the sucrose.
3. In paragraph 1, A microneedle patch composition characterized by containing 1 to 8 weight percent of the ascorbic acid.
4. In paragraph 1, A microneedle patch composition characterized by containing 2% by weight of the ascorbic acid, 8% by weight of the sucrose, and 1 to 6% by weight of the citric acid.
5. In paragraph 1, A microneedle patch composition characterized by containing 2% by weight of the ascorbic acid, 6% by weight of the citric acid, and 2 to 8% by weight of the sucrose.
6. In paragraph 1, A microneedle patch composition characterized by containing 1 to 8 weight% of the ascorbic acid, 6 weight% of the citric acid, and 4 weight% of the sucrose.
7. In paragraph 1, The above-mentioned biodegradable polymer compound is hyaluronic acid and its salt, polyvinylpyrrolidone, polyvinyl alcohol, cellulose polymer, dextran, gelatin, glycerin, polyethylene glycol, polysorbate, propylene glycol, povidone, carbomer, gum ghatti, guar gum, glucomannan, glucosamine, dammer resin, rennet casein, locust bean gum, microfibrillated cellulose, psyllium seed gum, xanthan gum, arabino galactan, gum arabic, alginic acid, gelatin, gellan gum, carrageenan, karaya gum, curdlan, chitosan, chitin, and tara gum. A microneedle patch composition characterized by being composed of one or more selected from the group consisting of tamarind gum, tragacanth gum, furcelleran, pectin or pullulan, hydroxypropyl methylcellulose, hydroxyalkyl cellulose, ethyl hydroxyethyl cellulose, alkylcellulose, and carboxymethylcellulose.
8. The step of producing a microneedle patch using a microneedle patch composition according to either claim 1 or claim 7 selected Step of providing a pair of sheets; A step of spotting the microneedle patch composition on at least one of the pair of sheets; A step of moving the pair of sheets relative to each other so that they come closer to one another, thereby bringing the composition into contact with each other between the pair of sheets; and A method for producing a microneedle patch characterized by comprising the step of solidifying the above composition and separating the pair of sheets to form microneedles on the pair of sheets.
9. A microneedle patch comprising ascorbic acid, citric acid, sucrose, and a biodegradable polymer compound, manufactured by the manufacturing method according to paragraph 8.

Description

Microneedle patch composition, microneedle patch manufacturing method and microneedle patch The present invention relates to a microneedle patch composition, a method for manufacturing a microneedle patch, and a microneedle patch; more specifically, it relates to a microneedle patch composition capable of stabilizing and maintaining the content of pure vitamin C (ascorbic acid), a method for manufacturing a microneedle patch, and a microneedle patch. In general, vitamin C (ascorbic acid) (hereinafter referred to as 'ascorbic acid') can exert various effects on the human body. First, ascorbic acid acts as a major water-soluble antioxidant in human skin and protects skin cells from reactive oxygen species (ROS) generated by ultraviolet (UV) rays and environmental stress. In particular, ascorbic acid can alleviate oxidative stress caused by UV exposure and inhibit photoaging and photocarcinogenesis. In addition, ascorbic acid acts as a cofactor for the enzyme (prolyl-lysyl hydroxylase) required for the hydroxylation reaction of proline and lysine during the collagen synthesis process, thereby helping to stabilize the collagen triple helix structure. Furthermore, ascorbic acid increases the activity of fibroblasts in the dermis and has the effect of reducing collagen degradation by inhibiting the expression of matrix metalloproteinases (MMPs). Meanwhile, ascorbic acid can inhibit the step in the melanin biosynthesis pathway where tyrosine is oxidized to dopaquinone by tyrosinase. This is because ascorbic acid acts as a reducing agent that prevents the oxidation of melanin precursors by being oxidized in place of tyrosine and providing electrons. Accordingly, Vitamin C has the effect of reducing melanin deposition and improving pigmentation (whitening), and its efficacy has been clinically proven. However, ascorbic acid is easily oxidized and decomposed by environmental factors such as oxygen in the air, high temperature, metal ions, and light, and dehydration and browning occur. In particular, in water-soluble formulations, the decomposition rate increases rapidly at pH 5 or higher, and auto-oxidation is promoted in the presence of metal ions (Cu², Fe²). As a result, problems such as reduced concentration of active ingredients in the formulation, discoloration, and decreased efficacy frequently occur. In addition, ascorbic acid is water-soluble and exists in an ionized state, making it difficult to penetrate the stratum corneum. Accordingly, it is difficult to secure an effective concentration within the skin in general cream or serum formulations, so high-concentration, low-pH formulations or penetration-promoting technologies are required to achieve effective whitening and antioxidant effects. Furthermore, due to the oxidative properties of ascorbic acid, its content decreases during long-term storage, and its stability is further reduced due to cross-oxidation reactions when combined with other active ingredients. For this reason, the cosmetics industry frequently uses it in the form of stabilization derivatives (e.g., AA2G, MAP, SAP, etc.) or applies liposome/emulsion encapsulation technology. Meanwhile, microneedles are gaining attention as an active ingredient delivery system that combines the efficacy of conventional syringes with the convenience of patches, as they enable the direct delivery of active ingredients into the skin by penetrating the stratum corneum, which acts as the skin barrier. Since the delivery efficiency can be significantly improved when ascorbic acid is loaded into microneedles, if the stability of the loaded ascorbic acid is guaranteed, it is expected to exhibit much superior efficacy compared to currently commercially available ascorbic acid products in emulsion forms such as oil in water or water in oil. In the prior art, a technology for stabilizing retinol microneedles containing cyclodextrin (hereinafter β-Cyclodextrin) has been disclosed. This prior art is a technology for a microneedle composition that stabilizes retinol based on inclusion technology, and the stabilizer (β-Cyclodextrin) is a substance with a relatively high pKa. In this case, there is a limitation in that the retinol microneedle stabilization technology described above cannot be applied because ascorbic acid, which corresponds to pure vitamin C, is a substance that is stable in a low pH environment. FIG. 1 is a photograph showing a microneedle patch fabricated using the microneedle patch compositions according to the Comparative Example, Example 1 and Example 2. FIG. 2 is a graph evaluating the stability of ascorbic acid after 4 weeks under accelerated stability evaluation conditions in microneedle patches according to Comparative Example, Example 1, and Example 2. FIG. 3 is a photograph showing a microneedle patch fabricated using the microneedle patch composition according to the Comparative Example and Examples 3 to 7. FIG. 4 is a graph evaluating the stability of ascorbic acid after 4 weeks under acceler