Microneedle patch

Abstract

A microneedle patch comprises a microneedle layer and an adhesive layer. The microneedle layer includes a plurality of microneedles and is formed of a biocompatible component. The adhesive layer contains functional components, and the microneedle layer is arranged on the adhesive layer. The adhesive layer further comprises a first area and a second area. The second area surrounds the first area, and the microneedle layer is located in the first area.

Description

Technical Field

[0001] The present invention relates to the field of transdermal drug delivery, and more particularly to a microneedle patch and its composition. Background Art

[0002] A microneedle patch (MNP) is a novel transdermal drug delivery system (TDDS). The microneedles on the patch are very short and do not touch the nerves. It not only has no pain of subcutaneous injection, but also can carry bioactive ingredients or drugs through the stratum corneum of the skin into the human body. The MNP technology can be used in various fields such as aesthetic medicine, pharmaceuticals, and preventive medicine. Summary of the Invention

[0003] The present invention provides a microneedle patch that can provide a shorter action time and help accelerate the absorption of bioactive ingredients.

[0004] The present invention also provides a microneedle patch that can promote blood circulation in the skin.

[0005] To achieve one or some or all of the above purposes or other purposes, an embodiment of the present invention provides a microneedle patch, which includes a microneedle layer and an adhesive layer. The microneedle layer includes a plurality of microneedles and is composed of biocompatible components. The adhesive layer contains functional ingredients, and the microneedle layer is disposed on the adhesive layer. The adhesive layer also includes a first region and a second region. The second region surrounds the first region, and the microneedle layer is located in the first region.

[0006] In an embodiment of the present invention, the ratio of the area of the second region to the area of the first region is between 0.05 and 8.

[0007] Since the adhesive layer of the present invention includes a first region and a second region, wherein the second region surrounds the first region and the microneedle layer is located in the first region, on the one hand, the microneedle patch can subcutaneously release bioactive ingredients through the microneedle layer in the first region, and on the other hand, the functional ingredients can act on the skin through the adhesive layer, achieving effects such as increasing subcutaneous vasodilation, promoting skin blood circulation, and causing a heat sensation. The increased blood flow and the rising temperature also help accelerate the release of bioactive ingredients.

[0008] The present invention will be described in detail below with reference to the accompanying drawings and specific embodiments, but it is not limited to the present invention. Brief Description of the Drawings

[0009] Figure 1 It is a cross-sectional schematic view of the microneedle patch according to the first embodiment of the present invention.

[0010] Figure 2 It is a top view schematic view of the microneedle patch according to the first embodiment of the present invention.

[0011] Figures 3A to 3D Top view schematic diagram of the microneedle patch according to the second embodiment of the present invention.

[0012] Figure 4 Schematic diagram of the hourly degradation rate of the microneedle layer according to the embodiments and comparative examples of the present invention.

[0013] Among them, reference numerals:

[0014] 1, 1a, 1b, 1c, 1d: microneedle patch

[0015] 10: microneedle layer

[0016] 100: microneedle

[0017] 150: base layer

[0018] 151: first side

[0019] 152: second side

[0020] 20: adhesive layer

[0021] 201: adhesive layer part

[0022] 30: carrier layer

[0023] A1: first region

[0024] A2: second region

[0025] P1: outer contour

[0026] P2: inner contour

[0027] C: bioactive ingredient

[0028] F: functional ingredient Detailed implementation manners

[0029] The structural principle and working principle of the present invention will be specifically described below with reference to the drawings:

[0030] The foregoing and other technical contents, features and effects of the present invention will be clearly presented in the following detailed description of a preferred embodiment with reference to the drawings. The directional terms mentioned in the following embodiments are only with reference to the directions of the attached drawings. Therefore, the directional terms used are for illustration and not for limiting the present invention. In addition, the terms "first", "second", etc. mentioned in this specification or the scope of the patent application are only used to name the elements or to distinguish different embodiments or scopes, rather than to limit the upper or lower limits of the number of elements.

[0031] The present invention provides a microneedle patch, which can be used as a carrier for bioactive ingredients for transdermal absorption and transdermal drug delivery. The microneedle patch of the present invention can also have the effect of promoting the subcutaneous release of bioactive ingredients, achieving the effects of shortening the action time and accelerating absorption.

[0032] Figure 1 It is a schematic cross-sectional view of a microneedle patch according to an embodiment of the present invention. As Figure 1 shown, the microneedle patch 1 includes a microneedle layer 10 and an adhesive layer 20. The microneedle layer 10 is disposed on the adhesive layer 20 and is composed of biocompatible components. The "biocompatibility" of the components means that the material, compound or composition does not release toxic or harmful substances, causing local or systemic adverse reactions in the human body or other organisms, such as inflammatory reactions, immune reactions, and toxic reactions. In addition, in the embodiments of the present invention, the biocompatible component is a material, compound or composition that can be degraded / dissolved in the living body. In a preferred embodiment of the present invention, the biocompatible component includes one or more soluble polymer compounds, and the soluble polymer compounds impart solubility (or degradability) to the biocompatible component. The soluble polymer compound can be a natural or synthetic compound. For example, it can be, for example, maltodextrin, cyclodextrin, pullulan, carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, polylactic acid, sodium alginate, hyaluronic acid, chitosan, polyvinylpyrrolidone or a combination thereof, or a polymer whose monomers are, for example, maltose, sucrose, lactose, trehalose or a combination thereof.

[0033] As Figure 1 shown, in addition to being composed of biocompatible components, the microneedle layer 10 also contains a bioactive ingredient C. In the present invention, the bioactive ingredient means a component that can produce a biological effect on humans or other organisms, such as changing the physiological functions and biochemical metabolism of humans. In the embodiments of the present invention, due to the solubility of the biocompatible component, the microneedle layer 10 can achieve the effect of releasing the bioactive ingredient C therein. The bioactive ingredient C can be, for example, hyaluronic acid, niacinamide, vitamin C, peptide, centella asiatica, allantoin, dipotassium glycyrrhizinate, probiotic, yeast extract or a combination thereof, but is not limited thereto. For example, the bioactive ingredient C can also be a medicinally active ingredient. In addition, the bioactive ingredient C in the embodiments of the present invention can be more suitable for acting in a short time and / or for being rapidly absorbed by the organism. It should be noted that although the bioactive ingredient C is marked in the figure, it is only used to indicate that the microneedle layer 10 contains the bioactive ingredient C; the bioactive ingredient C in the microneedle layer 10 does not necessarily appear and can be seen.

[0034] As Figure 1As shown, the microneedle layer 10 includes a plurality of microneedles 100, whereby the microneedles can penetrate into the epidermis to release bioactive ingredient C subcutaneously. The microneedle layer 10 further includes a base layer 150, wherein the plurality of microneedles 100 are spaced apart from each other and are disposed on the same side of the base layer 150. The diameter length of the microneedles 100 is thicker closer to the base layer 150. Specifically, the shape can be, for example, a pyramid or a cone. The length of the microneedles 100 can be 100 to 1500 μm, such as 100 μm, 500 μm, 800 μm, 1000 μm, 1500 μm. The base layer 150 has opposite first and second surfaces 151 and 152. All the microneedles 100 are disposed on the same surface, such as the first surface 151, and the other surface, such as the second surface 152, can be used to connect the microneedle layer 10 to the adhesive layer 20.

[0035] The adhesive layer 20 may include a layer made of an adhesive. The adhesive can be a natural or synthetic polymer compound, such as a rubber-based polymer, an acrylic-based polymer, a silicone-based polymer, or a combination thereof, but is not limited thereto. The adhesive layer 20 preferably has an affinity for the skin and may have adhesiveness, but is not limited thereto. In addition, the adhesive layer 20 can also be a patch or a patch in a broad sense. When the adhesive layer 20 is in the form of a patch or a patch, the patch or the patch includes the aforementioned layer made of an adhesive. The adhesive layer 20 can further have forms such as a gel or an adhesive. In a preferred embodiment of the present invention, the adhesive layer 20 is a gel mainly composed of silica gel. As Figure 1 As shown, the microneedle patch 1 may further include a carrier layer 30. The carrier layer 30 is disposed on the side opposite to the side where the microneedle layer 10 is connected on the adhesive layer 20, and its material can be, for example, a natural or synthetic fabric such as cloth, or a natural or synthetic polymer such as a film. The material of the carrier layer 30 can also be selected based on several functional requirements such as waterproofness, breathability, antibacterial property, odor, aesthetics, and hand feel.

[0036] In an embodiment of the present invention, the adhesive layer 20 contains a functional ingredient F. The functional ingredient F can be added to the aforementioned adhesive during the preparation of the adhesive layer 20. In a preferred embodiment of the present invention, the main functions of the functional ingredient F are to promote blood circulation, increase vasodilation, induce a sense of heat, or a combination thereof. Based on these functions, the microneedle patch 10 helps to increase subcutaneous vasodilation and promote blood circulation in the skin. Due to the increased blood flow, the local temperature of the skin can rise, inducing a sense of heat. The increased blood flow and the rise in temperature also help to accelerate the degradation of the microneedles 100, thereby accelerating the release of the bioactive ingredient C. Any ingredient that can promote blood circulation, increase vasodilation, cause a rise in skin temperature, or induce a sense of heat can be used as the functional ingredient F in the embodiments of the present invention. Preferably, the functional ingredient F can be, for example, methyl salicylic acid, mint or its extract, capsaicin, vanillyl butyl ether, ginger or its extract, or a combination thereof. The present invention can also select or use a combination of various functional ingredients F based on other functions of the functional ingredient F, such as, but not limited to, reducing swelling and relieving pain. It should be noted that although the functional ingredient F is marked in the drawings, it is only used to indicate that the adhesive layer 20 contains the functional ingredient F; the functional ingredient F in the adhesive layer 20 may not necessarily be visible.

[0037] Figure 2 is Figure 1 a top view schematic diagram of the illustrated embodiment. As Figures 1 to 2 shown, the adhesive layer 20 can have a specific shape and can be divided into different regions, such as a first region A1 and a second region A2. The adhesive layer 20 further has a first region A1 and a second region A2 on the side connected to the microneedle layer 10. In an embodiment of the present invention, the second region A2 surrounds the first region A1. For example, when the first region A1 is a circular region, the surrounding second region A2 is an annular region. The microneedle layer 10 can be further located in the first region A1 of the adhesive layer 20. The shapes of the first region A1 and the second region A2 are not limited to standard geometric shapes and can also be irregular shapes, such as Figure 2 the micro-bent oblong shape shown. On the other hand, the outer contour of the second region A2 can correspond to the shape of the adhesive layer 20 in the top view direction. For example, in Figure 2 the illustrated embodiment, the adhesive layer 20 is in the shape of a micro-bent oblong and is equivalent to the shape of the outer contour P1 of the second region A2. When the first region A1 and the second region A2 are adjacent, the inner contour P2 of the second region A2 can correspond to the contour of the first region A1, and the contour of the first region A1, for example, corresponds to the contour of the base layer 150 of the microneedle layer 10.

[0038] Figures 3A to 3D Shown is a schematic diagram of other microneedle patch embodiments of the present invention, in which Figure 3A the first region A1 of the microneedle patch 1a is ear-shaped, Figure 3B the microneedle patch 1b and Figure 3CThe first region A1 of the microneedle patch 1c is circular. Figure 3D The first region A1 of the microneedle patch 1d is a rectangle with rounded corners. In Figure 3A , 3B and the embodiments shown in FIGS. 3A - 3D, the shape of the first region A1 generally corresponds to the shape of the adhesive layer 20, that is Figure 3A the adhesive layer 20 in Figure 3B is also ear-shaped, Figure 3D the adhesive layer 20 in Figure 3D is also circular, and Figure 3D the adhesive layer 20 in Figure 3D Figure 3C is also rectangular. However, the present invention is not limited thereto. In an embodiment of the present invention, the shape of the first region A1 may be different from the shape of the adhesive layer 20. For example, as shown in Figure 3C , the first region A1 is circular while the adhesive layer 20 is of other shapes such as a teardrop shape. The design where the shapes of the adhesive layer 20 and the first region A1 correspond or are different has the effect that, for example, when they correspond, the adhesive layer 20 can more completely cover the periphery of the microneedle layer 10, ensuring that it can affect the skin around the microneedles 100 as much as possible, promoting blood circulation, increasing vasodilation, causing a rise in skin temperature, and effectively accelerating the degradation of the microneedles 100. In other words, it avoids limiting the effect of the microneedles 100 due to the lack of the adhesive layer 20 around the microneedle layer 10. In addition, in response to usage requirements such as convenient tearing and different shapes of various body parts, the adhesive layer 20 can also be designed to have a shape different from that of the first region A1. In a preferred embodiment of the present invention, the adhesive layer 20 may only include the first region A1 and the second region A2, and the sum of the area of the first region A1 and the area of the second region A2 is equal to the area of the adhesive layer 20.

[0039] As shown in Figure 1 , 2 and FIGS. 3A - 3D, the second region A2 is equivalent to the part where the adhesive layer 20 protrudes outside the microneedle layer 10. Based on this design, on the one hand, the microneedle patch 1 can subcutaneously release the bioactive ingredient C through the microneedle layer 10 of the first region A1, and on the other hand, since the second region A2 protrudes outside the microneedle layer 10, the adhesive layer 20 can directly contact the skin. Thus, the microneedle patch 1 can cause the functional ingredient F to act on the skin through the adhesive layer 20, achieving effects such as increasing subcutaneous vasodilation, promoting skin blood circulation, warming the skin, and inducing a heat sensation. The increase in blood flow and the rise in temperature also help to accelerate the degradation of the microneedles 100, and thus accelerate the release of the bioactive ingredient C.

[0040] As shown in Figure 2 and 3A -3D, the degree to which the adhesive layer 20 protrudes is not limited to being consistent. For example, as shown in Figure 3CAs shown, the portion 201 of the water droplet-shaped tip of the adhesive layer 20 protrudes more. The greater the degree of protrusion of the adhesive layer 20, the more significantly the degree of vasodilation, blood circulation, and temperature rise can be expected to increase. In the embodiment of the present invention, the ratio of the area between the second region A2 and the first region A1 can roughly reflect the degree of protrusion of the adhesive layer 20 and the ratio of the adhesive layer 20 in contact with the skin of the microneedle layer 10. When the ratio of the area of the second region A2 to the area of the first region A1 is larger, it is preferably possible to cause a more significant increase in blood flow and temperature rise, and to more rapidly degrade the microneedles 100 and release the bioactive ingredient C.

[0041] The ratio of the area of the second region A2 to the area of the first region A1 can also be coordinated with the type and content of the functional ingredient F to obtain the desired degradation rate of the microneedles 100. Furthermore, the degradation rate of the microneedles 100 can be determined according to the type and content of the bioactive ingredient C. For example, the functional ingredient F can be formulated according to the desired action time of the bioactive ingredient C in the organism, so as to make the microneedles 100 have an appropriate degradation rate. In a preferred embodiment of the present invention, the ratio of the area of the second region A2 to the area of the first region A1 is between 0.05 and 8, such as 0.05, 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 5.5, 6.0, 7.0, 7.5, 8. The functional ingredient F can be one or more. Under the principle of safe dosage, the total amount of one or more functional ingredients F can account for 0.5 to 20 wt% of the weight of the adhesive layer 20, such as 0.5 wt%, 1 wt%, 2 wt%, 3 wt%, 4 wt%, 5 wt%, 6 wt%, 7 wt%, 8 wt%, 9 wt%, 10 wt%, 11 wt%, 12 wt%, 13 wt%, 14 wt%, 15 wt%, 16 wt%, 17 wt%, 18 wt%, 19 wt%, 20 wt%.

[0042] In a preferred embodiment of the present invention, the degradation rate of the microneedles 100 is further such that they can be completely (100%) degraded in less than four hours. Under the condition that the ratio of the area of the second region A2 to the area of the first region A1 is the same in the present invention, the microneedle degradation rates of the microneedle patch 1 containing the functional ingredient F and the microneedle patch without the functional ingredient F are tested. The test method can be, for example, at room temperature, such as 25 °C, attaching the microneedle patch 1 to the skin, and removing the microneedle patch 1 after, for example, 0.5, 1, 2, 4 hours, and measuring the length of the microneedles 100 therein. In a preferred embodiment of the present invention, repeated tests are carried out for different time groups, and the average value is calculated after measuring the length of the microneedles 100. The results are shown in Table 1 below and Figure 4 .

[0043] Table 1:

[0044]

[0045] The calculation formula for the degradation rate is: [(original length of the microneedle - length of the microneedle after n hours) / original length of the microneedle]*100%. Figure 4 The dots in it represent the average degradation rates at each time of Examples 1, 2, 3, 4 and the Comparative Example. Then, a linear regression analysis is performed to obtain the degradation rate trend curves of Examples 1, 2, 3, 4 and the Comparative Example.

[0046] Dividing the degradation rate by the number of hours can obtain the approximate degradation rate. For example, the degradation rate of the Comparative Example is approximately 33% per hour (66% / 2 = 33%), and that of Example 4 (the functional ingredient F is 5 wt% ginger extract) is approximately 45% per hour (90% / 2 = 45%). Therefore, the degradation rate of Example 4 is greater than that of the Comparative Example. Thus, it can be seen that the microneedle patch of the embodiment of the present invention can release the bioactive ingredient C subcutaneously due to the increased degradation rate, which helps to shorten the action time and accelerate the absorption of the bioactive ingredient.

[0047] In summary, the microneedle patch 1 of the embodiment of the present invention can subcutaneously release the bioactive ingredient C through the microneedle layer 10, and can make the functional ingredient F act on the skin through the adhesive layer 20, achieving effects such as increasing subcutaneous vasodilation, promoting skin blood circulation, raising skin temperature, and inducing a heat sensation. The increased blood flow and the rising temperature also help to accelerate the degradation of the microneedles 100, and thus accelerate the release of the bioactive ingredient. The microneedle patch 1 of the embodiment of the present invention further has the effects of shortening the action time and accelerating absorption.

[0048] Certainly, the present invention can also have many other embodiments. Without departing from the spirit and essence of the present invention, those skilled in the art can make various corresponding changes and deformations according to the present invention, but these corresponding changes and deformations should all fall within the protection scope of the appended claims of the present invention.

Claims

1. A microneedle patch, characterized in that: Include: a microneedle layer; the microneedle layer comprises a plurality of microneedles and is composed of a biocompatible component; and an adhesive layer containing an effective ingredient, and the microneedle layer is disposed on the adhesive layer; The adhesive layer includes a first area and a second area; the second area surrounds the first area, and the microneedle layer is located in the first area.

2. The microneedle patch according to claim 1, characterized in that The ratio of the area of ​​the second region to the area of ​​the first region is between 0.05 and 8.

3. The microneedle patch according to claim 1, characterized in that The microneedle layer further comprises at least one bioactive component and includes a base layer; the base layer has a first surface and a second surface opposite to the first surface; the plurality of microneedles are arranged on the first surface, and the microneedle layer is arranged in the first area with the second surface of the base layer.

4. The microneedle patch according to claim 1, characterized in that The effective ingredient is methyl salicylic acid, mint or its extract, capsaicin, vanillyl butyl ether, ginger or its extract or a combination thereof.

5. The microneedle patch according to claim 4, characterized in that The adhesive layer is further composed of at least one polymer compound, and the functional component accounts for 0.5-20wt% of the weight of the adhesive layer.

6. The microneedle patch according to claim 1, characterized in that The sum of the area of ​​the first region and the area of ​​the second region is equal to the area of ​​the adhesive layer.

7. The microneedle patch according to claim 1, characterized in that The shape of the adhesive layer corresponds to or is different from the shape of the first area.

8. The microneedle patch according to claim 7, characterized in that When the shape of the adhesive layer corresponds to the shape of the first region, the shape of the adhesive layer is the same as the shape of the first region.

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