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KR-20260062534-A - Microneedle containing poorly soluble minoxidil and manufacturing method thereof

KR20260062534AKR 20260062534 AKR20260062534 AKR 20260062534AKR-20260062534-A

Abstract

The present invention relates to a microneedle composition comprising a poorly soluble drug, a permeability enhancer, and a biocompatible polymer, wherein the poorly soluble drug is minoxidil or an acceptable salt thereof. According to the present invention, excellent drug delivery and absorption effects can be achieved by using a microneedle patch comprising a microneedle composition containing a penetration enhancer and a biocompatible polymer in the poorly soluble drug minoxidil.

Inventors

  • 진성규
  • 김희서

Assignees

  • 주식회사 마이크로엔팜

Dates

Publication Date
20260507
Application Date
20241029

Claims (12)

  1. A microneedle composition comprising a poorly soluble drug, a penetration enhancer, and a biocompatible polymer, The above-mentioned poorly soluble drug is a microneedle composition, which is minoxidil or an acceptable salt thereof.
  2. In paragraph 1, The above-mentioned permeability promoter is one or more selected from polysorbate 80, sodium lauryl sulfate (SLS), transcutol, labrasol, propylene carbonate, myristyl lactate, and D-α-tocopheryl polyethylene glycol succinate (TPGS), in a microneedle composition.
  3. In paragraph 1, The above-mentioned biocompatible polymer is one or more selected from polyvinylpyrrolidone, polyvinyl alcohol, sodium carboxymethyl cellulose, vinylpyrrolidone-vinyl acetate copolymer (copovidone), sodium alginate, gelatin, cyclodextrin, chitosan, hydroxypropylcellulose, and hydroxypropyl methylcellulose, forming a microneedle composition.
  4. In paragraph 1, The microneedle composition further comprises one or more solubilizing agents selected from water, acetonitrile, ethanol, isopropyl alcohol, benzyl alcohol, dimethyl sulfoxide, polyethylene glycol 400, and polyethylene glycol 600.
  5. In paragraph 1, The microneedle composition further comprises one or more sugars selected from sucrose, lactulose, lactose, maltose, trehalose, cellobiose, chitobiose, callose, laminarin, chrysolaminarin, xylan, arabinoxylan, mannan, fucoidan, and galactomannan.
  6. In paragraph 1, A microneedle composition containing the above minoxidil and permeability enhancer in a weight ratio of 2:1 to 3:1.
  7. A microneedle comprising any one of the microneedle compositions of paragraphs 1 through 6.
  8. The microneedles of paragraph 7, and Microneedle array including a support.
  9. The microneedle array of claim 8; and A microneedle patch comprising an adhesive patch.
  10. In Paragraph 9, The above microneedle patch contains minoxidil in an amount greater than 1.5 mg and less than 1.9 mg.
  11. In Paragraph 9, The above microneedle patch is characterized by being used by adhering it to the skin of a subject.
  12. A step of forming microneedles by injecting a microneedle composition comprising minoxidil or an acceptable salt thereof, a permeability enhancer, and a biocompatible polymer into a mold for manufacturing microneedles, A step of forming a support for the microneedles by injecting a water-soluble polymer onto the microneedles, and A method for manufacturing a microneedle array comprising the step of drying a microneedle array including the microneedle and support, and then separating the microneedle array from a mold.

Description

Microneedle containing poorly soluble minoxidil and manufacturing method thereof The present invention relates to microneedles loaded with poorly soluble minoxidil and a method for manufacturing the same. In general, microneedles are a drug delivery system for transdermal drug delivery, which enables drug delivery by administering the drug into the body through the stratum corneum of the skin using microneedles. In the case of drugs with low skin affinity or large molecular weight, it is difficult for the drug to penetrate the stratum corneum and reach the dermis; therefore, microneedles can be used to improve drug delivery to the stratum corneum and the dermis. In particular, soluble microneedles are a type of transdermal drug delivery system that increases drug delivery efficiency by loading drugs onto the microneedles themselves; because they are manufactured from water-soluble polymers with excellent biocompatibility, they dissolve and are absorbed within the body after penetrating the skin. Drugs loaded into conventional microneedle drug delivery systems have been largely limited to hydrophilic drugs, posing a limitation to the use of microneedles for poorly soluble drugs. Furthermore, drug release patterns have been primarily restricted to immediate-release microneedles, which has limited the types of drugs that can be applied and posed difficulties in replacing injectable drugs or existing transdermal drug delivery systems. Therefore, there is a need to develop microneedles that contain not only hydrophilic drugs but also poorly soluble drugs. The present invention can improve the limitations of the microneedles mentioned above, enables transdermal delivery of poorly soluble drugs, and provides the effect of improving hair growth by enhancing skin permeability through the provision of microneedles containing the poorly soluble drug minoxidil to a subject. FIG. 1 shows a method for fabricating a microneedle array according to an embodiment of the present invention. FIG. 2 is a microscopic photograph of a microneedle array according to an embodiment of the present invention, where (a) to (d) correspond to Examples 1 to 4, respectively. FIG. 3 shows the results of an evaluation of the insertion force of a microneedle patch according to Examples 1 to 5 and Comparative Example 3 of the present invention, where (a) to (e) correspond to Examples 1 to 5, respectively, and (f) corresponds to Comparative Example 3. Figure 4 is a graph showing the results of the skin permeability evaluation of minoxidil according to Examples 1 to 4 and Comparative Examples 1 to 3 of the present invention. The embodiments are described in detail below. However, various modifications may be made to the embodiments, so the scope of the patent application is not limited or restricted by these embodiments. It should be understood that all modifications, equivalents, and substitutions to the embodiments are included within the scope of the rights. The terms used in the embodiments are for illustrative purposes only and should not be interpreted as intended to be limiting. Singular expressions include plural expressions unless the context clearly indicates otherwise. In this specification, terms such as "comprising" or "having" are intended to indicate the existence of the features, numbers, steps, actions, components, parts, or combinations thereof described in the specification, and should be understood as not precluding the existence or addition of one or more other features, numbers, steps, actions, components, parts, or combinations thereof. Unless otherwise defined, all terms used herein, including technical or scientific terms, have the same meaning as generally understood by those skilled in the art to which the embodiments pertain. Terms such as those defined in commonly used dictionaries should be interpreted as having a meaning consistent with their meaning in the context of the relevant technology, and should not be interpreted in an ideal or overly formal sense unless explicitly defined in this application. In addition, when describing the embodiments, if it is determined that a detailed description of related prior art could unnecessarily obscure the essence of the embodiments, such detailed description is omitted. Components included in any one embodiment and components having common functions shall be described using the same names in other embodiments. Unless otherwise stated, the descriptions given in any one embodiment may also apply to other embodiments, and specific descriptions shall be omitted to the extent of overlap. Throughout the specification, "drug" refers to a substance used for the purpose of preventing, diagnosing, or treating a disease of the subject, and "poorly soluble drug" refers to a drug having low solubility in an aqueous solution and low biomembrane permeability. "Microneedle composition" refers to a compositional material of the components that make up the microneedle, and "microneedle" refers