CN-122005423-A - Microneedle system for treating hypertrophic scars and preparation method, application and medicament thereof

Abstract

The application discloses a microneedle system for treating hypertrophic scars, a preparation method, application and a medicament thereof, belonging to the technical field of medical treatment, and the technical scheme is that the microneedle system for treating the hypertrophic scars comprises a needle body and a load; the collagen enzyme provided by the application can break scar collagen barriers, increase drug tissue permeability and enzymolysis excessive deposited collagen fibers, and the 5-fluorouracil plays a role in inhibiting abnormal proliferation of fibroblasts, so that a microneedle system can synergistically inhibit and remove scars from a plurality of passages, and the synergy is realized.

Inventors

• LI YIRAN
• MEI LI
• HAN MENGKE
• WANG ANQI

Assignees

• 南方科技大学
• 青岛大学

Dates

Publication Date

20260512

Application Date

20260225

Claims (8)

1. 1. A microneedle system for treating a hypertrophic scar, the microneedle system comprising a needle and a load; The load is a mixture of collagenase and 5-fluorouracil, and the mass ratio of the collagenase to the 5-fluorouracil is 1:4-6.
2. 2. The microneedle system according to claim 1, wherein the needle is prepared by drying a needle solution, and the solute in the needle solution is at least one selected from sodium alginate, PVP, hyaluronic acid, gelatin, and pullulan; The mass ratio of the solute in the needle solution to the load is 9-12:0.1-1.
3. 3. The microneedle system according to claim 1 or 2, wherein the solute in the needle solution is a mixture of sodium alginate and pullulan, and the mass ratio of sodium alginate to pullulan is 0.8-1.2:10.
4. 4. The microneedle system according to claim 1, wherein a backing layer is further provided, said backing layer being bonded to a side of the needle body remote from the tip of the needle body in its length direction.
5. 5. A method of making the microneedle system of any one of claims 1-4, comprising the steps of: step 1, preparing needle body solution and solution containing a load respectively; Step 2, stirring the needle body solution, and then adding the load solution for continuous stirring to obtain a mixed solution; and 3, transferring the mixed solution into a mould, and vacuum drying to obtain the microneedle system.
6. 6. The method for preparing a microneedle system according to claim 5, wherein the step 2 specifically comprises the steps of placing a needle solution in a magnetic stirrer for stirring, then adding the 5-fluorouracil solution while continuously stirring for at least 10min, then placing in an ice-water bath for stirring and cooling to 4 ℃, adding the collagenase solution while continuously stirring, and continuously stirring for 5-10 min to obtain a mixed solution.
7. 7. Use of a microneedle system according to any one of claims 1-4 for the manufacture of a medicament for the treatment of hypertrophic scars.
8. 8. A medicament comprising a microneedle system according to any one of claims 1 to 4.

Description

Microneedle system for treating hypertrophic scars and preparation method, application and medicament thereof Technical Field The application belongs to the technical field of medical treatment, and in particular relates to a microneedle system for treating hypertrophic scars, and a preparation method, application and a medicament thereof. Background Hypertrophic scars (Hypertrophic Scar, HS) are a common pathological scar caused by hyperproliferation of connective tissue and excessive deposition of collagen after deep injury to the dermis of the skin. The pathological characteristics of the collagen are mainly represented by abnormal proliferation of fibroblasts, differentiation of myofibroblasts and imbalance of synthesis and degradation of extracellular matrix (especially type I and type III collagen). Current clinical treatment methods include pressure therapy, silicone formulations, intralesional injection of corticosteroids (e.g., triamcinolone acetonide) or 5-fluorouracil, laser therapy, surgical resection, and the like. However, these methods have significant limitations in that the external preparation is difficult to penetrate dense stratum corneum and scar tissue, the intra-lesion injection is severe in pain, requires professional operations and uneven drug distribution, and laser and surgery have disadvantages of large wounds, high costs, high recurrence risk, and the like. The microneedles (Microneedles, MNs) as a novel transdermal drug delivery technique can penetrate the skin barrier painlessly and minimally invasively, significantly improving the drug delivery efficiency. However, existing drug-loaded microneedles are often used for single drug delivery and single therapy is often limited in effectiveness for complex diseases caused by multiple factors such as hypertrophic scars. The Chinese patent application 202410308868.1 discloses a double-layer soluble microneedle for treating hypertrophic scar and a preparation method thereof, wherein the double-layer soluble microneedle consists of a needle tip and a needle body which are sequentially connected, the needle tip takes hyaluronic acid and polyvinylpyrrolidone as carriers, wherein the asiaticoside is contained in the carrier, and the asiaticoside is distributed in an amorphous state; It can be seen that in the above-described scheme, 5-fluorouracil has been disclosed as an important active substance for scar treatment, and it is considered that a good therapeutic effect of 5-fluorouracil on hypertrophic scars is its inhibitory effect on cells with high proliferation rate. Chinese patent application 202211526779.1 discloses a double-layer microneedle with controllable transdermal property and a preparation method thereof, wherein the main body part of the microneedle except a base is of an upper and lower layered double-layer structure, the upper layer is PcNP@drug compound obtained after PcNP is carried with a drug, the lower layer is HAT@Coll hydrogel obtained by compounding hyaluronic acid-tyrosine hydrogel HAT and collagenase Coll, and meanwhile, the scheme is pointed out in the 9 th section of the specification that the addition of collagenase enhances the transdermal property and cell penetration of the microneedle; It can be seen that in the above-described scheme, it further enhances the transdermal capability of the needle by layering collagenase under the needle to achieve deep delivery of the drug; In summary, the inhibition of cell proliferation by 5-fluorouracil and the enhancement of transdermal capability of microneedles by collagenase have been studied, but the use of both as active substances has not been suggested by the prior art. Thus, there is a great need in the art for a collagenase, 5-fluorouracil based hypertrophic scar multi-target treatment system. Disclosure of Invention The application aims to overcome the defects of the prior art and provide a microneedle system carrying a plurality of loads with scar treatment capability, wherein the loads comprise collagenase and 5-fluorouracil, wherein the 5-fluorouracil can inhibit abnormal proliferation of fibroblasts, and the collagenase can carry out enzymolysis and remove excessive deposited collagen fibers, and the collagenase and the 5-fluorouracil cooperate to further improve the scar improvement capability of the microneedle system. To achieve the above object, the present solution provides a microneedle system for treating a hypertrophic scar, the microneedle system comprising a needle body and a load; The load is a mixture of collagenase and 5-fluorouracil, and the mass ratio of the collagenase to the 5-fluorouracil is 1:4-6. As mentioned in the aforesaid chinese patent application 202410308868.1, chinese patent application 202211526779.1 discloses the application of 5-fluorouracil and collagenase in the treatment of hypertrophic scar, but the main cause of scar hyperplasia is abnormal proliferation of fibroblasts, which causes excessive accumulation of collagen