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Sustained-release soluble microneedle, preparation method and application

A technology of micro-needle and sustained-release drug, applied in the field of micro-needle, can solve the problems of toxic and side effects, decrease of drug bioavailability, etc., and achieve the effect of slowing down the release rate

Active Publication Date: 2021-03-16
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when the drug-loaded dissolvable microneedles are used locally on the skin, the microneedle matrix will dissolve rapidly in the skin, causing the drug to be released quickly and absorbed by some blood vessels, and it is impossible to maintain a stable drug concentration locally on the skin, which will not only cause toxicity side effects, and the bioavailability of the drug is also greatly reduced

Method used

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  • Sustained-release soluble microneedle, preparation method and application
  • Sustained-release soluble microneedle, preparation method and application
  • Sustained-release soluble microneedle, preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0033] This embodiment provides a preparation method of sustained-release soluble microneedles, which specifically includes the following steps:

[0034] (1) Preparation of the carrier coated with methotrexate by spray drying method: dissolving chitosan powder and methotrexate in 0.2% hydrochloric acid aqueous solution, spraying into a desiccator for drying after dissolving completely, collecting and preparing chitosan drug carrier of methotrexate.

[0035] (2) Microneedle mold preparation: Stir polydimethylsiloxane raw material (PDMS, Sylgard 184) and curing agent evenly at a mass ratio of 10:1, vacuumize to remove air bubbles, and mix the liquid polydimethylsiloxane containing curing agent The base siloxane was cast into a plastic Petri dish with a polymethacrylic microneedle positive film (the length of the positive film needle tip is 850 μm), and heated at 80 degrees Celsius for 2 hours. After the PDMS was cured, the microneedle positive film was carefully The membrane is...

Embodiment 2

[0040] This embodiment provides a preparation method of sustained-release soluble microneedles, which specifically includes the following steps:

[0041] (1) Preparation of methotrexate drug carrier by solvent evaporation method: dissolve a certain amount of polylactic acid-glycolic acid copolymer (PLGA) in dichloromethane, add an appropriate amount of methotrexate to disperse evenly, and pour 1% polyvinyl alcohol (PVA) solution, stirred at room temperature at high speed for 3 minutes to form an O / W emulsion, then continued to stir slowly at room temperature for 4 hours to volatilize the organic solvent, and after the organic solvent volatilized, washed and centrifuged to obtain the methotrexate drug carrier.

[0042] (2) Microneedle mold preparation: Stir polydimethylsiloxane raw materials and curing agent evenly at a mass ratio of 10:1, vacuumize to remove air bubbles, and cast liquid polydimethylsiloxane containing curing agent into Put the polymethacrylic acid microneedle po...

Embodiment 3

[0047] This embodiment provides a preparation method of sustained-release soluble microneedles, which specifically includes the following steps:

[0048] (1) Preparation of methotrexate drug carrier by solvent evaporation method: 20 mg of polyε-caprolactone-polyethylene glycol copolymer (PCL-PEG) and 4 mg of methotrexate were dissolved in 10 mL of dimethylformamide, Under the condition of stirring, slowly drop the solution into deionized water, continue to stir for 10 minutes, then carry out dialysis, wash and centrifuge after 24 hours of dialysis to obtain the drug carrier of methotrexate.

[0049] (2) Microneedle mold preparation: Stir polydimethylsiloxane raw materials and curing agent evenly at a mass ratio of 10:1, vacuumize to remove air bubbles, and cast liquid polydimethylsiloxane containing curing agent into Put the polymethacrylic acid microneedle positive film (the positive film needle tip length is 650 microns) in a plastic petri dish, heat at 80 degrees Celsius fo...

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Abstract

The invention discloses a sustained-release soluble microneedle, a preparation method and application. The microneedle comprises a base body, a needle body and a carrier which is distributed in the needle body and coated with a drug to be sustained-released, wherein the carrier comprises a degradable high polymer material or inorganic nanoparticles modified by a polymer. The method comprises the following steps of: preparing the carrier coated with the drug to be sustained-released by adopting one of an emulsion method, a dialysis method, a solvent evaporation method, a spray drying method anda polyelectrolyte protection method, wherein the carrier comprises the degradable high polymer material or the inorganic nanoparticles; and dissolving or dispersing the carrier coated with the drug to be sustained-released into a matrix solution, casting the matrix solution into a mold by utilizing a vacuumizing method, drying and demolding to obtain the sustained-release soluble microneedle. According to the sustained-release soluble microneedle, the degradable high polymer material or the inorganic nanoparticles modified by the polymer are used as the carrier of the drug, so that the release speed of the drug is slowed down.

Description

technical field [0001] The invention belongs to the field of microneedles, and more specifically relates to a sustained-release soluble microneedle, a preparation method and an application. Background technique [0002] When the microneedle is administered locally on the skin, it can effectively penetrate the stratum corneum of the skin without touching the nerves, which not only avoids adverse reactions caused by the drug passing through the gastrointestinal tract, but also does not cause pain, and increases the bioavailability of the drug. In addition, the operation of microneedles is simple and easy, and patients can use them without professional training. There are many types of microneedles, including hollow microneedles and solid microneedles, and solid microneedles are further divided into tissue pretreatment microneedles, soluble drug-loaded microneedles and insoluble drug-coated microneedles. Among them, the soluble microneedles constructed of polymer materials wit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/36A61K31/519A61K47/61A61K47/69A61M37/00A61P17/06A61P19/02A61P29/00
CPCA61K9/0021A61K47/36A61K31/519A61M37/0015A61K47/6923A61K47/61A61P17/06A61P19/02A61P29/00A61M2037/0053
Inventor 朱锦涛李沫杜虹瑶张连斌
Owner HUAZHONG UNIV OF SCI & TECH
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