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Soluble microneedle supported with hydrophobic drug and preparation method thereof

A hydrophobic drug, soluble technology, applied in the direction of drug devices, microneedles, drug delivery, etc., can solve the problem of not guaranteeing complete removal of organic solvents, easy residual organic solvents in microneedles, etc., to achieve good biocompatibility and improve water solubility. The effect of improving the solubility and improving the solubility

Active Publication Date: 2018-11-13
HUAZHONG UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the essence of this method is to use the solubility of organic solvents to drugs, and it cannot guarantee that the organic solvents can be completely removed. Organic solvents are easy to remain in the microneedles, and there is a great safety risk.

Method used

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  • Soluble microneedle supported with hydrophobic drug and preparation method thereof
  • Soluble microneedle supported with hydrophobic drug and preparation method thereof
  • Soluble microneedle supported with hydrophobic drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] This embodiment comprises the following steps:

[0030] 1. Stir and mix the PDMS precursor (Sylgard 184) and curing agent (mass ratio: 10:1), and inject it into a container with a microneedle male mold (the length of the microneedle is 50 μm) after the air bubbles are eliminated, and heat it to make it Completely cured, after curing, the microneedle positive mold and PDMS were separated to obtain the PDMS microneedle negative template.

[0031]2. Prepare an aqueous solution of triamcinolone acetonide (a hydrophobic hormone drug), wherein the content of triamcinolone acetonide in the drug solution is 0.1 wt%, and the content of dioleoyl lecithin is 0.01 wt%. Take hyaluronic acid powder, dissolve it in water, and magnetically stir for several hours to obtain a hyaluronic acid aqueous solution with a mass fraction of 60%.

[0032] 3. Add the triamcinolone acetonide aqueous solution into the PDMS mold, make the drug solution enter the tip of the mold under vacuum negative ...

Embodiment 2

[0035] This embodiment comprises the following steps:

[0036] 1. Stir and mix the PDMS precursor (Sylgard 184) and curing agent (mass ratio: 10:1). After the air bubbles are eliminated, inject it into a container with a microneedle male mold (the length of the microneedle is 900 μm), and heat it to make it Completely cured, after curing, the microneedle positive mold and PDMS were separated to obtain the PDMS microneedle negative template.

[0037] 2. Prepare an aqueous solution of methotrexate, wherein the content of methotrexate in the drug solution is 15 wt%, and the content of β-cyclodextrin is 20 wt%. Take chondroflavin powder, dissolve it in water, and magnetically stir for several hours to obtain a chondroflavin aqueous solution with a mass fraction of 30%.

[0038] 3. Add the methotrexate aqueous solution into the PDMS mold, make the drug solution enter the tip of the mold under vacuum negative pressure, and recover the excess drug solution on the surface of the temp...

Embodiment 3

[0041] This embodiment comprises the following steps:

[0042] 1. Stir and mix the PDMS precursor (Sylgard 184) and curing agent (mass ratio: 10:1). After the air bubbles are eliminated, pour it into a container with a microneedle male mold (the length of the microneedle is 2500 μm), and heat it to make it Completely cured, after curing, the microneedle positive mold and PDMS were separated to obtain the PDMS microneedle negative template.

[0043] 2. Prepare an aqueous solution of levofloxacin, wherein the content of levofloxacin in the drug solution is 30 wt%, and the content of polysorbate is 40 wt%. Take polyvinylpyrrolidone powder, dissolve it in water, and stir it magnetically for several hours to obtain an aqueous solution of polyvinylpyrrolidone with a mass fraction of 5%.

[0044] 3. Add the levofloxacin aqueous solution into the PDMS mold, make the drug solution enter the tip of the mold under centrifugal action, and recover the excess drug solution on the surface o...

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Abstract

The invention discloses a soluble microneedle supported with a hydrophobic drug and a preparation method thereof. The preparation method comprises the following steps: (1) taking a hydrophobic drug and a solubilizing substance with biocompatibility, and dissolving in water together to obtain a hydrophobic drug aqueous solution; (2) preparing a polymer aqueous solution; (3) adding the hydrophobic drug aqueous solution into a microneedle die, and filling a tip part of the microneedle die with the hydrophobic drug aqueous solution; and (4) adding the polymer aqueous solution to the microneedle die having the tip part supported with the hydrophobic drug, making the microneedle die filled with the polymer aqueous solution, drying, and demolding to obtain the soluble microneedle having the tip part supported with the hydrophobic drug. The solubility of the hydrophobic drug in water is increased by using the solubilizing substance with good biocompatibility, so that the content of the hydrophobic drug in the water can meet drug administration demand; the preparation process does not use any organic solvents at all, so environmental pollution is reduced, and the obtained soluble microneedle supported with the hydrophobic drug can improve the safety of drug administration.

Description

technical field [0001] The invention belongs to the field of drug delivery, and more specifically relates to a soluble microneedle loaded with hydrophobic drugs and a preparation method thereof. Background technique [0002] Human skin is divided into two layers, the dermis and the epidermis from the inside to the outside. The stratum corneum, which controls the transdermal absorption of drugs, is located in the epidermis without any nerves and blood vessels. Therefore, the transdermal absorption rate and dosage of most drugs are difficult to meet the administration requirements. Drug delivery through microneedles can largely solve this problem. After the microneedle pierces the stratum corneum of the skin, a tiny drug channel will be formed, and the drug can enter the skin through the drug channel, which greatly improves the utilization rate of the drug. Moreover, the microneedles are thin and sharp, and the puncture depth is generally only a few hundred microns, and will...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/24A61K47/36A61K47/40A61K47/26A61K47/32A61K31/58A61K31/519A61K31/5383A61M37/00
CPCA61K9/0021A61K31/519A61K31/5383A61K31/58A61K47/24A61K47/26A61K47/32A61K47/36A61K47/40A61M37/0015A61M2037/0053
Inventor 朱锦涛王华李钰策张连斌柳佩陶娟朱今巾杜虹瑶
Owner HUAZHONG UNIV OF SCI & TECH
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