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Double-drug-loaded polymer microneedle used for oral mucosa administration and preparation method of double-drug-loaded polymer microneedle

An oral mucosa and polymer technology, which is applied in the field of polymer microneedles loaded with dual drugs and their preparation, can solve problems such as difficulty in achieving curative effects, and achieve the effects of precise delivery, improved drug availability, and improved therapeutic effects.

Active Publication Date: 2021-09-03
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is sometimes difficult to achieve good curative effect by using a single GCs clinically.

Method used

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  • Double-drug-loaded polymer microneedle used for oral mucosa administration and preparation method of double-drug-loaded polymer microneedle
  • Double-drug-loaded polymer microneedle used for oral mucosa administration and preparation method of double-drug-loaded polymer microneedle
  • Double-drug-loaded polymer microneedle used for oral mucosa administration and preparation method of double-drug-loaded polymer microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] In this example, the water-soluble fluorescent dye sulforhodamine B (SRB) and the water-soluble fluorescent dye fluorescein isothiocyanate (FITC) were used as hydrophilic drug models to prepare two loaded drugs for oral mucosal administration. Polymer microneedles for hydrophilic drugs, the preparation process is as follows figure 1 As shown, the steps are as follows:

[0056] (1) Prepare the solution

[0057] Dissolve methacrylylated hyaluronic acid (HAMA), SRB and photoinitiator phenyl 2,4,6-trimethylbenzoyllithium phosphonate (LAP) in deionized water, let stand to remove air bubbles, Obtain solution A; in solution A, the concentration of HAMA is 100 mg / mL, the concentration of SRB is 1 mg / mL, and the concentration of LAP is 0.0025 mg / mL.

[0058] Dissolve HA and FITC in deionized water, let stand to remove air bubbles, and obtain solution B; in solution B, the concentration of HA is 300 mg / mL, and the concentration of FITC is 1 mg / mL.

[0059] Dissolve PVP in abso...

Embodiment 2

[0075] In this example, the drug-loaded polymer microneedles prepared in Example 1 were characterized and their dimensions were measured by scanning electron microscopy.

[0076] Paste the drug-loaded polymer microneedle on the sample stage, spray gold for 60s and then purge with nitrogen gas, observe its microscopic morphology and measure the size of the microneedle with a scanning electron microscope, the results are as follows Image 6 shown. Image 6 Figures (a) and (c) show that the drug-loaded polymer microneedles prepared in Example 1 are formed by a series of solid quadrangular pyramid-shaped drug-loaded microneedles arranged on the substrate (100, 10×10 matrix), The structure of the drug-loaded microneedle is uniform and complete, and the needle shape is sharp. from Image 6 It can be seen from the two figures (b) and (d) that the height of the drug-loaded microneedles is about 480 μm, and the length of the bottom of the drug-loaded microneedles is about 200 μm. In ...

Embodiment 3

[0078] In this example, SRB and the water-soluble dye methylene blue (MB) were used as the hydrophilic drug model to prepare polymer microneedles loaded with two hydrophilic drugs for oral mucosal administration, and the preparation method was basically the same as in the example , the only difference is that the concentration of SRB in solution A is 15 mg / mL, and the concentration of MB in solution B is 15 mg / mL.

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Abstract

The invention provides a double-drug-loaded polymer microneedle used for oral mucosa administration. The polymer microneedle is composed of a substrate and drug-loaded microneedles distributed on one side of the substrate in an array, each drug-loaded microneedle is composed of a tip part, a middle part and a bottom part, and the tip part and the middle part are loaded with drugs; the base material of the tip part is a degradable biocompatible high polymer material with a three-dimensional network structure, and the base materials of the middle part and the bottom part are water-soluble biocompatible high polymer materials; and after the polymer microneedle is administrated through the oral mucosa, the substrate and the middle part of the drug-loaded microneedle are dissolved firstly to release the drug loaded on the middle part, the tip part of the drug-loaded microneedle is separated from the middle part and is retained in the oral mucosa, and the drug loaded on the tip part is gradually released along with swelling and degradation of the base material of the tip part. The polymer microneedle can realize gradient order drug release, and can better realize drug combined treatment of oral mucosa diseases.

Description

technical field [0001] The invention belongs to the field of transmucosal drug delivery systems, and relates to a polymer microneedle loaded with dual drugs for oral mucosal drug delivery and a preparation method thereof. Background technique [0002] Microneedles (MNs) are a novel drug delivery system that provides a painless solution for breaking tissue barriers. Microneedles are micro-arrays composed of micron-sized needles. The height of the needles is generally between 25 and 2000 μm. The drug delivery mechanism is to create micropores on the surface of the tissue, break the physiological barrier, and relieve the delivery of hydrophilic drugs and macromolecular drugs. Confinement, delivering drugs directly into tissues. Due to the small size of the microneedle, it will not irritate the nerves deep in the tissue during use. The administration process is painless, minimally invasive and safe, which can improve patient compliance, especially for children and the elderly. ...

Claims

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Application Information

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IPC IPC(8): A61M37/00A61K9/00A61K31/58A61K31/573A61K31/715A61K47/36A61K47/38A61K47/32A61K47/42A61P1/02
CPCA61M37/0015A61K9/0021A61K9/006A61K31/58A61K31/573A61K31/715A61K47/36A61K47/38A61K47/32A61K47/42A61P1/02A61M2037/0053A61K2300/00
Inventor 巨晓洁李新娇褚良银江潞汪伟刘壮谢锐
Owner SICHUAN UNIV
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