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Microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine and preparation method of microneedle patch

A technology of polylysine and insulin, which is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, and pharmaceutical formulas, etc. It can solve the problems of non-degradable particles, high preparation costs, and unfavorable disease control. Achieve the effect of low production cost, mild loading process and pain-free

Inactive Publication Date: 2021-08-10
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First, the pain caused by subcutaneous injection is strong, and patients need to inject insulin subcutaneously 2 to 3 times a day, so the burden of injection pain is greater for patients
Second, in order to control blood sugar at a normal level (100-200mg / dL), patients need to adjust the dosage of insulin more accurately. Insufficient dosage of insulin will keep blood sugar at high blood sugar level, and excessive dosage will lead to hypoglycemia. unfavorable
The first type is reported by Wang et al. The method of free radical polymerization is used to synthesize phenylboronic acid-based particles. The particles are not degradable, so there are hidden dangers in the safety of long-term use.
Patent CN109125912A reported the second type of microneedle patch containing insulin-loaded phenylboronic acid-based particles. The phenylboronic acid-based particles were prepared based on the modification technology of gold nanoclusters. The biocompatibility is good, but the preparation cost is high

Method used

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  • Microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine and preparation method of microneedle patch
  • Microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine and preparation method of microneedle patch
  • Microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine and preparation method of microneedle patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1: microneedle patch

[0055] Mix 0.1010g of pullulan, 1.0172g of water and 0.0250g of insulin-loaded phenylboronic acid-based ε-polylysine particles to obtain the precursor of the microneedle patch. Add the precursor to the female microneedle mold, centrifuge at 3500rpm for 40min at a temperature of 25°C, inject the precursor into the needle groove of the female microneedle mold, and dry the precursor. The drying temperature is 30°C, the pressure is 0.1MPa, and the drying time is 24h. The microneedle patch obtained after drying is taken out to obtain a microneedle patch containing insulin-loaded phenylboronic acid-based ε-polylysine.

[0056] The results of this implementation case are as follows Figure 1-Figure 2 shown. figure 1 This is the electron micrograph of the microneedle patch containing insulin-loaded phenylboronic acid-based ε-polylysine. The microneedle patch was obtained through a simple centrifugation process, and the microneedle has a uniform...

Embodiment 2

[0058] Embodiment 2: microneedle patch

[0059] Mix 0.0562g of sodium hyaluronate, 1.0005g of water and 0.0251g of insulin-loaded phenylboronic acid-based ε-polylysine particles to obtain the precursor of the microneedle patch. Add the precursor to the female microneedle mold, centrifuge at 4000rpm for 100min at a temperature of 30°C, inject the precursor into the needle groove of the female microneedle mold, and dry the precursor. The drying temperature is 25°C, the pressure is 0.1MPa, and the drying time is 48h. The microneedle patch obtained after drying is taken out to obtain a microneedle patch containing insulin-loaded phenylboronic acid-based ε-polylysine.

Embodiment 3

[0060] Embodiment 3: microneedle patch

[0061] Mix 0.1002g of polyvinylpyrrolidone and 1.0005g of water with 0.0262g of insulin-loaded phenylboronic acid-based ε-polylysine particles to obtain the precursor of the microneedle patch. Add the precursor to the female microneedle mold, place it in a negative pressure environment, the pressure is 0.001MPa, the time is 0.5h, the temperature is 25°C, inject the precursor into the needle groove of the microneedle female mold, and dry the precursor. The drying temperature is 25°C, the pressure is 0.1MPa, and the drying time is 48h. The microneedle patch obtained after drying is taken out to obtain a microneedle patch containing insulin-loaded phenylboronic acid-based ε-polylysine.

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Abstract

The invention discloses a microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine and a preparation method of the microneedle patch. The microneedle patch is mainly composed of a substrate and microneedle bodies arranged on the substrate in an array mode, and the microneedle bodies and the substrate are made of polymers and phenylboronic acid base epsilon-polylysine loaded with insulin. The preparation method is simple, the raw materials are easy to obtain, and the biocompatibility is good; the problem of insulin inactivation is not generated, and phenylboronic acid-based epsilon-polylysine can be completely hydrolyzed, so that excretion of phenylboronic acid-based epsilon-polylysine particles in vivo is facilitated; the insulin-loaded phenylboronic acid-based epsilon-polylysine has glucose response performance and can automatically adjust the release rate and the release dosage of insulin; insulin can be delivered in a subcutaneous injection mode, and a microneedle of the microneedle patch containing the insulin-loaded phenylboronic acid-based epsilon-polylysine can effectively pierce the skin; the microneedle patch containing insulin-loaded phenylboronic acid-based epsilon-polylysine delivers insulin through a transdermal drug delivery method, so that the pain caused by subcutaneous injection of insulin can be avoided.

Description

technical field [0001] The invention belongs to the technical field of polymer materials, and in particular relates to a microneedle patch containing insulin-loaded phenylboronic acid-based ε-polylysine and a preparation method thereof. Background technique [0002] Diabetes mellitus is a chronic disease caused by the lack or impairment of insulin secretion function. It is mainly characterized by high blood sugar. In severe cases, it can further induce damage to the functions of the heart, nerves, eyes, and kidneys. According to statistics from the International Diabetes Federation, the number of people with diabetes in the world reached 463 million in 2019. With the aggravation of the disease, diabetic patients gradually increase their dependence on antidiabetic drugs, especially exogenous insulin. At present, subcutaneous insulin injection is a common method for diabetic patients to supplement exogenous insulin. However, the subcutaneous injection causes a strong sense o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K47/34A61K9/70A61P3/10
CPCA61K38/28A61K47/34A61K9/0021A61K9/7023A61P3/10
Inventor 俞豪杰沈迪王立
Owner ZHEJIANG UNIV
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