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Polypeptide nanoparticle for treating diabetes mellitus, polypeptide nanoparticle microneedle and preparation method of polypeptide nanoparticle microneedle

A technology of nanoparticles and diabetes, which is applied in the field of pharmaceutical preparations and its preparation, can solve the problems of low drug loading, limit the large-scale production and application of microneedles, and low drug stability, achieve low hygroscopicity, and cause skin allergic reactions , less prone to skin allergic reactions

Inactive Publication Date: 2020-04-24
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, low drug loading and low drug stability are the main factors that limit the large-scale production and application of microneedles.

Method used

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  • Polypeptide nanoparticle for treating diabetes mellitus, polypeptide nanoparticle microneedle and preparation method of polypeptide nanoparticle microneedle
  • Polypeptide nanoparticle for treating diabetes mellitus, polypeptide nanoparticle microneedle and preparation method of polypeptide nanoparticle microneedle
  • Polypeptide nanoparticle for treating diabetes mellitus, polypeptide nanoparticle microneedle and preparation method of polypeptide nanoparticle microneedle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The preparation method of polypeptide nanoparticles loaded with polypeptide drugs is as follows:

[0052] 1. Use 0.2% acetic acid solution to prepare low molecular weight chitosan solutions with concentrations of 2mg / ml; 2.5mg / ml; 1mg / ml; 0.5mg / ml respectively, and stir and swell for 12h;

[0053] 2. Prepare a sodium tripolyphosphate solution with a concentration of 1.2mg / ml; 0.8mg / ml; 0.4mg / ml; 0.2mg / ml with deionized water;

[0054] 3. Prepare an exenatide acetate solution with a concentration of 10 μg / ml with deionized water;

[0055] 4. Add the sodium tripolyphosphate and exenatide acetate mixture dropwise to the chitosan solution under stirring at a speed of 200, 400, 600, 800, 1000, 1200 rad / min (mixed at a volume ratio of 1:1) Make it into nanoparticle; obtain polypeptide nanoparticle powder after freeze-drying.

Embodiment 2

[0057] The encapsulation efficiency and drug loading capacity of the drug were measured by centrifugation with a fluorescent microplate reader. An appropriate amount of the prepared polypeptide nanoparticle solution was taken and centrifuged at 15,000 rad / min for 30 minutes. Calculate the encapsulation efficiency and drug loading of the drug.

[0058] Encapsulation rate = (m 投药 -m 上清液含药 ) / m 投药 ×100%

[0059] Drug loading = (m 投药 -m 上清液含药 ) / m 载药纳米粒 ×100%

[0060] It was determined that the encapsulation efficiency and drug loading capacity of FITC-EX4 chitosan nanoparticles were 74.26% and 25.61%, respectively.

Embodiment 3

[0062] The in vitro release method of polypeptide nanoparticles for treating diabetes is as follows:

[0063] Get the exenatide chitosan nanoparticle solution 3ml that example 1 prepares in the 14K dialysis bag, set the aqueous solution that contains equal amount of exenatide and place in the dialysis bag as a control group, the dialysis bag is placed in 70ml pH7. 4PBS in a 100ml release tube. Put it into a full-temperature shaking incubator, set the shaking speed to 100rad / min, and shake at a temperature of 37°C. 1ml was sampled at 1, 2, 3, 6, 9, 12, 24, 36, 60, and 72 hours respectively, and the same volume of pH 7.4 PBS was added at the same time.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations and preparation methods thereof, and particularly relates to a polypeptide nanoparticle for treating diabetes, a polypeptidenanoparticle microneedle and a preparation method of the polypeptide nanoparticle microneedle. The method comprises the following steps: 1) preparing chitosan nanoparticles entrapped with exenatide;2) preparing a polymer composite microneedle with strong hardness, high solubility and good biocompatibility by a physical crosslinking technology; and 3) freeze-drying the nanoparticles into a powder, and loading the powder into the polymer microneedle to prepare the dry powder drug-loaded microneedle. The exenatide nanoparticle freeze-dried powder is loaded by utilizing holes naturally formed inthe preparation process of the polymer microneedle to prepare the exenatide dry powder microneedle for treating type 2 diabetes. A exenatide chitosan nanoparticle microneedle transdermal patch disclosed by the invention can effectively reduce the risks of strong inflammation and immune system reaction caused by the medicine, so the painless, needleless, transdermal and slow blood glucose-releasing purposes are achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and preparation methods thereof, and in particular relates to a polypeptide nanoparticle for treating diabetes, a polypeptide nanoparticle microneedle and a preparation method thereof. Background technique [0002] As of 2017, the International Diabetes Federation (IDF) counted as many as 451 million people with diabetes worldwide. In 2017 alone, the number of deaths caused by diabetes reached 5 million. Since diabetes is prone to comorbidities such as neuropathy, end-stage renal disease, retinopathy, and cardiovascular disease, the annual cost of diabetes-related treatment reaches more than 850 billion US dollars. The high prevalence and high cost of treatment of diabetes have brought a great burden to the financial and health systems of countries all over the world. [0003] Type II diabetes, also known as adult-onset diabetes, mostly occurs after the age of 35, accounting f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/22A61K9/19A61K9/70A61K47/38A61K9/14A61P3/10
CPCA61K38/22A61K9/19A61K9/7023A61K9/0021A61K9/146A61K47/38A61P3/10
Inventor 严琴英翁嘉绮杨根生郭钫元王炜炜陈凡方敏文娇丽
Owner ZHEJIANG UNIV OF TECH
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