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Insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particle and preparation method thereof

A polylysine and fatty acid technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of high scale production cost, complex synthesis process, etc. Low cost, simple synthesis process, and low insulin burst performance

Pending Publication Date: 2022-06-17
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the problems of phenylboronic acid-based polymer particles

Method used

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  • Insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particle and preparation method thereof
  • Insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particle and preparation method thereof
  • Insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0047]实施例1：

[0048]将1.2856g 4-羧基-3-氟苯硼酸、0.2649g正丁酸、1.9120g 1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐和1.1563g N-羟基丁二酰亚胺投入90g二甲基亚砜和10克水中搅拌，得到混合物A，搅拌速率为400rpm，时间为90min，温度为常温。将1.0004gε-聚赖氨酸投入10g水中搅拌，搅拌速率为400rpm，时间为10min，温度为常温，得到混合物B。将混合物A和混合物B混合搅拌，搅拌速率为500rpm，时间为2000min，温度为常温，得到混合物C。将混合物C装入透析袋，透析袋截留分子量为1000Da，装有混合物C的透析袋置于水中透析，每隔一段时间将透析水换为新鲜水，每次换水时间间隔为6h，换水次数为9次，透析水体积为3升。透析完毕后，将透析袋中的混合物冻干，得到产物苯硼酸 / 脂肪酸双改性ε-聚赖氨酸。

Example Embodiment

[0049]实施例2：

[0050]将1.2705g 4-羧基-3-氟苯硼酸、0.2923g正己酸、1.7997g 1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐和1.0925g N-羟基丁二酰亚胺投入50g二甲基亚砜、25g N，N-二甲基甲酰胺和25g N，N-二甲基乙酰胺中搅拌，得到混合物A，搅拌速率为400rpm，时间为90min，温度为常温。将1.0202gε-聚赖氨酸投入10g水中搅拌，搅拌速率为400rpm，时间为10min，温度为常温得到混合物B。将混合物A和混合物B混合搅拌，搅拌速率为500rpm，时间为2000min，温度为常温，得到混合物C。将混合物C装入透析袋，透析袋截留分子量为1000Da，装有混合物C的透析袋置于水中透析，每隔一段时间将透析水换为新鲜水，每次换水时间间隔为6h，换水次数为9次，透析水体积为4升。透析完毕后，将透析袋中的混合物冻干，得到产物苯硼酸 / 脂肪酸双改性ε-聚赖氨酸。

Example Embodiment

[0051]实施例3：

[0052]将1.3005g 4-羧基-3-氟苯硼酸、0.3626g正辛酸、1.9001g 1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐和1.0005g N-羟基丁二酰亚胺投入70g二甲基亚砜和30g四氢呋喃中搅拌，得到混合物A，搅拌速率为400rpm，时间为90min，温度为常温。将1.0006gε-聚赖氨酸投入10g水中搅拌，搅拌速率为400rpm，时间为10min，温度为常温得到混合物B。将混合物A和混合物B混合搅拌，搅拌速率为500rpm，时间为2000min，温度为常温，得到混合物C。将混合物C装入透析袋，透析袋截留分子量为1000Da，装有混合物C的透析袋置于水中透析，每隔一段时间将透析水换为新鲜水，每次换水时间间隔为6h，换水次数为9次，透析水体积为3升。透析完毕后，将透析袋中的混合物冻干，得到产物苯硼酸 / 脂肪酸双改性ε-聚赖氨酸。

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Abstract

The invention discloses insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particles and a preparation method thereof. The phenylboronic acid/fatty acid dual-modified epsilon-polylysine particles are prepared through a grafting reaction, and insulin-loaded dual-modified epsilon-polylysine particles are prepared by soaking the phenylboronic acid/fatty acid dual-modified epsilon-polylysine particles in an insulin solution. The preparation method disclosed by the invention is simple; the insulin-loaded dual-modified epsilon-polylysine particles have low insulin burst release performance, can automatically adjust the release dose of insulin according to the real-time blood glucose level, can effectively relieve the symptom of hyperglycemia, and meanwhile, avoids the problem of hypoglycemia caused by excessive insulin; the insulin-loaded phenylboronic acid/fatty acid dual-modified epsilon-polylysine particles can be used for delivering insulin by adopting subcutaneous injection and microneedle transdermal delivery modes.

Description

technical field [0001] The invention belongs to the technical field of polymer materials, and in particular relates to insulin-loaded phenylboronic acid / fatty acid double-modified ε-polylysine particles and a preparation method thereof. Background technique [0002] Diabetes is a chronic disease characterized by hyperglycemia, with 537 million diabetics worldwide (2021 data from the International Diabetes Federation). The cause of diabetes is the impairment or complete loss of insulin secretion function, which may also lead to damage to the functions of the heart, nerves, eyes, kidneys, etc. as the disease progresses, thereby threatening life safety. The administration of exogenous insulin can significantly alleviate the symptoms of hyperglycemia in diabetic patients, but the inaccurate dosage during the treatment is the main reason for the poor blood sugar control in diabetic patients, and hypoglycemia caused by excessive dosage is particularly fatal. Therefore, exogenous ...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K9/16A61K9/00A61K47/34A61P3/10
CPCA61K38/28A61K9/1641A61K9/0021A61P3/10
Inventor 俞豪杰沈迪王立
Owner ZHEJIANG UNIV
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