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Insulin-loaded nanoparticles and application thereof

A nanoparticle, loaded technology, applied in the field of insulin loaded nanoparticles, can solve problems such as poor patient compliance, and achieve the effect of good thermal stability and uniform size

Active Publication Date: 2018-11-02
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insulin administration is the first choice for the treatment of type 1 diabetes, mainly injection therapy, but long-term frequent injections lead to poor patient compliance, local subcutaneous tissue, cell proliferation or hardening, and high insulin response

Method used

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  • Insulin-loaded nanoparticles and application thereof
  • Insulin-loaded nanoparticles and application thereof
  • Insulin-loaded nanoparticles and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1 Preparation of Nanoparticles

[0083] 1. Experimental operation

[0084] Prepare 5 mg / ml KGM solution, take 2 ml KGM solution, add 1 mg insulin, and mix well.

[0085] Prepare 5mg / ml ConA solution, take 1.88ml ConA solution, add 100μL KCl solution (0.1 M), 10μL CaCl 2 Solution (0.01 mM), 10μL of MnCl 2 Solution (0.01 mM), finally get 2ml mixed solution, ConA solution, KCl solution, CaCl in the whole system 2 Solution, MnCl 2 The molar concentration ratio of the solution is 9.8×10 4 : 1×10 4 :1:1. Shake at a constant speed for 6 h at room temperature.

[0086] Add 2ml of the activated ConA solution and the cross-linking agent sodium trimetaphosphate to the solution dissolved with KGM and insulin so that the final concentration of the cross-linking agent sodium trimetaphosphate is 0.125 mg / ml. Shake well at 4℃ for 1 h . Then the solution was placed in 120ml PBS solution (pH 6.8) and magnetically stirred for 4 h. KGM and ConA were cross-linked to form insulin-loaded na...

Embodiment 2

[0089] Example 2 Glucose Sensitive Detection of Particles

[0090] 1. Experimental operation

[0091] The KGM-INS-ConA nanoparticles prepared in Example 1 were placed in glucose solutions of different concentrations (0 mg / dl, 100 mg / dl, 400 mg / dl) for in vitro release. Observe the dissolution and release of particles by centrifugation at three time points of 0 h, 4 h, and 8 h, and take pictures for observation.

[0092] 2. Experimental results

[0093] Such as figure 1 It shows that the structure of KGM-INS-ConA nanoparticles undergoes reversible loose or tight changes when the glucose concentration increases or decreases.

[0094] KGM-INS-ConA nanoparticles were added to glucose solutions of different concentrations (0 mg / dl, 100 mg / dl, 400 mg / dl), and it was observed that the particles in the glucose solutions of different concentrations were at 0 h, 4 h, 8 The amount of dissolution increased in different degrees at h (such as figure 2 ). Comparing the dissolution of particles in ...

Embodiment 3

[0095] Example 3 Nanoparticle precipitation comparison

[0096] 1. Experimental operation

[0097] The KGM-INS-ConA nanoparticles and KGM-INS nanoparticles prepared in Example 1 were centrifuged (5000 rpm) to collect the precipitate and observe

[0098] 2. Experimental results

[0099] Obvious white precipitates can be seen in the KGM-INS-ConA nanoparticle centrifuge tube, and there is almost no white precipitate in the same position of the KGM-INS nanoparticle centrifuge tube (such as image 3 ). It can be seen that, due to the specific binding between KGM and ConA, KGM-INS-ConA nanoparticles loaded with insulin are formed. Without ConA, KGM cannot be combined with it, and there is almost no obvious formation of nanoparticles. This indicates that the cross-linking of ConA and KGM can form a carrier for insulin transport, and ConA is an important raw material for preparing insulin-loaded nanoparticles.

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Abstract

The invention discloses insulin-loaded nanoparticles. The insulin-loaded nanoparticles are obtained by carrying out reversible crosslinking reaction on glucomannan, concanavalin A and a crosslinking agent. The invention develops glucose induction type insulin oral nanoparticles prepared from a natural polymer; a glucose induction type insulin oral transportation system can be constructed by utilizing the nanoparticles; the system has basic properties of a transportation system which has glucose induction performance, can control blood glucose and has low toxin; the insulin-loaded nanoparticleshave a relatively good effect in bodies and have a slow glucose lowering effect for relatively long time; the blood glucose control curative effect of the glucose induction type insulin oral transportation system is improved, and the insulin-loaded nanoparticles have relatively great application potential in the fields of development of diabetes mellitus treatment, natural polymer medical functions and the like.

Description

Technical field [0001] The present invention relates to the technical field of treatment of diabetes, and more specifically, to a nanoparticle loaded with insulin and its application. Background technique [0002] Diabetes is an endocrine disease, manifested by persistent high blood sugar, which easily induces complications in the patient's eyes, heart, kidneys, feet, blood vessels, nerves and other tissues and organs. At present, the number of diabetic patients in the world is still increasing, and diabetes has become one of the diseases that endanger human health. Insulin administration is the first choice for the treatment of type I diabetes, mainly injection therapy, but frequent injections for a long time lead to poor patient compliance, local subcutaneous tissue, cell proliferation or sclerosis, and high insulin response. Therefore, many studies are devoted to the application of nanomaterials to deliver insulin via oral route, which can alleviate the discomfort of patients...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/51A61K47/36A61K47/42A61P3/10
CPCA61K38/28A61P3/10A61K9/0053A61K9/5161A61K9/5169
Inventor 关燕清张丽丘佳妮
Owner SOUTH CHINA NORMAL UNIVERSITY
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