Glucose-sensitive self-regulated insulin release micro-gel carrier and preparation method thereof

A glucose-sensitive, microgel technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of slow release, automatic "on-off" release of insulin, Low LCST issues, to achieve good biocompatibility

Inactive Publication Date: 2015-05-06
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Current phenylboronic acid systems have the disadvantage of displacing glycosylated insulin even at low glucose concentrations (i.e. euglycemia) and therefore cannot be counted as A truly autonomous insulin delivery system
Afrassiabi AL et al. improved and synthesized PNIPAAm and P(NIPAAm-co-MAAc) gels, and studied the controlled release characteristics of these temperature-sensitive gels to myoglobin. The results showed that high temperature Release slowly when LCST (volume ph

Method used

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  • Glucose-sensitive self-regulated insulin release micro-gel carrier and preparation method thereof
  • Glucose-sensitive self-regulated insulin release micro-gel carrier and preparation method thereof
  • Glucose-sensitive self-regulated insulin release micro-gel carrier and preparation method thereof

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Experimental program
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Embodiment 1

[0044] (1) Synthesis of vinyl functional group RGD polypeptide: Glycine (FMOC-Gly-OH) protected by 9-fluorenylmethoxycarbonyl group from the amino group, carboxyl group on the amino group and side group were respectively protected by 9-fluorenylmethoxycarbonyl group and tert-butyl The protected aspartic acid (FMOC-Asp(OtBu)-OH), the amino group and the guanidine group on the side group were respectively replaced by 9-fluorenylmethoxycarbonyl and 2,2,4,6,7-pentamethyl-2H- Starting from benzofuran-5-sulfonyl-protected arginine (FMOC-Arg(Pbf)-OH), a small molecule polypeptide containing RGD sequence was synthesized by means of peptide solid-phase synthesis, and then reacted with acrylic acid to obtain a vinyl function The RGD sequence small molecule polypeptide with a strong hydrophilic group, the synthesis steps are as follows (see the synthesis schematic diagram figure 1 ).

[0045] Weigh 1.50 g of 2-chlorotrityl chloride resin, put it into a porous filter funnel polypepti...

Embodiment 2

[0070] (1) Synthesis of vinyl functional group RGD polypeptide: see Example 1.

[0071] (2) Synthesis of 3-acrylamidophenylboronic acid: See Example 1.

[0072] (3) Preparation of glucose-sensitive microgel: Weigh 118.4 mg (0.62 mmol, 9.3 mol%) of monomer 3-acrylamidophenylboronic acid, 280 mg (0.7 mmol, 10.5 mol%) of hydrophilic RGD polypeptide containing vinyl functional groups mol%), N - Isopropylacrylamide 565 mg (5 mmol, 74.9 mol%) and cross-linking agent N,N' -Methylenebisacrylamide 32.3 mg (0.21 mmol, 3.1 mol%), and measure 100 mL of distilled water, add it to a three-necked flask equipped with a condensing device, a nitrogen conduit, a constant pressure dropping funnel, and a magnetic stir bar, and open the Stir, blow nitrogen for 30 min, and heat to 60-80 o C, 34.2 mg (0.15 mmol, 2.2 mol%) of the initiator ammonium persulfate (APS) was added through a constant-pressure dropping funnel at a speed of 1000 r / min, and reacted for 24 h under a nitrogen atmosphere to pr...

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Abstract

The invention provides a glucose-sensitive self-regulated insulin release micro-gel carrier and a preparation method thereof. The preparation method of the glucose-sensitive self-regulated insulin release carrier comprises the following steps: performing free radical polymerization on three monomers namely 3-acryloyl aminophenylboronic acid, hydrophilic RGD polypeptide containing ethenyl functional groups and N-isopropylacrylamide to obtain a glucose-sensitive nano gel, and then combining the glucose-sensitive nano gel with insulin to obtain a medicine-loaded micro-gel. According to the glucose-sensitive self-regulated insulin release micro-gel carrier provided by the invention, the release of insulin can be automatically 'opened and closed' according to the changes of glucose concentrations at human body temperature.

Description

technical field [0001] The invention designs a glucose responsive microgel system capable of self-regulating and releasing insulin according to the blood sugar level. The invention belongs to the technical fields of drug controlled release and biomaterials. Background technique [0002] Diabetes mellitus is a group of common diseases characterized by hyperglycemia. It is a syndrome of sugar, fat, protein and electrolyte metabolic disorders caused by defects in insulin secretion and its biological effects or both. At present, there is no cure for diabetes. , can only delay and control the symptoms of diabetes through a variety of treatment methods. Although people have developed oral hypoglycemic agents such as sulfonylurea insulin secretagogues, biguanide hypoglycemic agents, α-glucosidase inhibitors, and thiazolidinedione insulin sensitizers, insulin therapy is still a major problem in type Ⅰ diabetes. (i.e. insulin-dependent diabetes mellitus), the drug of choice for dis...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K38/28A61K47/42A61K47/34A61P3/10
Inventor 刘红杜鹏陈勇王宗春
Owner HUBEI UNIV
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