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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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  • 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 phase transition temperature), release faster when lower than LCST temperature, better meet the requirements of controlled release (Afrassiabi AL, Hoffman AS, Cadwell LA. Effect of temperature on the release rate of biomolecules from thermally reversible hydrogels. J Membrane Sci 1986, 33: 191-200); however, this gel system has the problem that the LCST is too low, and it cannot be automatically "on-off" according to the glucose concentration change at body temperature "Release insulin

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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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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