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Method for preparing oral insulin-loaded nano-micelles

A technology of nano-micelle and insulin, which is applied in the field of preparation of insulin-loaded nano-micelle, which can solve the problems of difficult absorption, insulin degradation and inactivation, and drug failure, and achieve high drug loading, encapsulation efficiency, stability and dispersion Good sex, relief of pain and inconvenience

Inactive Publication Date: 2017-12-29
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insulin is a polypeptide drug, which has the disadvantages of short half-life and easy destruction in the body. Since polypeptide drugs are easily destroyed after oral administration, the drug is ineffective. Therefore, insulin is mainly administered clinically by injection at present.
However, long-term frequent insulin injections not only bring great pain and inconvenience to patients, but also often cause side effects such as local skin edema, bruising, infection, and subcutaneous fat atrophy.
Therefore, oral administration of insulin has become a research hotspot for researchers at home and abroad. However, there are two main problems in oral administration of insulin: one is that insulin is easily degraded and inactivated by acid and enzyme in the gastrointestinal tract; the other is that insulin has a large molecular weight. , poor membrane permeability, difficult to be absorbed

Method used

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  • Method for preparing oral insulin-loaded nano-micelles
  • Method for preparing oral insulin-loaded nano-micelles
  • Method for preparing oral insulin-loaded nano-micelles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Preparation of insulin-loaded nanomicelles

[0039] Polymer P(MMA 30 -co-MAA 35 )-b-PAEMA 40 (Average molecular weight = 11529) 100mg, organic solvent N,N-dimethylformamide 10ml according to the mass ratio of 0.009:1 at 25 ℃ for 12h to form a polymer solution; insulin 10mg, pH = 2.0 medicinal hydrochloric acid 10ml of the solution was made into insulin acid solution according to the mass ratio of 0.001:1; under stirring at 25°C, slowly add the insulin solution dropwise into the polymer solution, continue stirring at 25°C for 0.5h, and then transfer the polymer micellar solution into the dialysis bag (Molecular weight cut-off MWCO=7000D), dialyze with acetic acid-sodium acetate buffer solution with pH=5.0 for 24h to remove the organic solvent and unencapsulated free drug in the micellar solution, in which the polymer micellar solution and acetic acid-acetic acid The volume ratio of sodium buffer solution was 1:100. During the dialysis process, the dialysate was cha...

Embodiment 2

[0054] Embodiment 2 operation steps are the same as embodiment 1, polymer is changed into P(MMA 30 -co-MAA 35 )-b-P(AEMA) 30 (average molecular weight = 9907) was used to prepare insulin-loaded nanomicelles. The potential of the obtained insulin-loaded nanomicelles was 15.7mV, the particle size was 213.8nm, the drug loading was 5.9%, and the encapsulation efficiency was 62.4%.

Embodiment 3

[0055] Embodiment 3 operation steps are the same as embodiment 1, polymer is changed into P(MMA 30 -co-MAA 45 )-b-P(AEMA) 30 (average molecular weight = 12457) was used to prepare insulin-loaded nanomicelles. The potential of the obtained insulin-loaded nanomicelles was 11.2mV, the particle size was 575.2nm, the drug loading was 7.0%, and the encapsulation efficiency was 74.1%.

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Abstract

The invention discloses a method for preparing insulin-loaded nano-micelles with pH (potential of hydrogen) sensibility and membrane adhesive ability. The method includes dissolving insulin in dilute acid solution to form insulin solution; dissolving poly (methyl methacrylate-co-methacrylic acid)-b-polymethacrylic acid ammonia ethyl ester copolymers P (MMA-co-MAA)-b-PAEMA in organic solvents to form polymer solution; slowly adding the insulin solution into the polymer solution; removing the solvents by means of dialysis in acetic acid-sodium acetate buffer solution with the pH of 5.0-6.0; carrying out centrifuging and freeze drying to obtain the insulin-loaded nano-micelles. The method has the advantages that the prepared insulin-loaded nano-micelles with the pH sensibility and the membrane adhesive ability are suitable for oral administration, have uniform particle sizes and are high in medicine loading capacity and entrapment efficiency.

Description

technical field [0001] The invention relates to the technical field of drug-loaded nanoparticle micelles, in particular to a method for preparing insulin-loaded nanomicelles. Background technique [0002] Diabetes has become a major killer threatening human health. For type 1 diabetes, insulin is the only drug to lower blood sugar; for type 2 diabetes, insulin can promote the regeneration of islet cells. Insulin is a polypeptide drug, which has the disadvantages of short half-life and easy destruction in the body. Because polypeptide drugs are easily destroyed after oral administration, making the drug ineffective, insulin is currently mainly administered clinically by injection. However, long-term frequent insulin injections not only bring great pain and inconvenience to patients, but also often cause side effects such as local skin edema, bruising, infection, and subcutaneous fat atrophy. Therefore, oral administration of insulin has become a research hotspot for researc...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K9/107A61K47/32A61K31/704A61K31/337A61K31/405A61P3/10
Inventor 曾繁楚杨倩倩吴志民刘跃进李丹
Owner XIANGTAN UNIV
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