Novel insulin-phospholipid-chitosan self-assembled microparticle carrier and preparation thereof

A technology of insulin and chitosan, which is applied in the field of medicine, can solve problems such as the inability to form a clear and transparent solution, and achieve the effects of avoiding protein denaturation and drug leakage, high encapsulation rate, and low burst release

Active Publication Date: 2016-06-01
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insulin is not only highly hydrophilic, but also a macromolecular drug, and it is difficult to be entrapped into the self-assembled nanoparticles of phospholipid chitosan. Moreover, insulin, phospholipid and chitosan cannot eve

Method used

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  • Novel insulin-phospholipid-chitosan self-assembled microparticle carrier and preparation thereof
  • Novel insulin-phospholipid-chitosan self-assembled microparticle carrier and preparation thereof
  • Novel insulin-phospholipid-chitosan self-assembled microparticle carrier and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Embodiment 1: insulin phospholipid complex series

[0042] According to the method described in the invention patent application 201180002259.4, the mass ratio of insulin:phospholipids is respectively 1:3, 1:5, 1:10, 1:20 and 1:50, and the preparation is as follows:

[0043] The prescribed amount of insulin was dissolved in methanol solution containing trifluoroacetic acid; the prescribed amount of soybean lecithin was dissolved in methylene chloride, and the above two solutions were mixed to form a clear solution. Rotate the solution under reduced pressure at 30-50°C until the solvent is evaporated to dryness, then blow with nitrogen to evaporate the residual solvent, place it in a vacuum drying oven, scrape it into a closed container after drying, and obtain a series of insulin Dry powders of phospholipid complexes, labeled complexes A, B, C, D, E.

[0044] In the above method, trifluoroacetic acid is replaced by glacial acetic acid, and other conditions remain uncha...

Embodiment 2

[0049] Embodiment 2: insulin phospholipid complex series

[0050] The mass ratio of insulin: phospholipids was 1:3, 1:5, 1:10, 1:20 and 1:50 respectively, and prepared as follows:

[0051] Take the prescribed amount of insulin and dissolve it in DMSO solution containing glacial acetic acid; dissolve the prescribed amount of soybean lecithin in DMSO, and mix the above two solutions to form a clear solution. This solution was lyophilized to obtain a series of dry powders of insulin-phospholipid complexes, labeled as complexes F, G, H, I, J.

Embodiment 3

[0052] Embodiment 3: insulin phospholipid complex series

[0053] Dissolve 10 mg of insulin in acid-containing methanol solution; dissolve 100 mg of egg yolk lecithin in dichloromethane, and mix the above two solutions to form a clear solution. Rotate the solution under reduced pressure at 30-50°C until the solvent is evaporated to dryness, then blow with nitrogen to evaporate the residual solvent, place it in a vacuum drying oven, scrape it into a closed container after drying, and obtain a series of insulin Dry powder of phospholipid complex, labeled as complex K.

[0054] In the above method, synthetic phospholipids are substituted for egg yolk phospholipids, and the other conditions remain unchanged to obtain complex L.

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Abstract

The invention discloses a novel insulin-phospholipid-chitosan self-assembled microparticle carrier and a drug delivery system thereof, wherein the mass ratio of insulin to phospholipid is 1 to (3-100); and the mass ratio of chitosan to the phospholipid is 1 to (5-50). The self-assembled microparticle carrier disclosed by the invention is prepared by preparing an insulin-phospholipid compound from the insulin and a proper amount of the phospholipid material in a special environment, injecting a non-aqueous solvent organic phase of the insulin-phospholipid compound to an aqueous-phase solution of the chitosan, and self-assembling in a warm stirring condition, so that the insulin-phospholipid-chitosan microparticle carrier is formed. The insulin-phospholipid-chitosan microparticle carrier disclosed by the invention is free from the addition of a cross-linking agent, is represented in a circular or elliptic form and has a multilayer capsule structure; the grain size distribution of the microparticle carrier is 50-5000nm and a drug entrapment rate reaches 70% or above; the microparticle carrier is good in quality stability in a gastrointestinal fluid environment and low in burst release; the microparticle carrier can break through the limitation of an enzyme barrier and a membrane barrier; and the microparticle carrier is used for preparing insulin non-injection drug delivery systems such as oral drug delivery, mucosal drug delivery, percutaneous drug delivery and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an insulin-phospholipid-chitosan self-assembled microparticle carrier with a lipid complex as an intermediate carrier and its preparation and preparation method. Background technique [0002] With the continuous development of biotechnology, the application of protein and peptide drugs is becoming more and more extensive. As a protein polypeptide drug with hypoglycemic effect, insulin has been administered clinically by injection for many years. Long-term frequent injections cause great discomfort and pain to patients. Therefore, the non-injection method of insulin has given Drugs have been receiving a lot of attention. Among them, the administration of insulin by oral administration can simulate the metabolic mode of insulin in the body, so it has become a research hotspot in the way of insulin administration. In view of the main problems faced by its oral administration, suc...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K47/24A61K47/36A61K9/14A61P3/10
Inventor 刘玉玲刘黎瑶周翠萍夏学军董武军
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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