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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 even form a clear and transparent solution. Therefore, so far, there have been no research reports on the preparation of nanoscale or microscale drug delivery carriers by combining insulin, phospholipids, and chitosan in any form.

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

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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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