A kind of amino acid-chitosan nano drug loading system, its preparation method and application

A technology of chitosan nanometer and drug-loading system, which is applied in the fields of pharmaceutical formulations, nervous system diseases, and cardiovascular system diseases, etc. Reduce the effect of ischemic perfusion injury

Active Publication Date: 2022-03-22
WUHAN HONGYUE MEDICAL SCI INC
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Aiming at the above defects or improvement needs of the prior art, the present invention provides an amino acid-chitosan nano-loading system, its preparation method and application. The encapsulation efficiency and drug loading capacity are high, and the amino acid active ingredients are carried into the brain to achieve the purpose of amino acid administration in the central nervous system, thereby solving the technical problem of side effects caused by excessive peripheral drug administration

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  • A kind of amino acid-chitosan nano drug loading system, its preparation method and application
  • A kind of amino acid-chitosan nano drug loading system, its preparation method and application
  • A kind of amino acid-chitosan nano drug loading system, its preparation method and application

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[0046] The preparation method of the amino acid-chitosan nano-loading system provided by the invention comprises the following steps:

[0047] (1) Dissolving chitosan in deionized water and configuring a concentration of chitosan is a chitosan solution of 10-50 mg / mL;

[0048] (2) To the chitosan solution prepared in step (1), add 10-100 mg / mL of amino acid to be loaded, mix evenly, adjust the pH value between 5-7, and prepare a mixed solution;

[0049] (3) The mixed solution obtained in the step (2) is continuously stirred more than 30min, while adding concentration dropwise at 1-10mg / mL sodium tripolyphosphate (STPP) aqueous solution, making the mass ratio of chitosan and STPP at 100 ~150:1, the amino acid-chitosan nanometer drug delivery system provided by the invention is prepared.

[0050] Among them, the concentration of chitosan affects the morphology of nanoparticles to a certain extent. If it is too low, it will not be able to form nanoparticles, and if it is too hig...

Embodiment 1

[0065] An amino acid-chitosan nanometer drug-carrying system, which comprises chitosan nanospheres and amino acid active ingredients packaged therein; the chitosan nanospheres contain oligomeric chitosan And sodium tripolyphosphate; the average particle size is about 266nm, the Zeta potential is about 14mV, the drug loading is about 29%, the amino acid encapsulation rate is about 39%, and the total release in vitro is about 58% within 3 days.

[0066] The Mw of the oligomeric chitosan is 800-1000, and the degree of deacetylation is ≥93%.

[0067] The amino acid active ingredient is: proline.

[0068] The preparation method of the amino acid-chitosan nano-loading system provided by the present embodiment comprises the following steps:

[0069] (1) dissolving chitosan in deionized water and configuring a concentration of chitosan is a chitosan solution of 10 mg / mL;

[0070] (2) To the chitosan solution prepared in step (1), add 10 mg / mL of amino acid to be loaded, mix evenly, ...

Embodiment 2

[0074] An amino acid-chitosan nano drug-carrying system, which comprises chitosan nano-microspheres and amino acid active ingredients packaged therein; And sodium tripolyphosphate; the average particle size is about 227nm, the Zeta potential is about 16mV, the drug loading is about 28%, the amino acid encapsulation rate is about 40%, and the total release in vitro is about 55% within 3 days.

[0075] The Mw of the oligomeric chitosan is 800-1000, and the degree of deacetylation is ≥93%.

[0076] The amino acid active ingredient is: proline.

[0077] The preparation method of the amino acid-chitosan nano-loading system provided by the present embodiment comprises the following steps:

[0078](1) dissolving chitosan in deionized water and configuring a concentration of chitosan is a chitosan solution of 10 mg / mL;

[0079] (2) To the chitosan solution prepared in step (1), add 10 mg / mL of amino acid to be loaded, mix evenly, adjust the pH value between 5-7, and prepare a mixed ...

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Abstract

The invention discloses an amino acid-chitosan nano drug loading system, its preparation method and application. The drug-loading system includes chitosan nanospheres and amino acid active ingredients packaged therein; the chitosan nanospheres contain chitosan oligosaccharides and sodium tripolyphosphate in a mass ratio of 100 to 150:1, Amino acid encapsulation efficiency 30‑40%. The preparation method comprises: (1) dissolving chitosan in deionized water to prepare a chitosan solution with a concentration of 10-50 mg / mL; (2) adding 10-100 mg / mL of amino acid to be loaded, mixing evenly, and adjusting the pH Value is between 5-7, makes mixed solution; (3) constantly stir more than 30min, dropwise add concentration simultaneously in 1-10mg / mL sodium tripolyphosphate aqueous solution, make the quality of chitosan and sodium tripolyphosphate The ratio is between 100 and 150:1. The drug-carrying system is applied to the preparation of brain-injecting drugs.

Description

technical field [0001] The invention belongs to the field of nano drug loading, and more specifically relates to an amino acid-chitosan nano drug loading system, its preparation method and application. Background technique [0002] Stroke is a serious brain injury disease caused by cerebral blood vessel rupture causing bleeding or blockage causing ischemia. Acute attack, which is common in middle-aged and older people, is a major disease with the highest mortality and disability rates, and has a high recurrence rate and many complications. If it is not diagnosed and treated in time within 6 hours of the acute phase, it can cause serious complications and even death. Thrombolytic therapy is currently recognized as the most effective treatment for stroke. The time window for intravenous thrombolytic therapy for ischemic stroke is narrow. Intravenous thrombolysis is limited to 4.5 hours, and arterial thrombolysis can be extended appropriately. . [0003] The implementation o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/62A61K47/36A61K47/30A61K31/198A61K31/401A61K31/4172A61P9/10A61P7/04A61P25/00A61P25/28A61P25/16
CPCA61K9/5161A61K9/5115A61K9/0019A61K31/198A61K31/401A61K31/4172A61P9/10A61P7/04A61P25/00A61P25/28A61P25/16
Inventor 万芪高靖辰
Owner WUHAN HONGYUE MEDICAL SCI INC
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