Hyaluronic acid artesunate, nano-micelle preparation of hyaluronic acid artesunate, and preparation method and use of nano-micelle preparation

A technology of artesunate and nano micelles, applied in nanotechnology, nanotechnology, nanomedicine, etc., to achieve the effects of good responsive release characteristics, strong tumor cytotoxicity, and strong targeting

Pending Publication Date: 2020-12-18
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But up to now, there is no report of a kind of nano drug preparation combining ASA and HA

Method used

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  • Hyaluronic acid artesunate, nano-micelle preparation of hyaluronic acid artesunate, and preparation method and use of nano-micelle preparation
  • Hyaluronic acid artesunate, nano-micelle preparation of hyaluronic acid artesunate, and preparation method and use of nano-micelle preparation
  • Hyaluronic acid artesunate, nano-micelle preparation of hyaluronic acid artesunate, and preparation method and use of nano-micelle preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] (1) Dissolve ASA in dimethyl sulfoxide, add the activator EDC·HCl according to the molar ratio of ASA and activator as 1:2, carry out carboxyl activation at 45°C for 0.5h under the protection of nitrogen, and then add The formamide solution of HA, the molar ratio of ASA to HA is 1:2, and the esterification reaction is carried out at 45°C for 48h under the protection of nitrogen;

[0049](2) Dialyzing the material obtained in step (1) to obtain HA-ASA dialyzate;

[0050] (3) After the HA-ASA dialysate obtained in step (2) is vacuum freeze-dried, the corresponding HA-ASA raw material is obtained;

[0051] (4) Dissolving the HA-ASA raw material obtained in step (3) in dimethyl sulfoxide to obtain an organic solution of HA-ASA, and ultrasonically dispersing at room temperature for 0.5 h;

[0052] (5) The organic solution of HA-ASA obtained in step (4) was slowly added to 9 times the volume of deionized water, placed on a shaking table at room temperature for 3 hours, and t...

Embodiment 2

[0056] (1) Dissolve ASA in dimethyl sulfoxide, add the activator EDC·HCl according to the molar ratio of ASA and activator at a ratio of 1:2, carry out carboxyl activation at 50°C for 1 h under nitrogen protection, and then add HA formamide solution, the molar ratio of ASA to HA is 1:2, and the esterification reaction is carried out at 50°C for 36h under the protection of nitrogen;

[0057] (2) Dialyzing the material obtained in step (1) to obtain HA-ASA dialyzate;

[0058] (3) After the HA-ASA dialysate obtained in step (2) is vacuum freeze-dried, the corresponding HA-ASA raw material is obtained;

[0059] (4) dissolving the HA-ASA raw material obtained in step (3) in dimethyl sulfoxide to obtain an organic solution of HA-ASA; ultrasonically disperse at room temperature for 1 h;

[0060] (5) Slowly add the organic solution of HA-ASA obtained in step (4) to 9 times the volume of deionized water, place it on a shaker at room temperature for 1 hour, and then dissolve the HA-ASA...

Embodiment 3

[0064] (1) Dissolve ASA in dimethyl sulfoxide, add the activator EDC·HCI according to the molar ratio of ASA and activator as 1:2, carry out carboxyl activation at 45°C for 2 hours under the protection of nitrogen, and then add HA formamide solution, the molar ratio of ASA to HA is 1:2, and the esterification reaction is carried out at 45°C for 36h under the protection of nitrogen;

[0065] (2) dialyze the material obtained in step (1) to obtain HA-ASA dialysate;

[0066] (3) After the HA-ASA dialysate obtained in step (2) is vacuum freeze-dried, the corresponding HA-ASA raw material is obtained;

[0067] (4) Dissolving the HA-ASA raw material obtained in step (3) in N,N-dimethylformamide to obtain an organic solution of HA-ASA; ultrasonically disperse at room temperature for 0.5h;

[0068] (5) Slowly add the organic solution of HA-ASA obtained in step (4) to 9 times the volume of deionized water, place it on a shaker at room temperature for 3 hours, and then perform dialysis...

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Abstract

The invention discloses hyaluronic acid artesunate, a nano-micelle preparation of hyaluronic acid artesunate, and a preparation method and use of the nano-micelle preparation. The active ingredient hyaluronic acid artesunate consists of artesunate and hyaluronic acid, wherein artesunate serves as a main active ingredient, hyaluronic acid serves as a carrier and a targeting molecule and is connected with artesunate through a chemical bond to form hyaluronic acid artesunate, and then self-assembly is performed to form a nano-micelle and freeze-drying is performed to obtain the nano-micelle preparation. A particle size of the hyaluronic acid artesunate nano-micelle is 100-200 nm, the freeze-dried preparation is good in stability, and has a relatively good acidity responsive release characteristic after being injected into a body, and cytotoxicity tests prove that compared with the artesunate pure medicine, the nano-micelle preparation has stronger tumor cytotoxicity effects. The nano-micelle preparation has the characteristics of strong targeting property, long circulation and low toxicity.

Description

technical field [0001] The invention belongs to the technical field of antitumor drugs, and in particular relates to a nano-micelle preparation and its preparation method and application. Background technique [0002] Artesunate (Artesunate, abbreviated as ASA), Mr 384.42, the chemical name is dihydroartemisinin-l,2-α-succinic acid monoester, is a new antimalarial drug artemisinin with sesquiterpene lactones One of the important derivatives. As a new antimalarial drug with a new structure, ASA has the characteristics of high efficiency, quick action, low toxicity, and is not easy to produce tolerance; it has good solubility, flexible dosage form, and convenient administration, so it is widely used in clinical practice. Since it was successfully developed in 1980, many scholars have conducted in-depth research on the pharmacological effects of ASA, and found that ASA not only has antimalarial effects, but also has immune regulation, anti-tumor, liver protection, anti-inflamm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/357A61K47/10A61K47/26A61K47/61A61P35/00B82Y5/00
CPCA61K9/1075A61K9/19A61K31/357A61K47/10A61K47/26A61K47/61A61P35/00B82Y5/00
Inventor 侯振清陈诗端范仲雄王衍戈邢驰坤
Owner XIAMEN UNIV
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