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Preparation method and application of chitosan oligosaccharide modified betulinic acid drug delivery system

A technology of betulinic acid and chitosan oligosaccharides, which can be used in drug delivery, drug combination, and pharmaceutical formulations. It can solve the problems of limited preparation and achieve excellent biocompatibility and biodegradability.

Active Publication Date: 2020-09-11
HARBIN INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its high water solubility also greatly limits its preparation as a nano-drug delivery system.

Method used

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  • Preparation method and application of chitosan oligosaccharide modified betulinic acid drug delivery system
  • Preparation method and application of chitosan oligosaccharide modified betulinic acid drug delivery system
  • Preparation method and application of chitosan oligosaccharide modified betulinic acid drug delivery system

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Synthesis of compound chitooligosaccharide-betulinic acid (COS-BA):

[0040] The synthesis of chitooligosaccharide-betulinic acid (COS-BA) is mainly prepared by a one-pot method under the catalysis of the condensation agent EDC / NHS. The specific synthesis method is explored as follows: 40mg betulinic acid BA, 20mg 1-(3 -Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), 21mg N-hydroxysuccinimide (NHS) were dissolved in organic reagent acetone (4mL), then 1mL chitooligosaccharide (COS, degree of polymerization 2-6, 96 mg) aqueous solution was slowly added dropwise to the above organic reagent, followed by stirring and reacting at room temperature under an ice bath for 24 h. Thin-layer chromatography detects the reaction situation; after the reaction, use petroleum ether: acetone=5:1 to remove unreacted betulinic acid and intermediate by-products, and use petroleum ether:acetone=3:1 to separate the point with the highest content COS-BA.

[0041]The synthesis ...

Embodiment 2

[0044] Construction of drug-loading system (i.e. preparation of COS-BANPs):

[0045] A certain amount of COS-BA was dissolved in DMSO to prepare a COS-BA mother solution with a concentration of 33.5 mM. 40 μl of DMSO sample was quickly added dropwise to 1 M double-distilled water under ultrasonic conditions, followed by ultrasonication for 10 min and centrifugation at 13500 rpm to obtain COS-BANPs.

Embodiment 3

[0047] Carrying chemotherapy drugs: Take the drug paclitaxel PTX as an example.

[0048] (1) COS-BA@PTX NPs were prepared by co-precipitation method.

[0049] First prepare PTX and COS-BA DMSO mother solution with a concentration of 20mM, take 50μL COS-BA solution and 10μL PTX solution, mix well, slowly drop the solution into 2mL water while stirring; continue stirring on a magnetic stirrer for 4h , transferred to a dialysis bag (MW=3000) for dialysis for 24 hours to remove organic reagents, and centrifuged at 13500rpm to obtain COS-BA@PTXNPs.

[0050] from image 3 It can be seen that when COS-BA is assembled with the chemotherapeutic drug PTX, the particle morphology also presents a spherical trend, but the particle diameter is smaller, with an average diameter of about 84nm, which further shows that the combination of PTX and COS-BA can change the shape of nanoparticles. size, PTX loaded successfully.

[0051] (2) Determination of PTX content in COS-BA@PTX NPs.

[0052]...

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Abstract

The invention discloses a preparation method and application of a chitosan oligosaccharide modified betulinic acid drug delivery system. Betulinic acid is modified on the basis of active chitosan oligosaccharide to prepare amphipathic active unit molecules, so that on one hand, the anticancer activity of the chitosan oligosaccharide and the betulinic acid can be combined, and the purpose of safelyand efficiently synergistically enhancing the anticancer effect is achieved; and on the other hand, by means of the amphipathy of the molecules, the purpose of drug delivery can be achieved in a micelle or self-assembly form. As the drug delivery system, on one hand, traditional chemotherapy drugs can be carried to achieve the purpose of multiple chemotherapy, and the anticancer curative effect is enhanced; and on the other hand, a photosensitizer can be carried, so that the purpose of triple synergistic enhancement of the anticancer curative effect is achieved by combining with phototherapyand the like on the basis of realizing safe chemotherapy, and clinical cancer treatment is expected to be overcome and solved.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and relates to a preparation method based on active chitosan oligosaccharide bridging natural small molecule nanocarriers and its synergistic anticancer application. Background technique [0002] At present, cancer is one of the malignant diseases that seriously threaten the safety of human life. Tumor treatment methods based on the combination of chemotherapy, phototherapy, hyperthermia, and immunotherapy have been widely explored and used in clinical cancer treatment. However, traditional chemotherapeutic drugs (such as paclitaxel, doxorubicin hydrochloride, etc.) have defects such as low bioavailability and high toxicity and side effects. Even the combined therapy based on this often has certain side effects. Therefore, it is of great significance to explore safe and efficient chemotherapy drugs and combine them with phototherapy or hyperthermia to achieve cancer cure. [0003] Chitosan o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/61A61K47/54A61K31/56A61K31/337A61K41/00A61P35/00
CPCA61K47/6907A61K47/61A61K47/549A61K31/56A61K31/337A61K41/0071A61P35/00A61K2300/00
Inventor 杨鑫程建军刘秀
Owner HARBIN INST OF TECH
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