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Tumor targeted cordycepin nanometer capsules

A technology of nanocapsules and cordycepin, which can be used in antitumor drugs, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as clinical application limitations and inactivation.

Inactive Publication Date: 2019-09-17
南京广方生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cordycepin can interfere with the synthesis of RNA and DNA in gene cells and inhibit the division of abnormal cells such as cancer cells. Live, the use of ADA inhibitors plays an important role in the expression of its anti-tumor activity, but this also makes it subject to certain limitations in clinical application

Method used

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  • Tumor targeted cordycepin nanometer capsules
  • Tumor targeted cordycepin nanometer capsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Preparation of RGD-ApoAI: Weigh 50mg of ApoAI, dissolve it in 100ml of water, stir well to dissolve it. Weigh 60mg of glutaraldehyde, dissolve it in 10ml of water, drop it into the ApoAI solution under stirring, and react for 1h; dissolve 80mg of RGD in 10ml of water, add the above-mentioned ApoAI solution, stir and react for 1h, put it into a dialysis bag, and use pH 7.0 phosphoric acid The buffer solution was dialyzed for 24 hours, and then freeze-dried to make RGD-ApoAI for use.

Embodiment 2

[0020] Weigh 30mg of cordycepin and dissolve in 5ml of water to obtain liquid A. Dissolve 480mg of soybean lecithin, 60mg of cholesterol and 5mg of sodium cholate in 15ml of chloroform completely, stir and mix with liquid A, place in an eggplant-shaped bottle, and place in a water bath at 35°C In the process, remove the organic solvent by decompression and rotary concentration, and form a uniform film on the bottle wall, add 5ml of water to wash the film, put it in an ultrasonic breaker for 30 minutes, continue to reduce the pressure and rotary concentration to remove the organic solvent, and make nano-lipid capsules , stored at 4°C.

Embodiment 3

[0022] Weigh 10mg of lyophilized RGD-ApoA I, add it into 10ml nano-lipid capsules, oscillate and mix, ultrasonically oscillate to disperse, and let stand at low temperature for 12 hours to make tumor-targeting cordycepin nanocapsules.

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Abstract

The invention discloses tumor targeted cordycepin nanometer capsules and a preparation method thereof. The method comprises the following steps of firstly preparing RGD modified apolipoprotein A I(ApoAI), and then constructing nanometer capsules from the RGD modified apolipoprotein A I(ApoAI), phospholipid and cordycepin. RGD peptide is a specific ligand of an integrin alpha v beta 3, and the integrin alpha v beta 3 gene is subjected to zero expression or little expression in majority of normal organ systems and normal vascular endothelial cells, and is subjected to overexpression on the surfaces of various tumor cells and tumor regenerated blood vessel endothelial cells, so that after being subjected to RGD modification, the nanometer capsules have good targeting effects on tumors, the effective concentration of cordycepin in tumor positions can be increased, and the antitumor effects of the cordycepin can be reinforced.

Description

technical field [0001] The invention belongs to the technical field of targeted drugs, in particular to a method for preparing a tumor-targeted cordycepin nanocapsule, which can be used for the treatment of tumors. Background technique [0002] Cordycepin is a natural biologically active substance extracted from Cordyceps militaris, chemically named 3'-deoxyadenosine, which has various biological activities such as tumor inhibition, anti-plasmodium, anti-virus, and immune regulation. Cordycepin can interfere with the synthesis of RNA and DNA in gene cells and inhibit the division of abnormal cells such as cancer cells. Live, the use of ADA inhibitors plays an important role in the expression of its anti-tumor activity, but this also makes it subject to certain limitations in clinical application. [0003] Nano-lipid capsules have good cell affinity and drug sustained-release performance. Using nano-liposomes as the drug carrier of cordycepin, and through tumor-targeted modi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/7076A61K47/64A61P35/00
CPCA61K31/7076A61K47/64A61K47/6929A61P35/00
Inventor 郑珩张彦余永柱
Owner 南京广方生物科技有限公司
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