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Supramolecule assembly of targeting-delivery anticancer adamplatin and preparation of supramolecule assembly

A technology of supramolecular assembly and targeted delivery, which is applied in the direction of antineoplastic drugs, drug combinations, heavy metal active ingredients, etc., can solve the problems of high toxicity and side effects, and achieve improved anticancer activity, simple preparation process, and reduced toxicity and side effects Effect

Inactive Publication Date: 2012-10-03
NANKAI UNIV
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Problems solved by technology

However, cisplatin has a lot of toxic and side effects, and has significant myelosuppression, renal toxicity and neurotoxicity, which has a great impact on the patient's physical condition and quality of life. Therefore, a new targeted drug delivery system is designed to improve anticancer drug treatment. Efficacy and reducing toxic and side effects have become the focus and challenge of chemists, biologists and medical workers

Method used

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  • Supramolecule assembly of targeting-delivery anticancer adamplatin and preparation of supramolecule assembly
  • Supramolecule assembly of targeting-delivery anticancer adamplatin and preparation of supramolecule assembly
  • Supramolecule assembly of targeting-delivery anticancer adamplatin and preparation of supramolecule assembly

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Embodiment

[0025] A preparation of a supramolecular assembly for targeted delivery of adamantane cisplatin prodrug, the steps are as follows:

[0026] 1) Dissolve 100mg (0.0022mmol) of sodium hyaluronate with a molecular weight of 46,000 in 30mL of phosphate buffer solution with a pH of 7.2 and a concentration of 1mmol, and then add 167.7mg (0.875mmol) of 1-ethyl-(3-dimethyl Aminopropyl) carbodiimide hydrochloride and 190mg (0.875mmol) N-hydroxysulfosuccinimide, stirred for 30 minutes to obtain a reaction solution;

[0027] 2) Dissolve 588.5mg (0.5mmol) of 6-deoxy-6-ethylenediamine-β-cyclodextrin in 5mL of phosphate buffer solution with a pH of 7.2, and then add it to the above reaction solution. Stir under low pressure for 24 hours, then put it into a dialysis bag with a cut-off range of 8000-14000 for continuous dialysis for 5 days, and freeze-dry the resulting solution to obtain cyclodextrin-modified hyaluronic acid (HACD).

[0028] Detection shows that the nuclear magnetic character...

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Abstract

The invention discloses a supramolecule assembly of targeting-delivery anticancer adamplatin. The supramolecule assembly is a binary supramolecule assembly which is synthesized on the basis of cyclodextrin-decorated hyaluronic acid and adamplatin. A preparation method of the supramolecule assembly is characterized in that the cyclodextrin-decorated hyaluronic acid and the adamplatin are respectively synthesized, and through the strong non-covalent interaction of cyclodextrin and adamantine and the amphiphilic action of molecules, a supermolecule nano particle which takes the hydrophilic hyaluronic acid as a shell and the adamplatin as a core is formed. The supramolecule assembly disclosed by the invention has the advantages that the supramolecule assembly of the targeting-delivery anticancer adamplatin has a simple synthetic route, is low in preparation cost and high in productivity, and is suitable for amplification synthesis and practical production application; and through endocytosis in which a malignant cell surface hyaluronic acid receptor serves as a medium, the supramolecule assembly (HAP) is brought in cancer cells in a target manner, so that the protection of normal cells and the targeting selective killing of cancer cells are realized, the anti-cancer activity is obviously improved, and toxic and side effects are obviously reduced.

Description

【Technical field】 [0001] The invention relates to the technical field of targeted delivery of anticancer drugs, in particular to a supramolecular assembly and its preparation for targeted delivery of adamantane-cisplatin prodrugs. 【Background technique】 [0002] Due to the impact of environmental pollution, chemical pollution, electromagnetic radiation, free radical toxins and human genetic factors in today's society, cancer has become one of the major diseases that threaten human health. In order to combat this disease, human beings have invented various treatment methods, mainly including surgical treatment, radiotherapy and chemotherapy, etc. Among them, cisplatin is a broad-spectrum anti-cancer chemotherapy drug widely used in clinical practice. It has the advantages of synergistic effect of multiple anticancer drugs and no cross-resistance. However, cisplatin has a lot of toxic and side effects, and has significant myelosuppression, renal toxicity and neurotoxicity, wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K33/24A61K31/282A61P35/00
Inventor 刘育杨洋张瀛溟
Owner NANKAI UNIV
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