Synthesis of beta-CD-LA (cyclodextrin-linoleic acid) molecules and application of aggregate formed by beta-CD-LA molecules as drug delivery system

A linoleic acid and molecular technology, applied in the field of medicine, can solve problems such as restricted use, non-specific distribution of adverse reactions, poor water solubility of drugs, etc.

Inactive Publication Date: 2019-01-04
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
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Problems solved by technology

Chemotherapy is the most effective way to treat various cancers. However, traditional chemotherapy drugs have poor water solubility, instability in the systemic circulation, non-specific distribution causing serious adverse reactions and multidrug resistance, which greatly limit their clinical application. usage of

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  • Synthesis of beta-CD-LA (cyclodextrin-linoleic acid) molecules and application of aggregate formed by beta-CD-LA molecules as drug delivery system
  • Synthesis of beta-CD-LA (cyclodextrin-linoleic acid) molecules and application of aggregate formed by beta-CD-LA molecules as drug delivery system
  • Synthesis of beta-CD-LA (cyclodextrin-linoleic acid) molecules and application of aggregate formed by beta-CD-LA molecules as drug delivery system

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Embodiment Construction

[0024] Specific embodiments of the present invention are given below to further describe the structure of the present invention, but it is not considered that the present invention is limited to the following embodiments.

[0025] The preparation method of β-CD-LA micelles of the present invention and the application as a drug carrier are realized through the following technical scheme:

[0026] (1) The synthetic method of β-CD-LA molecule of the present invention:

[0027] Accurately weigh a certain amount of linoleic acid and add it to a round bottom flask, then add 20mL THF to the flask, and ultrasonically dissolve the linoleic acid. Then, DCC and NHS were added and reacted at room temperature for 24h. After reaching the specified reaction time, accurately weigh a certain amount of β-CD-NH 2 (β-CD-NH 2 The molar ratio to linoleic acid is 1:2) into a round bottom flask, ultrasonically dissolved and stirred at room temperature for 24 hours. After the reaction, the reactio...

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Abstract

The invention relates to synthesis of beta-CD-LA (cyclodextrin-linoleic acid), preparation of a beta-CD-LA micelle and a beta-CD-LA-Dox nanodrug and biological evaluation methods in vitro and in vivo,and belongs to the field of medicines. The preparation method comprises the following steps: firstly, LA activates a carboxylic acid group into a reactive carboxylic acid group under the action of DCC and NHS, and then is subjected to reaction with cyclodextrin, and beta-CD-LA molecules are generated. The beta-CD-LA molecules are self-assembled in an aqueous solution, and the micelle can be formed. Lipophilic anticancer drug doxorubicin is loaded into the beta-CD-LA micelle with an organic solvent volatilization method, and the beta-CD-LA-Dox nanodrug is formed. The beta-CD-LA micelle formedby the beta-CD-LA molecules has good biocompatibility, water solubility and stability. The beta-CD-LA-Dox nanodrug has slow pH-responsive release property and is capable of inducing apoptosis in cancer cells. Besides, the beta-CD-LA-Dox nanodrug can induce tumor cell apoptosis in tumor tissue and has anti-tumor effect, thereby having good application prospect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a micelle with good biocompatibility, water solubility and stability, a drug-loaded micelle with good water solubility and stability, and a biological evaluation method in vivo and in vitro. Background technique [0002] Cancer is the most harmful disease among various diseases. In the future, cancer will become the main cause of human death worldwide. Chemotherapy is the most effective way to treat various cancers. However, traditional chemotherapy drugs have poor water solubility, instability in the systemic circulation, non-specific distribution causing serious adverse reactions and multidrug resistance, which greatly limit their clinical application. usage of. To solve this problem, a series of drug carriers have emerged, such as micelles, liposomes, dendrimers, inorganic nanoparticles, and gels. Drug carriers increase the water solubility, stability, safety and therapeu...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/12A61K47/40A61K31/704A61P35/00
CPCA61K47/12A61K47/40A61P35/00A61K9/1075A61K31/704
Inventor 闫苗苗魏光成蔡安然李静辛美秀
Owner BINZHOU MEDICAL COLLEGE
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