Supermolecular nanoparticle for targeting delivery of camptothecin and preparation method thereof

A nanoparticle, targeted delivery technology, applied in the directions of non-active components of medical preparations, non-active components of polymer compounds, medical preparations containing active components, etc. The effect of reducing toxic and side effects, simple preparation process and great application prospects

Inactive Publication Date: 2016-12-21
NANKAI UNIV
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  • Abstract
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  • Application Information

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Problems solved by technology

In addition, camptothecin and its derivatives will be hydrolyzed and deactivated under alkaline aqueous conditions, which is also a headache for medical workers.

Method used

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  • Supermolecular nanoparticle for targeting delivery of camptothecin and preparation method thereof
  • Supermolecular nanoparticle for targeting delivery of camptothecin and preparation method thereof
  • Supermolecular nanoparticle for targeting delivery of camptothecin and preparation method thereof

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Embodiment

[0022] A supramolecular nanoparticle for targeted delivery of camptothecin is a binary supramolecular assembly synthesized based on cyclodextrin-modified camptothecin and adamantane-modified hyaluronic acid, wherein the molecular formula of adamantane-modified hyaluronic acid is (C 14 h 21 NO 11 ) 239 (C 27 h 41 N 3 o 11 ) 36 , an average of 36 adamantane units are modified on one polymer chain, and the chemical formula of cyclodextrin-modified camptothecin is C 73 h 101 N 5 o 39 ; The binary supramolecular assembly is based on the strong non-covalent interaction between cyclodextrin and adamantane and the amphiphilic interaction between molecules, forming a hydrophilic hyaluronic acid as the shell and a hydrophobic camptothecin as the core. Supramolecular nanoparticles, the size of nanoparticles is 70-90nm.

[0023] The preparation method of the targeted delivery camptothecin supramolecular nanoparticles, the steps are as follows:

[0024] 1) Dissolve 500 mg (4.5 ...

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Abstract

Supermolecular nanoparticle for targeting delivery of camptothecin is a binary supermolecular assembly synthesized on the basis of cyclodextrin modified camptothecin and adamantane modified hyaluronic acid. According to the binary supermolecular assembly, through non-covalent interaction and intermolecular amphiphilic action between cyclodextrin and adamantine, supermolecular nanoparticles with hydrophilic hyaluronic acid as the shell and hydrophobic camptothecin as the core are formed, and the particle size of the nanoparticles is 70-90 nm. The invention has the following advantages: the supermolecular nanoparticle has simple synthesis route, low production cost and high yield, and is suitable for amplified synthesis and practical production; by endocytosis of the hyaluronic acid receptor over-expressed on the surface of malignant cells and used as a medium, supermolecular nanoparticles HACPTPs are targeted into the cancer cells to realize protection of normal cells and targeted selective killing of cancer cells; antitumor activity is remarkable; and toxic and side effect is obviously reduced.

Description

technical field [0001] The invention relates to the technical field of targeted delivery of anticancer drugs, in particular to supramolecular nanoparticles for targeted delivery of camptothecin and a preparation method thereof. Background technique [0002] In today's society, due to environmental pollution, food safety issues, and unhealthy lifestyles and other factors, the incidence of cancer is increasing year by year, and the imperfect treatment methods make the mortality rate of cancer remain high. Although emerging treatment methods such as immunotherapy and gene therapy have been developed by scientists in recent years, and some have entered clinical trials, there is still a long way to go for these methods to be put into practical application. Traditional treatments are limited to surgery, radiation and chemotherapy. Among them, chemotherapy is the most commonly used tumor suppression method after surgery, but its strong toxic and side effects bring great pain to pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4745A61K47/36A61K47/40A61P35/00
CPCA61K9/5036A61K31/4745A61K47/40
Inventor 刘育杨洋张瀛溟王丽华
Owner NANKAI UNIV
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