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Fucoidan-based theragnostic Composition

A technology for fucoidan and conjugates, which is applied in the field of preparation of diagnostic and therapeutic agent compositions, can solve the problems of inability to obtain photodynamic therapy effects, increased steps and costs, and difficulty in mass production of conjugates, and achieves inhibition of smooth muscle cells. proliferative effect

Inactive Publication Date: 2020-05-26
NAT CANCER CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although this hydrophilic polymer-photosensitizer and conjugate are helpful for improving the hydrophilicity of the photosensitizer, they do not have specific targeting to cancer cells or cells related to other diseases. Therefore, in order to Targeting cells is specific and must bind target ligands such as folic acid or antibodies or aptamers to the polymer in one step
In this case, the steps and costs required for the preparation increase, and the mass production of the conjugate is difficult
Moreover, although the hydrophilic polymer accounts for more than 70% of the mass in the hydrophilic polymer and photosensitizer conjugate, the therapeutic effect is only obtained by means of the photosensitizer, and the hydrophilic polymer itself has no treatment for cancer cells, etc. effect, thus having the great disadvantage that not only is the therapeutic effect achievable in relation to the mass low, but also that the photodynamic therapy effect cannot be obtained in the absence of light reaching the site of delivery of the polymer-photosensitizer conjugate
[0006] In addition, attempts have been made to use conjugates of fluorescent dyes that bind ligands that can target specific cells and hydrophilic polymers (i.e., ligand-fluorescent dye-hydrophilic polymer conjugates) to treat cancer and other lesions. Imaging diagnosis, in this case, only the imaging diagnosis function of the target site can be obtained, and in order to obtain the therapeutic effect, it is necessary to go through a complicated process of further binding or loading the drug on the polymer

Method used

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  • Fucoidan-based theragnostic Composition
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  • Fucoidan-based theragnostic Composition

Examples

Experimental program
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Effect test

Embodiment 1

[0091] [Example 1] Preparation of Flamma774-fucoidan conjugate

[0092] The amine group of Flamma774, which is a near-infrared fluorescent dye of Bioacts, and the carboxyl group of fucoidan, are used to synthesize a covalent conjugate using a coupling agent. Flamma774-amine is a fluorescent substance with a substance mass of 971.15g / mol, a maximum excitation wavelength of 774nm, and a maximum release wavelength of 806nm. The near-infrared fluorescent dye conjugate has high permeability to biological tissues, so it can be used for biological imaging in drug delivery and tumor research. The fucoidan was produced by Sigma-Aldrich with a molecular weight of 18,000 Da extracted from Fucus.

[0093] Various coupling agents can be used to bind fluorescent dyes to fucoidan, where N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC) and N- Hydroxythiosuccinimide (thio-NHS) activates the dye to obtain a fucoidan-NHS ester conjugate, which is combined with Flaamma774-amine. T...

Embodiment 2

[0095] [Example 2] Preparation of ATTO 655-fucoidan conjugate

[0096] A coupling agent is used to form a covalent conjugate between the amine group of ATTO 655 as a fluorescent dye and the carboxyl group of fucoidan. ATTO 655-amine is a fluorescent substance with a substance mass of 798g / mol, a maximum excitation wavelength of 1663nm, and a maximum release wavelength of 680nm. The fucoidan was produced by Sigma-Aldrich with a molecular weight of 18,000 Da extracted from Fucus.

[0097] Use N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysulfosuccinimide (thio-NHS) to activate fucoidan to obtain Fucoidan-NHS ester conjugate, combined with ATTO 655-amine. To explain the process in more detail, dissolve 10 mg of fucoidan in 0.1M 2-(N-morpholine)ethanesulfonic acid (MES) buffer, add 19.7 mg of EDC, 2.17 mg of thio-NHS, and stir for approximately 30 minutes. Then, after separation using a PD-10 column, 0.399 mg of ATTO655-amine fluorescence was added...

Embodiment 3

[0099] [Example 3] Preparation of ZW800-fucoidan conjugate

[0100] The amine group of the near-infrared fluorescent dye ZW800 developed by the research group of Professor Cui Xuezhu of Harvard University and the carboxyl group of fucoidan form a covalent conjugate using a coupling agent. ZW800-amine is a near-infrared fluorescent substance with a substance mass of 887g / mol, a maximum excitation wavelength of 753nm, and a maximum emission wavelength of 772nm. The fucoidan was produced by Sigma-Aldrich with a molecular weight of 18,000 Da extracted from Fucus.

[0101] Use N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysulfosuccinimide (thio-NHS) to activate fucoidan to obtain Fucoidan-NHS ester conjugate, combined with ZW800-amine. The reaction ratios of fucoidan and ZW800 fluorescent dye are 1:2 and 1:4, respectively. If the process is described in more detail, 20mg fucoidan is dissolved in 0.1M 2-(N-morpholine)ethanesulfonic acid (MES) buffer, ...

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Abstract

The present invention relates to a fucoidan-based theragnostic composition, and more particularly, to preparation and use of a theragnostic composition which uses a conjugate of a fluorescent dye or aphotosensitizer and fucoidan, thereby not only allowing for fluorescence imaging diagnosis of lesions for cancer or vascular diseases but also allowing a therapeutic effect thereon to be obtained atthe same time. The conjugate obtained by covalent bonding of a fluorescent dye or a photosensitizer and fucoidan, according to the present invention, is not only useful for fluorescence imaging diagnosis of tumor tissues and ophthalmic vascular diseases, but also may exhibit a therapeutic effect on cancer cells and coronary artery smooth muscle cells, and a neovascularization inhibitory effect inophthalmic diseases. In addition, in a case where photodynamic therapy is further implemented on the conjugate according to the present invention, cancer and vascular diseases may be effectively treated with low adverse effects.

Description

Technical field [0001] The present invention relates to a fucoidan-based diagnostic and therapeutic agent (theragnostic) composition, more specifically, the present invention relates to the preparation and use of a diagnostic and therapeutic agent composition, by using a fluorescent dye or a photosensitizer and fucoidan to covalently The combined conjugate not only enables fluorescent imaging diagnosis of cancer or vascular disease lesions, but also obtains therapeutic effects at the same time. Background technique [0002] Diagnosis and treatment are the two main categories in the clinical application of diseases. Recently, the concept of diagnosis and treatment has been introduced that uses the imaging function of therapeutic agents to simultaneously diagnose and treat. [0003] The photosensitizer used in photodynamic therapy (PDT) has the characteristics of absorbing light of a specific wavelength and generating a fluorescent signal. It has the advantage of using it for the flu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K49/00A61K47/61A61P35/00A61P9/10A61P27/06
CPCA61K41/0057A61K41/0071A61K49/0054A61K47/61A61P35/00A61P9/10A61P27/06A61K49/0028A61K49/0032A61P27/02A61K2123/00A61K2121/00A61K47/549
Inventor 崔容斗赵美显李妍
Owner NAT CANCER CENT
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