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Albumin nano-particle preparation of donor-receptor type fluorescent molecule containing aggregation-induced emission group in near infrared II region

A technology of aggregation-induced luminescence and albumin nanotechnology, which is applied in the direction of medical preparations containing active ingredients, preparations for in vivo tests, non-effective ingredients of polymer compounds, etc., and can solve the problem of organic small molecule fluorescent probes that have not been retrieved problems, achieve good light-to-heat conversion ability, achieve clear imaging, and improve water solubility

Active Publication Date: 2020-02-14
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the literature at home and abroad, there are no organic small molecule fluorescent probes with the functions of NIR-II region fluorescence imaging and photothermal therapy.

Method used

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  • Albumin nano-particle preparation of donor-receptor type fluorescent molecule containing aggregation-induced emission group in near infrared II region
  • Albumin nano-particle preparation of donor-receptor type fluorescent molecule containing aggregation-induced emission group in near infrared II region
  • Albumin nano-particle preparation of donor-receptor type fluorescent molecule containing aggregation-induced emission group in near infrared II region

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Compound 1 (BPBBT) is a donor-acceptor NIR-II fluorescent molecule with an AIE group,

[0050]

[0051] Dissolve human serum albumin in water and mix evenly so that the protein concentration is 1.5% (w / v), weigh 30g of 1.5% albumin aqueous solution (w / v) in a 50ml beaker, and accurately weigh 30.0mg of BPBBT Dissolve in an organic solvent (chloroform: absolute ethanol = 15: 85), prepare according to the drug mass: protein mass = 1: 15, the ratio of the organic solvent to the water in the protein aqueous solution is 1: 44, stir at high speed, and prepare crude milk , to obtain a white emulsion; the white emulsion is homogenized under a pressure of 20000psi, so that the particle size is controlled at 50-200nm; after the organic solvent in the obtained BPBBT albumin nanoparticle solution is removed by a rotary evaporator, a 0.22 μm sterile Membrane filtration, freeze-drying, obtain the lyophilized powder of BPBBT nanoparticle, the particle size of nano-preparation, poly...

Embodiment 2

[0059] Compound 2 (BTPBBT) is a donor-acceptor NIR-II fluorescent molecule with an AIE group,

[0060]

[0061] Dissolve human serum albumin in water, and mix evenly to make the protein concentration 0.5% (w / v), weigh 30g of 0.5% albumin aqueous solution (w / v) in a 50ml beaker. Accurately weigh 30.0mg of BTPBBT and dissolve it in an organic solvent (dichloromethane: absolute ethanol = 15: 85), according to the drug quality: protein quality = 1: 15, the ratio of organic solvent to water in the protein aqueous solution is 1: 30 Ratio preparation, high-speed stirring, preparation of coarse milk, to obtain a white emulsion; the white emulsion is homogenized under a pressure of 20000psi, so that the particle size is controlled at 50-200nm; the obtained BTPBBT albumin nanoparticles (BTPBBT nanoparticles ) After removing the organic solvent in the solution, filter it with a sterile filter membrane of 0.22 μm, freeze-dry to obtain the freeze-dried powder of albumin nanoparticles of...

Embodiment 3

[0068] Compound 3 (TPABBT) is a donor-acceptor NIR-II fluorescent molecule with AIE group.

[0069]

[0070]Dissolve human serum albumin in water and mix evenly so that the protein concentration is 3.5% (w / v), weigh 30g of 3.5% albumin aqueous solution (w / v) in a 50ml beaker, and accurately weigh 30.0mg of TPABBT Dissolve in an organic solvent (chloroform: anhydrous methanol = 20: 80), prepare according to the ratio of drug quality: protein quality = 1: 30, and the ratio of organic solvent to water in the protein aqueous solution is 1: 88, stir at high speed, and prepare thick milk to obtain a white emulsion; the white emulsion is homogenized under 20000psi pressure, so that the particle size is controlled at 50-200nm; after the organic solvent in the obtained TPABBT albumin nanoparticles (TPABBT nanoparticles) solution is removed by a rotary evaporator , filtered with a sterile filter membrane of 0.22 μm, and freeze-dried to obtain the freeze-dried powder of albumin nanopa...

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Abstract

The invention belongs to the field of pharmaceutical preparation, and relates to an albumin nano-particle preparation of a donor-receptor type fluorescent molecule containing an aggregation-induced emission group in a near infrared II region. By adopting an emulsifying high-pressure homogenization method, bovine serum albumin, human serum albumin or recombinant human serum albumin and the donor-receptor type fluorescent molecule containing the aggregation-induced emission group are processed so that nano-particles are prepared; albumin is bonded with the fluorescent molecule , so that rotation in the molecule is limited, molecular conformation is changed, and twisted intramolecularcharge transfer and aggregation-induced emission effect are changed, so that the nano-particle preparation having good fluorescence imaging and photothermal conversion is obtained. The nano-particle preparation can emit fluorescence in the near infrared II region under irradiation of infrared light, and a part of light energy is transformed into heat energy, and an image-guided photothermal therapy for cancers is realized. The albumin nano-particle preparation can be used for preparing a medicine for conducting fluorescence imaging and photothermal therapy in the near infrared II region (NIR-II, 1000nm to 1700nm), and the aim of integration of diagnosis and treatment is fulfilled.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an albumin nano-preparation of a donor-acceptor fluorescent molecule in the near-infrared II region containing an aggregation-inducing luminescent group and a preparation method thereof. Background technique [0002] The prior art discloses that malignant tumors are the number one killer threatening human health, therefore, effective diagnosis and treatment of tumors is particularly important. At present, near-infrared II region (NIR-II, 1000-1700nm) fluorescence imaging technology has gradually developed into an efficient tumor diagnosis method. Compared with near-infrared I region (NIR-I, 700-950nm) fluorescence imaging Its longer wavelength, extremely low background autofluorescence and tissue scattering interference, deeper tissue penetration, and higher spatial resolution and contrast have attracted more and more attention from scholars, doctors and pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00A61K41/00A61K9/51A61K47/42A61P35/00
CPCA61K49/0093A61K49/0056A61K41/0052A61K49/0021A61K9/5169A61P35/00
Inventor 高帅魏国光章思航陆伟
Owner FUDAN UNIV
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