Porphyrin dimer salt complex loaded with targeting polypeptide-modified ferritin nanoparticles and use and preparation method thereof

A technology of porphyrin dimer salt and porphyrin dimer is applied in the field of medicine, which can solve the problems of low ferritin drug loading rate, tumor targeting to be improved, and increase ferritin transfer rate, etc., and achieve significant tumor cells. Killing effect, increasing tumor targeting, and efficient tumor treatment

Active Publication Date: 2016-03-16
上海光声制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application was found to be limited by the low drug loading of ferritin and the need for improved tumor targeting
Increasing the transfer rate of ferritin is a great challenge in the field

Method used

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  • Porphyrin dimer salt complex loaded with targeting polypeptide-modified ferritin nanoparticles and use and preparation method thereof
  • Porphyrin dimer salt complex loaded with targeting polypeptide-modified ferritin nanoparticles and use and preparation method thereof
  • Porphyrin dimer salt complex loaded with targeting polypeptide-modified ferritin nanoparticles and use and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] In embodiment 1, the present invention provides an R-Fn-porphyrin dimer salt complex, wherein:

[0079] Fn is ferritin;

[0080] R is a targeting polypeptide, preferably arginine-glycine-aspartic acid,

[0081] R-Fn refers to arginine-glycine-aspartic acid modified ferritin nanoparticles, wherein R:Fn=1-24 (preferably 24);

[0082] R-Fn-DVDMS is a complex formed by R-Fn and porphyrin dimer salt, and the porphyrin dimer salt is wrapped in the inner cavity of R-Fn: and

[0083] The porphyrin dimer salt is a compound of formula (1), (2) or (3),

[0084]

[0085] in

[0086] R is independently selected from C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 1-6 Alkoxy and C 1-6 Acyl (optionally one of them), which is optionally substituted by one or more substituents selected from halogen and hydroxyl,

[0087] M is an alkali metal, alkaline earth metal or NH 4 + ,

[0088] p is the reciprocal of the valence number of M.

[0089] In the present invention, the targ...

Embodiment 2

[0092] This example is a preferred version of Example 1, providing the R-Fn-porphyrin dimer salt complex as described in Example 1, wherein R is independently selected from C optionally substituted by one or more hydroxyl groups 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl and C 1-6 Acyl, M is alkali metal or NH 4 + , and p is 1.

Embodiment 3

[0094] This embodiment is a preferred version of Example 2, which provides the R-Fn-porphyrin dimer salt complex as described in Example 2, wherein R is independently selected from -CH=CH 2 , -CH(OH)CH 3 and-COCH 3 , M is an alkali metal or NH 4 + , and p is 1.

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Abstract

The invention discloses a porphyrin dimer salt complex loaded with targeting polypeptide-modified ferritin nanoparticles and a use and a preparation method thereof; the complex has the structure of R-Fn-porphyrin dimer salt, wherein Fn is ferritin, and R is a targeting polypeptide; the ferritin is chemically modified by the targeting polypeptide, and the porphyrin dimer salt is wrapped by the targeting polypeptide-modified ferritin. The preparation method comprises the steps: adjusting the pH value of a PBS solution of R-Fn to 2-3 with HCl, then adding the porphyrin dimer salt, mixing and carrying out a reaction for 20-40 min, then adjusting the pH value of the mixed liquid to 7-8, continuing to stir for 1-3 h, filtering with a filter, and thus obtaining the R-Fn-porphyrin dimer salt complex. The invention provides the novel diagnosis and treatment integrated complex having good biological compatibility, having high targeting property on tumor and having combined treatment of PDT and PTT.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a photosensitizer complex, a preparation method thereof and an application thereof in drug production for photodynamic therapy (photodynamic therapy, PDT) and photothermal therapy (photothermal therapy, PTT). More specifically, the present invention relates to complexes of targeted polypeptide-modified ferritin nanoparticles and porphyrin dimer salts, methods for their preparation, pharmaceutical compositions containing them and their use in the preparation of fluorescent imaging and phototherapy Use in medicine. Background technique [0002] Phototherapy is a new type of treatment, which utilizes the photothermal or photodynamic effects of drugs, has special spatiotemporal selectivity and minimal invasiveness, and can perform fluorescence imaging and optical therapy at the same time. Phototherapy mainly includes photothermal therapy and photodynamic therapy. Photothermal therapy refers...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K49/00A61K47/48A61P35/00
CPCA61K41/0052A61K41/0071A61K49/0036
Inventor 刘刚黄超张绍良陈小元张君楚成超杨彩霞
Owner 上海光声制药有限公司
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