Conjugate for photodynamic diagnosis or therapy and method for preparing same

一种光动力学诊断、轭合物的技术，应用在化学仪器和方法、体内试验用的配制品、硅化合物有效成分等方向，能够解决光敏剂难累积、光敏剂浓度降低、治疗长等问题

Inactive Publication Date: 2013-08-21
帕纳斯伊泰(株) +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, PDT is difficult to apply to bulky tumor cells that cannot pass light
The disadvantage of PDT is that the metabolism of the photosensitizer in the body is very slow, and therefore it is retained in the body for a long time, resulting in phototoxic side effects, and it hardly accumulates in tumor cells, resulting in a decrease in the concentration of the photosensitizer in the tumor cells, which cannot achieve sufficient treatment Effect
[0007] In addition, photosensitizers have a long half-life, which makes it inconvenient for patients to stay in a dark environment after treatment, and photosensitizers are difficult to accumulate in tumor cells
In addition, therapeutic compounds accumulate in the body for a long time (including treatment time), which leads to various side effects in the body
In addition, most photosensitizers used in PDT are hydrophilic products and do not penetrate the skin easily, requiring multiple treatments over a long period of time, which makes the treatment too long

Method used

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  • Conjugate for photodynamic diagnosis or therapy and method for preparing same
  • Conjugate for photodynamic diagnosis or therapy and method for preparing same
  • Conjugate for photodynamic diagnosis or therapy and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Preparation of nano-microspheres for photodynamic diagnosis or treatment

[0102] Preparation of phthalocyanine-based compounds

[0103] Synthesis of precursor R1

[0104] Add 4-methoxy-3,6-tert-butylphenol 3.66g (15.6mmol) and 4-nitrophthalonitrile 2.70g (15.6mmol) in the DMSO of 100ml and use N 2 Purge, then increase temperature to reflux. From start to reflux for 4 hours, to which K was added 2 CO 3 2.86g, which was then kept for 24 hours.

[0105] After refluxing for 24 hours, 100 ml of water was added thereto, followed by stirring, and then K was removed 2 CO 3 and DMSO to precipitate a slightly viscous white substance. Sufficient ether was added thereto to extract only the product, which was then dried by an evaporator to obtain pale yellow product 1-1-1.

[0106] Synthesis of COOH precursor R2

[0107] Add 2.405 g (12.37 mmol) of pentyl-4-hydroxybenzoate and 2 g (11.56 mmol) of 4-nitrophthalonitrile to 82.5 ml of anhydrous DMSO and wash with N 2 Purg...

Embodiment 2

[0120] characteristic analysis of nano microspheres

[0121] Measurement of the size and shape of nanospheres

[0122] Three samples of biocompatible substances prepared in Example 1 (in which a phthalocyanine-based compound was bound to acetylated chondroitin sulfate) were dissolved at a concentration of 1 mg / ml, and then measured by using dynamic light scattering (DLS). The size and shape were confirmed by using field emission scanning electron microscopy (FE-SEM). Here, samples were diluted with 0.1M NaCl for accurate size measurement. The results are shown in Figures 7 to 11 . Such as Figures 9 to 11 As shown, the size and shape of nanospheres formed by combining a phthalocyanine-based compound with chondroitin sulfate as a biocompatible polysaccharide via an ester bond are distributed in the range of 100 to 800 nm and centered at about 230 nm. Furthermore, in 3A, the large particles represent the case of a small amount of photosensitizer (Ac-Cs-Zn-PC-COOH1), and ...

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Abstract

The present invention relates to a conjugate of acetylated biocompatible polysaccharide and phthalocyanine compound for photodynamic diagnosis or therapy and to a method for preparing the same, and more particularly, to a conjugate for photodynamic diagnosis or therapy and to a method for preparing the same, in which biocompatible polysaccharide is acetylated and a phthalocyanine compound is bound to the acetylated polysaccharide. The conjugate for photodynamic diagnosis or therapy according to the present invention is characterized in that the polysaccharide is acetylated to improve solubility in a solvent and thus enable various chemical modifications, and the conjugate may specifically target tumor cells, has superior cancer cell selecting and accumulating capacity, and has excellent effects of killing cancer cells when near infrared ray is irradiated.; The conjugate of the present invention may not show cytotoxicity for cells other than cancer cells even when near infrared ray is irradiated, and thus exhibits superior in vivo stability, and therefore, may be valuably used in disease diagnosis or therapy using photodynamics.

Description

technical field [0001] The present invention relates to conjugates of acetylated biocompatible polysaccharides and phthalocyanine-based compounds for use in photodynamic diagnosis or therapy and methods for their preparation, and more particularly to biocompatible conjugates in which the acetylated Polysaccharides combined with phthalocyanine-based compounds are capable of having excellent accumulation ratio and target ratio against cancer cells and exhibiting excellent stability in cells other than cancer cells, and a preparation method thereof. Background technique [0002] Photodynamic therapy (PDT) is a technique for treating untreatable diseases such as cancer or treating diseases such as acne by using a light-sensitive substance (hereinafter referred to as "photosensitizer") without surgery. Since the early 21st century, PDT has been actively studied and is currently being used to increase immunity in cancer diagnosis and treatment, autologous bone marrow transplantati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/695A61K31/315A61K49/06A61K49/10A61K49/12A61K31/702C09B47/04
CPCA61K41/0071A61K49/0036A61K49/0054A61P35/00A61P43/00A61K31/555A61K41/0076A61K47/61
Inventor 罗建李方园裴秉灿
Owner 帕纳斯伊泰(株)
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