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Photosensitizer particles for medical imaging and/or photodynamic therapy

A light-sensing and particle-based technology, applied in the fields of light-sensing particle developer and photodynamic therapy agent, medical imaging and/or photodynamic therapy, manufacturing or using these agents, can solve the problem of damaging photodynamic therapy to kill malignant cells, Hypoxia, lack of oxygen and other problems

Inactive Publication Date: 2016-02-03
薛富盛
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in solid tumors, the growth rate of tumor cells tends to be faster than angiogenesis, resulting in a hypoxic environment, where tumor cells are often exposed to oxygen deprivation
Photodynamic therapy's ability to kill malignant cells is compromised when tumor cells are hypoxic

Method used

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  • Photosensitizer particles for medical imaging and/or photodynamic therapy
  • Photosensitizer particles for medical imaging and/or photodynamic therapy
  • Photosensitizer particles for medical imaging and/or photodynamic therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Preparation and properties of PPLA, CPLA and CPCL conjugates

Embodiment 11

[0108] Example 1.1: PPLA

[0109] The preparative steps were performed entirely under dry nitrogen. Solvents and reagents were dried with sodium / benzophenone (for hexane, toluene, and THF) or anhydrous magnesium sulfate (for benzyl alcohol) at reflux for at least 24 hours. Recrystallize L-lactide (L-Lactide) from toluene solution for later use.

[0110] The preparation process of the catalyst used in the ring-opening polymerization (ROP) of the PPLA conjugate is as follows. N,N-dimethylethylenediamine (N,N-dimethylthane-1,2-diamine; 8.8 g, 100 mmol), 2-hydroxybenzaldehyde (12.2 g, 100 mmol) and aqueous hydrogen chloride (35%, 0.30 mL) the mixture was added to anhydrous THF (30 mL) and stirring was continued for 1 day. The volatiles were removed under vacuum to give 2-[(2-dimethylamino-ethylimino)methyl]phenol (2-[(2-dimethylamino-ethylimino)methyl]phenol; abbreviated DAIP-H; yellow Oil; Yield: 18.2 g; Yield: 95%). In a sealed tube, DAIP-H (1.92 g, 10 mmol) and Ca(OMe) 2 ...

Embodiment 12

[0115] Example 1.2: CPLA

[0116] In this example, the 4-arm chlorin-polylactic acid was synthesized from m-tetra-3-hydroxymethylphenylchlorin (meta-tetra-3-hydroxymethylphenylchlorin, m-THMPC) (CPLA) adapter.

[0117] The synthesis method of m-THMPC is as follows. First, NaBH was added to the 4 (0.425 g, 9.25 mmol) was added to a solution of dialdehyde (5 g, 37 mmol) dissolved in a mixture of absolute alcohol (75 mL) and THF (100 mL). The mixture was then kept stirring for 10 hours with the temperature maintained between about 0 and -5°C. Before the solvent was evaporated, 2M HCl was added for neutralization and the pH of the reaction mixture was adjusted to pH5. Then, water (200 mL) was added to the residue, followed by extraction with ethyl acetate. Combine the organic extracts with MgSO 4 Drying followed by evaporation of the solvent. The product was purified by column chromatography in ethyl acetate-hexane (30 / 70) to give Hydroxymethylaldehyde as a colorless liquid...

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Abstract

Photosensitizer particle contrast agents are suitable for medical imaging and / or photodynamic therapy. The photosensitizer particle contrast agent has a shell and a core encased by the shell. The shell consists essentially of multiple photosensitizer conjugates. Each photosensitizer conjugate consists of a photosensitizer and at least one biodegradable polymer covalently bound to the photosensitizer. The core has an echogenic contrast-enhancing material loaded therein. The photosensitizer of at least one of the multiple photosensitizer conjugates has a magnetic contrast-enhancing agent, e.g., a paramagnetic ion, chelated thereto. Methods for medical imaging use imaging compositions containing the photosensitizer particle contrast agents.

Description

technical field [0001] The present invention relates to a photosensitive particle used in medical imaging and / or photodynamic therapy (PDT for short). In particular, the present invention relates to photosensitive particle imaging agents and photodynamic therapy agents (PDTagents), and methods of making or using these agents. Background technique [0002] Generally, medical imaging techniques are used to generate images of animal (including human) body parts for purposes of diagnosis, treatment and / or scientific research. [0003] Diagnostic or medical ultrasound (diagnosticormedicalsonography), also known as ultrasound examination (ultrasonography), is an imaging technique based on ultrasound to visualize the subcutaneous tissue / organ of an individual. The concept of ultrasound examination is different from other medical imaging methods. Its operating principle is realized through the sending and receiving of sound waves. High-frequency, broad-spectrum sound waves are sen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/30A61K49/12
CPCA61K41/0071A61K47/593A61K47/6935A61K47/6937A61P35/00A61N5/062A61N2005/0662
Inventor 赖秉杉徐嘉延
Owner 薛富盛
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