Solubilizing BODIPY photosensitizer and preparation method and application thereof in preparing medicine for treating body surface diseases

A photosensitizer and body surface technology, which is applied in the field of medicine and medical treatment, can solve the problems of complex synthesis methods, high cost, and toxicity, and achieve the effects of high extinction coefficient, low production cost, and good dispersibility

Active Publication Date: 2019-11-05
景遐斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] The purpose of the present invention is to solve the existing water-soluble BODIPY photosensitizer complex, costly and toxic problems, and to provide a solubilized BODIPY photosensitizer, preparation method and application in the preparation of medicines for treating body surface diseases

Method used

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  • Solubilizing BODIPY photosensitizer and preparation method and application thereof in preparing medicine for treating body surface diseases
  • Solubilizing BODIPY photosensitizer and preparation method and application thereof in preparing medicine for treating body surface diseases
  • Solubilizing BODIPY photosensitizer and preparation method and application thereof in preparing medicine for treating body surface diseases

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preparation example Construction

[0061] The present invention also provides a preparation method of a solubilized BODIPY photosensitizer, the method comprising: dissolving fat-soluble BODIPY powder or aza-BODIPY powder in an organic solvent, wherein the organic solvent is preferably acetone or ethanol to obtain an organic solution , the concentration of the organic solution is preferably 0.5-5mg / ml, then the organic solution is quickly added dropwise to the ultrapure water in stirring, the fast is preferably 30-60 drops / min, and the ultrapure The volume ratio of water and organic solution is preferably 10-100:1. Use a stirrer or a rotary evaporator to stir or evaporate at room temperature, evaporate the organic solvent to obtain a solubilized BODIPY or aza-BODIPY aqueous solution, and finally add ultra-pure Water adjusts the final concentration of the photosensitizer, and the final concentration of the solubilized BODIPY photosensitizer is preferably 10-500 μg / ml.

[0062] According to the present invention, ...

Embodiment 1

[0072] Preparation of embodiment 1 solubilizing compound (formula 1-formula 18)

[0073] Weigh 1.0 mg of the BODIPY compound (Formula 1-Formula 18) in Table 2, dissolve it in acetone, then quickly drop the acetone solution (30-60 drops / min) into the stirring ultrapure water, and continue stirring at room temperature Acetone was volatilized for 8 hours, and the volume of the aqueous solution was adjusted with ultrapure water to obtain a BODIPY aqueous solution;

[0074] Table 2

[0075]

[0076]

[0077]

Embodiment 2

[0078] Preparation of embodiment 2 solubilizing compound (formula 5) lyophilized powder

[0079] Take by weighing 3.0 mg of the BODIPY compound (formula 5) in Table 2, dissolve it with 1 ml of acetone, then quickly drop (60 drops / min) the acetone solution into 100 ml of ultrapure water under stirring, and continue stirring at room temperature for 8 hours to evaporate Acetone was adjusted to a total volume of 100ml with ultrapure water to obtain a red BODIPY aqueous solution with a BODIPY concentration of 30 μg / ml.

[0080] Add 5g of lysine to the aqueous solution as a lyoprotectant, stir to dissolve at room temperature, filter, and distribute into vials, 20ml each. Freeze-dried to obtain a red freeze-dried powder, each bottle containing BODIPY 600μg.

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Abstract

The invention provides a solubilizing BODIPY photosensitizer and a preparation method and application thereof in preparing medicine for treating body surface diseases, and belongs to the field of medicine and medical methods. The photosensitizer is obtained by dissolving fat-soluble BODIPY or aza-BODIPY in an organic solvent and achieving solubilization by conversion from an organic solution to awater system. The preparation method of the solubilizing BODIPY photosensitizer and the application of the solubilizing BODIPY photosensitizer in preparing the medicine for treating the body surface diseases are also provided. The BODIPY photosensitizer prepared by the preparation method can be applied at a lower drug concentration and dosage, the light intensity required for photoexcitation is about 10-100 mW / cm<2>, the illumination time is 10-30 minutes, the total excitation energy is about 10-180 J / cm<2>, and the tolerance and compliance of patients are significantly improved.

Description

technical field [0001] The invention belongs to the field of medicine and medical treatment methods, and in particular relates to a solubilized BODIPY photosensitizer, a preparation method and an application in preparation of medicines for treating body surface diseases. Background technique [0002] The principle of photodynamic therapy for the treatment of microbial infections on the body surface is to apply a photosensitizer to the infected area, that is, the area where the pathogenic microorganisms are located, and then irradiate the area with light of an appropriate wavelength. The photosensitizer directly interacts with the substrate / solvent under the excitation of light to generate oxygen-containing free radicals (type I reaction), or generate singlet oxygen (type II reaction). These active oxygen components such as oxygen-containing free radicals and singlet oxygen lead to the death of pathogenic microorganisms through lipid peroxidation, membrane damage and organell...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02A61K41/00A61P31/20A61P31/10A61P31/04A61P17/10A61P17/00A61P17/02A61P35/00
CPCC07F5/022A61K41/0057A61P31/20A61P31/10A61P31/04A61P17/10A61P17/00A61P17/02A61P35/00
Inventor 景遐斌郑敏王雪林文孩
Owner 景遐斌
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