Reduction-sensitive activated photodynamic nano-drug preparation and preparation method and application thereof

A nano-drug and photodynamic technology, which is applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of weak targeting of photosensitizers and poor photodynamic therapy effects, and achieve the goal of improving effectiveness and prolonging stability Effect

Inactive Publication Date: 2016-01-27
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The photosensitizer loaded by the nano-graphene oxide of this patent has relatively weak targeting, which makes the effect of photodynamic therapy poor

Method used

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  • Reduction-sensitive activated photodynamic nano-drug preparation and preparation method and application thereof
  • Reduction-sensitive activated photodynamic nano-drug preparation and preparation method and application thereof
  • Reduction-sensitive activated photodynamic nano-drug preparation and preparation method and application thereof

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Embodiment 1

[0069] A reduction-sensitive activated photodynamic nano drug dosage form, the preparation method comprising the following steps:

[0070] (1) Under the protection of nitrogen, add 0.62mmol of EDC·HCl, 0.23mmol of NHS to the dissolved 0.2mmol CH 3 In the dichloromethane solution of O-PEG-COOH, stir and react for 5h; then add 1mmol of cystamine dropwise to the reaction solution in the previous step, and continue the reaction at room temperature for 24h to obtain PEG-SS-NH 2 The crude product, after two purifications by precipitation in cold diethyl ether, was dried under vacuum to give PEG-SS-NH 2 .

[0071] (2) Add 10mgEDC to 10mL GQD solution with a concentration of 1mg / mL, sonicate for 5min; then add 100mgPEG-SS-NH 2 Add it into the above solution, and stir at room temperature for 24 hours; finally, through dialysis in an aqueous solution, the reaction impurities are removed to obtain disulfide bonded, PEG-modified graphene quantum dots GQD-SS-PEG.

[0072] (3) Add 1 mL o...

Embodiment 2

[0075] A reduction-sensitive activated photodynamic nano drug dosage form, comprising a carrier GQD-SS-PEG and a photosensitizer Ce6 loaded on the GQD-SS-PEG, wherein the photosensitizer loading is 5 wt%.

[0076] The preparation method of the above-mentioned reduction-sensitive activated photodynamic nano drug dosage form comprises the following steps:

[0077] (A) Add 7 mg of EDC to 8 mL of GQD solution with a concentration of 1 mg / mL, sonicate for 3 min, and then add 80 mg of PEG-SS-NH 2 , stirred at room temperature to react for 20h, and then dialyzed in water to remove impurities in the reaction product to obtain GQD-SS-PEG aqueous solution;

[0078](B) Add 0.5 mL of photosensitizer DMSO solution with a concentration of 25 μg / mL to 8 mL of GQD-SS-PEG aqueous solution with a concentration of 1 mg / mL, mix and sonicate for 0.2 h, then stir and react at room temperature and in the dark for 10 h;

[0079] (C) After the reaction product of step (B) is centrifuged, the resultin...

Embodiment 3

[0095] A reduction-sensitive activated photodynamic nano-pharmaceutical dosage form, comprising a carrier GQD-SS-PEG and a photosensitizer loaded on the GQD-SS-PEG, wherein the photosensitizer is loaded in an amount of 9 wt%.

[0096] The preparation method of the above-mentioned reduction-sensitive activated photodynamic nano drug dosage form comprises the following steps:

[0097] (A) Add 15mg EDC to 15mL GQD solution with a concentration of 1mg / mL, sonicate for 10min, then add 150mgPEG-SS-NH 2 , stirred at room temperature to react for 28h, and then dialyzed in water to remove impurities in the reaction product to obtain GQD-SS-PEG aqueous solution;

[0098] (B) Add 1.5 mL of photosensitizer DMSO solution with a concentration of 25 μg / mL to 15 mL of GQD-SS-PEG aqueous solution with a concentration of 1 mg / mL, mix and sonicate for 1 h, then stir and react at room temperature and in the dark for 15 h;

[0099] (C) After the reaction product of step (B) is centrifuged, the re...

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Abstract

The invention relates to a reduction-sensitive activated photodynamic nano-drug preparation and a preparation method and application thereof. The nano-drug preparation comprises a carrier GQD-SS-PEG and a photosensitizer loaded on the GQD-SS-PEG, wherein loading amount of the photosensitizer is 5-9wt%. The nano-drug preparation is prepared by the following steps: (A), adding EDC into a GQD solution for ultrasonic treatment, adding PEG-SS-NH2, stirring at room temperature for reaction, and removing impurities in a reaction product to obtain a GQD-SS-PEG water solution; (B), adding a photosensitizer DMSO solution into the GQD-SS-PEG water solution, mixing before ultrasonic treatment, and stirring for reaction at room temperature and in darkness; (C), centrifugally separating the reaction product of the step (B), subjecting supernate to ultrafiltration to remove unloaded photosensitizer to obtain a final target product. The nano-drug preparation is mainly used for inhibiting tumor growth. Compared with the prior art, the nano-drug preparation has the advantages that the photosensitizer is high in targeting ability, and the nano-drug preparation is high in treatment effectiveness and has selective killing characteristic.

Description

technical field [0001] The invention relates to the field of photodynamic therapy, in particular to a reduction-sensitive activated photodynamic nano-medicine dosage form and its preparation method and application. Background technique [0002] Photodynamic therapy (PDT) is a new type of tumor therapy developed in recent years to damage tumor tissue through biological photosensitization. It induces the destruction of tumor cell tissue by using photosensitizers absorbed by tumor cells and applying light of a specific wavelength. Compared with conventional treatment methods such as traditional surgery, chemotherapy, and radiotherapy, the advantages of PDT are: (1) It can selectively eliminate primary and recurrent tumors in specific parts without damaging normal tissues; (2) It can be combined with chemotherapy. It is performed simultaneously with radiotherapy, and both have a certain synergistic effect; (3) It can reduce the scope of surgery and improve the prognosis of pati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/14A61K47/04A61K47/34A61P35/00
Inventor 任天斌吴志勇李艳董海青李永勇
Owner TONGJI UNIV
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