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A kind of liposome with photodynamic effect and its preparation and application

A liposome and photodynamic technology, applied in the field of pharmaceutical preparations, can solve the problem of inability to monitor the effect in real time, and achieve the effect of fluorescence enhancement

Active Publication Date: 2021-01-15
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention solves the technical problem in the prior art that the combination of drugs and photosensitizers cannot monitor the effect in real time, and provides liposomes with photodynamic effects, wherein chemotherapeutic drugs or antibacterial drugs are embedded in the hydrophobic cavity of the liposomes , a photosensitizer is embedded in the hydrophobic cavity and / or hydrophilic cavity of the liposome, and the photosensitizer is a polypyridinium salt with aggregation-induced luminescent properties

Method used

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  • A kind of liposome with photodynamic effect and its preparation and application
  • A kind of liposome with photodynamic effect and its preparation and application
  • A kind of liposome with photodynamic effect and its preparation and application

Examples

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Embodiment 1

[0052] This embodiment provides a liposome integrating chemotherapy and photodynamic diagnosis and treatment, which is prepared from the following raw materials in weight percentage: phosphatidylcholine (S100) 65.8%, cholesterol 13.2%, chloroform: absolute ethanol (V:V=1:1) 10.9%, paclitaxel 4.1%, TPCI 6.0%.

[0053] The preparation method of the liposome integrating chemotherapy and photodynamic diagnosis and treatment is as follows:

[0054] Weigh 240mg of phosphatidylcholine (S100), 48mg of cholesterol, 15mg of paclitaxel, and 22mg of TPCI and mix them together, then add 40mg of chloroform: anhydrous ethanol mixture (V:V=1:1) to make it completely After dissolving, evaporate the organic solvent under reduced pressure at 40°C to form a thin film, then add 0.9% NaCl for hydration, and conduct probe ultrasonication under ice bath conditions, ultrasonic power is 20%, ultrasonic time is 13min, and ultrasonic frequency is working The time is 9s, and the interval is 1s; the ultra...

Embodiment 2

[0056] This embodiment provides a liposome integrating chemotherapy and photodynamic diagnosis and treatment, which is prepared from the following raw materials in weight percentage: phosphatidylcholine (S100) 60.3%, cholesterol 10.9%, chloroform: absolute ethanol (V:V=1:1) 18.6%, Paclitaxel 4.1%, TPCI 6.1%.

[0057] The preparation method of the liposome integrating chemotherapy and photodynamic diagnosis and treatment is as follows:

[0058] Weigh 220mg of phosphatidylcholine (S100), 40mg of cholesterol, 15mg of paclitaxel, and 22mg of TPCI and mix them together, then add 68mg of chloroform: anhydrous ethanol mixture (V:V=1:1) to make it completely After dissolving, evaporate the organic solvent under reduced pressure at 40°C to form a thin film, then add 0.9% NaCl for hydration, and conduct probe ultrasonication under ice bath conditions, ultrasonic power is 20%, ultrasonic time is 15min, and ultrasonic frequency is working The time is 3s, and the interval is 3s; the ultra...

Embodiment 3

[0060] This embodiment provides a liposome integrating chemotherapy and photodynamic diagnosis and treatment, which is prepared from the following raw materials in weight percentage: phosphatidylcholine (S100) 69.3%, cholesterol 10.5%, chloroform: absolute ethanol (V:V=1:1) 10.9%, paclitaxel 4.4%, TPCI 4.9%.

[0061] The preparation method of the liposome integrating chemotherapy and photodynamic diagnosis and treatment is as follows:

[0062] Weigh 253mg of phosphatidylcholine (S100), 38mg of cholesterol, 16mg of paclitaxel, and 18mg of TPCI and mix them together, then add 40mg of chloroform: anhydrous ethanol mixture (V:V=1:1) to make it completely After dissolving, evaporate the organic solvent under reduced pressure at 40°C to form a thin film, then add 0.9% NaCl for hydration, and conduct probe ultrasonication under ice bath conditions, ultrasonic power is 20%, ultrasonic time is 12min, and ultrasonic frequency is working The time is 9s, and the interval is 1s; the ultra...

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Abstract

The invention discloses a liposome with a photodynamic action, and a preparation method and application thereof, and belongs to the field of pharmaceutical preparations. The liposome is of a phospholipid bilayer structure, and cholesterol is embedded in the phospholipid bilayer structure; a chemotherapeutic drug or an antibacterial drug is embedded in a hydrophobic cavity of the phospholipid bilayer structure; a photosensitizer, namely poly-pyridinium salt with aggregation-induced luminescent properties, is embedded in the hydrophobic cavity and / or a hydrophilic cavity of the phospholipid bilayer structure. The preparation method includes adding phospholipid, the cholesterol, the drug and the photosensitizer to a co-solvent, and volatilizing the co-solvent after complete dissolution to form a film; adding the film to an aqueous phase for hydration, and then performing ultrasonication to enable the phospholipid to form the liposome of the bilayer structure. The liposome has the cell nucleus property of illuminating dead cells, and can diagnose the antitumor curative effect at an early stage and trace the antitumor effect in real time.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a liposome with photodynamic effect and its preparation and application. Background technique [0002] In 2015, there were about 3.929 million cases of malignant tumors nationwide, and about 2.338 million deaths. That is to say, more than 10,000 people are diagnosed with cancer every day, and 7.5 people are diagnosed with cancer every minute. Although a variety of anticancer drugs have been developed and used in chemotherapy, they often cause adverse side effects in patients, cause physical and mental pain, and the treatment efficiency is very low. Chemotherapeutic drugs commonly used in clinical practice include paclitaxel, doxorubicin, irinotecan, 10-hydroxycamptothecin and so on. [0003] Photodynamic therapy (PDT) is a new method applied to the treatment of solid tumors, and it is also clinically accepted as a palliative therapy for the treatment of ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K41/00A61K45/06A61K47/28A61K49/00A61P31/04A61P35/00
CPCA61K9/127A61K9/1277A61K41/0057A61K45/06A61K47/28A61K49/0021A61K49/0084A61P31/04A61P35/00A61K2300/00
Inventor 罗亮梁华庚王修霞章小平孟凡玲童军伟
Owner HUAZHONG UNIV OF SCI & TECH
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