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Photosensitive liposome and application thereof

A liposome and photosensitive technology, applied in liposome delivery, photodynamic therapy, medical preparations of non-active ingredients, etc., can solve problems such as difficult to meet urgent needs

Active Publication Date: 2020-10-23
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, traditional liposomes have become increasingly difficult to meet the urgent need for flexible adjustment of dosage regimens in current clinical applications

Method used

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  • Photosensitive liposome and application thereof
  • Photosensitive liposome and application thereof
  • Photosensitive liposome and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0042]The preparation method of the above-mentioned photosensitive liposome can be prepared according to the conventional photosensitive liposome preparation process, for example: various lipid materials (including at least one unsaturated phospholipid), photosensitizer and active ingredients (such as lipid Soluble anticancer drug tetravalent cisplatin), dissolved in chloroform:methanol (5:1) solution, at 55-60°C, the organic solvent was removed by rotary evaporation to obtain a film that was dry and uniformly attached to the bottom of the glass bottle. The obtained film is hydrated with ultrapure water at room temperature to form a uniform liposome solution, so that the concentration range of the photosensitizer in the photosensitive liposome is 10-40 μg / mL. Then, extrude through a polycarbonate membrane (for example, with a pore size of 100 nm), and repeatedly extrude several times, and the obtained tetravalent cisplatin photosensitive liposomes are stored at 4-7° C. for futu...

Embodiment 1 4

[0062] The preparation of embodiment 1 tetravalent cisplatin photosensitive liposome

[0063] (1) Materials and dosage: (the dosage of 5mL liposome, the following table 1)

[0064] Table 1

[0065]

[0066] (2) Preparation method

[0067] Weigh various lipid materials (including unsaturated phospholipids), photosensitizers and fat-soluble anticancer drugs according to the amounts in Table 1, dissolve them in 12mL of chloroform:methanol (5:1) solution, and store at 55-60°C The organic solvent was removed by rotary evaporation to obtain a dry film that evenly adhered to the bottom of the glass bottle. The obtained film was hydrated with 5 mL of ultrapure water at room temperature for 10 min to form a uniform liposome solution. Then, it was squeezed through a polycarbonate membrane with a pore size of 100 nm. After repeated extrusion 5 times, it was loaded into a cellulose acetate dialysis bag (MWCO: 3500 Da) and dialyzed in water for 24 hours. The obtained tetravalent c...

experiment example 1 4

[0074] Characterization of experimental example 1 tetravalent cisplatin photosensitive liposome

[0075] Use a dynamic light scattering instrument (DLS) to measure the tetravalent cisplatin photosensitive liposomes prepared in Example 1 and the tetravalent cisplatin photosensitive liposomes (0.5W / cm 2 , 3min) particle size, the test results are as follows figure 1 As shown, the average particle size of tetravalent cisplatin photosensitive liposome is 128nm. After laser irradiation, due to the oxidation of phospholipids, the tetravalent cisplatin photosensitive liposomes undergo membrane fusion, which makes the tetravalent cisplatin photosensitive liposomes combine together and increases the particle size of the photosensitive liposomes.

[0076] Draw 10 μ L of prepared tetravalent cisplatin photosensitive liposomes with a pipette gun and irradiate with 650 nm laser (0.5 W / cm 2 , 3min) after the tetravalent cisplatin photosensitive liposomes, dripped onto the special copper...

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Abstract

The present invention relates to a photosensitive liposome and application thereof. The photosensitive liposome comprises a lipid material and a photosensitizer, the lipid material comprises at leastone unsaturated phospholipid, the unsaturated phospholipid accounts for 20-50% by molar mass of the lipid material, and the concentration of the photosensitizer in the photosensitive liposome is 10-40[mu]g / mL. The photosensitive liposome disclosed by the invention can generate singlet oxygen under laser irradiation to oxidize unsaturated phospholipid in the liposome, change the hydrophilicity andhydrophobicity of the liposome and release entrapped contents; after the laser is removed, the structural integrity of the liposome can be recovered; and the photosensitive liposome can be subjectedto membrane fusion under laser irradiation, and the particle size is increased. The photosensitive liposome provided by the invention can be used for carrying drugs, and can realize repeated induced release of the drugs by virtue of long-time retention of tumor tissues, so that the administration frequency is reduced, and the patient compliance is improved. After single injection, treatment can bestarted and stopped at any time through exogenous laser, the dosing scheme is flexibly adjusted, and treatment is conducted multiple times according to needs.

Description

technical field [0001] The invention relates to the field of liposomes, in particular to a photosensitive liposome and its application for preparing antitumor drugs. Background technique [0002] Responsive nanocarriers can release drugs under endogenous or exogenous stimuli, which is very suitable for tumor therapy. Endogenous stimuli mainly include pH, redox, enzymes, temperature, etc. Exogenous stimuli mainly include ultrasound, light and rays. For responsive nanocarriers that rely on endogenous stimuli, the controlled release method largely depends on in vivo factors, and these factors vary greatly among individuals, often showing zero or first order under continuous stimulation conditions. Drug release, it is difficult to achieve effective intracellular concentration, especially in tumors with low sensitivity to chemotherapy drugs. For responsive nanocarriers that rely on exogenous stimuli, the triggering method of physical signals is less dependent on environmental ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K41/00A61K47/24A61P35/00
CPCA61K9/127A61K41/0057A61K41/0071A61K47/24A61P35/00
Inventor 喻志强杨媛媛于梦于玲马文邹斌华陈归孙锐
Owner SOUTHERN MEDICAL UNIVERSITY
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