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Photosensitive liposomes and their applications

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, improve patient compliance, maintain effective concentration, The effect of restoring structural integrity

Active Publication Date: 2021-10-01
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 liposomes and their applications
  • Photosensitive liposomes and their applications
  • Photosensitive liposomes and their applications

Examples

Experimental program
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Effect test

preparation example Construction

[0042]The preparation method of the above-mentioned photoreceptic liposome can be prepared according to conventional photosensitive liposome, for example, various liposomes (at least one unsaturated phospholipid), photosensitizer, and active ingredients (for example, fat), photosensitizers and active ingredients (for example, lipids), photosensitizers and active ingredients (for example, lipids) Soluble anti-cancer drugs were cisplatin), dissolved in chloroform: methanol (5: 1) solution, 55-60 ° C and evaporated to remove organic solvent, resulting in dryness, uniformly attached to the glass bottle. Film. The obtained film was hydrated by ultrapure water to hydrate a homogeneous liposome solution, allowing the photosensitive agent in the concentration of 5-40 μg / ml in the photosensitive liposome. Then, the extrusion of the polycarbonate film (e.g., 100 nm of a pore diameter), and repeatedly squeezed several times, the quadrated cisplatin photoreceptic liposome was stored in 4 to...

Embodiment 1 4

[0062] Example 1 Preparation of tetrability cisplatin photoresist

[0063] (1) Materials and quantities: (5ml liposome), Table 1 below

[0064] Table 1

[0065]

[0066] (2) Preparation method

[0067] The various lipid materials (including unsaturated phospholipids), photosensitizers, and lipid-soluble anticancer drugs are weighed in Table 1, dissolved in 12 ml of chloroform: methanol (5: 1), 55-60 ° C The organic solvent was removed to remove the organic solvent to give a dry, uniformly attached to the film of the glass bottle. The resulting film was hydrated with 5 ml of ultrapure water to form a homogeneous liposome solution for 10 min. Then, the extrusion of the polycarbonate film, a pore diameter of 100 nm, and the acetate dialysis bag (MWCO: 3500 Da) was placed in water after dialysis 24 h after repeated extrusion. The obtained tetrability cisplatin photosensitive liposomes were stored at 4 to 7 ° C. The tetrability cisplatin photosensitive liposomes used in the followin...

experiment example 1 4

[0074] Experimental example 1 Characterization of tetrability cisplatin photorestated lesom

[0075] Using a Dynamic Light Scatterometer (DLS) to determine the quadrated cisplatin photorestoryctivomer and a quadrated cisplatin photosensitive liposome (0.5 W / cm) after 650 nm laser irradiation with 650 nm 2 , 3min) particle size, test results such as figure 1 As shown, the average particle diameter of the tetrability cis platinum photoinitrid is 128 nm. After laser irradiation, since the oxidation of phospholipids causes the film fusion of the tublatin permeable liposome, the tetraviolabus is bonded together, and the particle size of the photosensitive liposome is increased.

[0076] 10 μl of the prepared tetramiplatin photosensitive liposomes were taken with a pipette and laser irradiation with 650 nm (0.5 w / cm) 2 After 3 minutes, the quadratic copper side of the transmissive electron microscope (TEM) was dried overnight, and it was obtained after the plane was tested. figure ...

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Abstract

The invention relates to a photosensitive liposome and an application thereof, which comprises a lipid material and a photosensitizer, the lipid material includes at least one unsaturated phospholipid, and the molar mass ratio of the unsaturated phospholipid to the lipid material is 20-50%. The concentration of the photosensitizer in the photosensitive liposome is 10‑40 μg / mL. The photosensitive liposome of the present invention can generate singlet oxygen under laser irradiation, oxidize the unsaturated phospholipids in the liposome, change the hydrophilicity and hydrophobicity of the liposome, and release the contained content; after removing the laser, It can also restore the structural integrity of the liposome; the photosensitive liposome can undergo membrane fusion under laser irradiation and increase the particle size. The photosensitive liposome provided by the present invention can be used for drug loading, and can achieve repeated induced release of drugs by means of long-term retention in tumor tissues, reduce the frequency of administration, and improve patient compliance. After a single injection, the treatment can be started and stopped at any time through the external source laser, the dosing regimen can be flexibly adjusted, and multiple treatments can be performed as needed.

Description

Technical field [0001] The present invention relates to the field of liposomes, and in particular, to a photoreceptic liposome and its application thereof for the preparation of anti-tumor drugs. Background technique [0002] The responsive nano carrier can release the drug under endogenous stimulation or exogenous stimulation, which is ideal for tumor treatment. Endogenous stimuli mainly includes pH, redox reduction, enzyme, temperature, and the like. Exogenous stimuli mainly includes ultrasound, light and rays. For the response nano-carrier relying on endogenous stimulus, its control is largely dependent on in vivo factors, and the individual differences between these factors are large, and often appear to be zero or primary under continuous stimulation conditions. Drug release, it is difficult to achieve effective intracellular concentration, especially a tumor having a lower sensitivity of chemotherapy drugs. For a responsive nano carrier relying on exogenous stimuli, the phy...

Claims

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Application Information

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Patent Type & Authority Patents(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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