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Rupturable PEG modified adriamycin liposome preparation method

A doxorubicin lipid and liposome technology, applied in the field of medicine, can solve the problems of low tumor accumulation, and achieve the effects of good dispersion, improved anti-tumor efficiency and high drug loading capacity

Inactive Publication Date: 2016-02-10
孙仁
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

TAT peptide, as a potent cell-penetrating peptide, is modified in liposomes to promote efficient liposome entry, but the non-selective specificity of TAT leads to its low tumor accumulation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0012] The preparation method of cleavable PEG-loaded doxorubicin liposome comprises the following steps.

[0013] (1) Put the prescribed amount of SPC, Cho, DSPE-PEG-TAT, and DSPE-PEG-OMe in a 50ml eggplant-shaped bottle, dissolve in chloroform and then evaporate to form a film, put it in a vacuum desiccator overnight, add 2.5ml of PBS buffer, In an air-bath shaker, 35°C, 150rpm, 28min hydration, water-bath ultrasonication for 5min to remove the membrane, and probe ultrasonication to prepare liposomes co-modified with TAT and blocking PEG (lipid concentration 2.068μmol / ml); among them, Rh - For PE-labeled liposomes, it is necessary to add fluorescently-labeled phospholipids to the lipid material, and the dosage is 20 μg per liposome.

[0014] (2) After the lipid material was drained to form a film, 1 mL of ammonium sulfate buffer was added, hydrated and ultrasonicated to prepare uniform small single-lamellar liposomes. The 1mL liposome was eluted with a certain buffer soluti...

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Abstract

The invention belongs to the technical field of medicines, particularly relates to an adriamycin liposome preparation method and provides an adriamycin liposome preparation method with a function of improving tumor accumulation and tumor cell entering efficiency. The method includes the steps: (1) putting prescribed SPC, Cho, DSPE-PEG-TAT, DSPE-PEG-OMe into a 50ml eggplant-shaped flask, dissolving in chloroform, performing rotary evaporation to form a membrane, staying overnight in a vacuum drier, and adding 2.5ml of PBS buffer solution; (2) sucking dry a lipid material to form a membrane, adding 1ml of ammonium sulfate buffer solution, and ultrasonically hydrating to prepare uniform single unilamellar vesicles; (3) eluting the 1ml of single unilamellar vesicles with a certain buffer solution, replacing an external water phase through a gel column, and incubating at a certain temperature to obtain adriamycin liposome.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a preparation method of doxorubicin-loaded liposomes. Background technique [0002] After the lipid material was drained to form a film, 1 mL of ammonium sulfate buffer was added, hydrated and ultrasonicated to prepare uniform small single-lamellar liposomes. The 1mL liposome was eluted with a certain buffer solution and passed through a SephadexG50 gel column to replace the outer water phase, and the liposome fraction was collected in a 2mL volumetric flask. After constant volume with the outer water phase buffer solution, add an appropriate amount of doxorubicin hydrochloride Aqueous plain solution, incubated at a certain temperature to obtain doxorubicin liposomes. An ideal tumor-targeted drug delivery system needs to have both high-efficiency tumor accumulation and strong cell entry. Modifying polyethylene glycol on the surface of liposomes can significantly prolong the c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61K47/10A61K47/42A61P35/00
Inventor 孙仁
Owner 孙仁
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