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Long-circulating liposome capable of avoiding accelerated blood clearance (ABC) phenomenon, and preparation method and application thereof

A long-circulation liposome technology that accelerates blood clearance, applied in liposome delivery, blood diseases, medical preparations of non-active ingredients, etc., can solve liposome long-circulation function reduction, toxic side effects, and poor therapeutic effect and other problems to achieve the effect of increasing serum stability and simplifying treatment operations

Inactive Publication Date: 2015-05-27
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This phenomenon leads to a decrease in the enrichment of the drug at the target site, poor therapeutic effect, and even clinical toxic side effects.
Some researchers avoid this phenomenon of PEGylated liposomes by changing the chemical structure of PEG on the surface of liposomes or changing the route of administration, but this greatly reduces the long-term circulation function of liposomes and cannot meet the requirements of treatment.
[0004] Therefore, the current PEGylated liposomes are difficult to meet the needs of clinical application because of the process of affecting the endocytosis of liposomes and the escape of endosomes, and the ABC phenomenon of multiple administrations.

Method used

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  • Long-circulating liposome capable of avoiding accelerated blood clearance (ABC) phenomenon, and preparation method and application thereof
  • Long-circulating liposome capable of avoiding accelerated blood clearance (ABC) phenomenon, and preparation method and application thereof
  • Long-circulating liposome capable of avoiding accelerated blood clearance (ABC) phenomenon, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The preparation of embodiment 1 liposome pharmaceutical preparation

[0057] 1) Prepare blank liposomes: weigh phospholipid POPC 60.00mg, cholesterol 24.74mg and DSPE-PCB 20 40.86mg in a 100mL round bottom flask, add 30mL of chloroform to fully dissolve the solid, shake well. Using a rotary evaporator at a rotational speed of 140 rpm and a temperature of 55° C., the solvent chloroform was removed by rotary evaporation under reduced pressure to form a thin oil film, which was dried with a vacuum pump for 12 hours to ensure that the chloroform was completely removed. Add 30 mL of 200 mM ammonium sulfate solution into the flask, and use an ultrasonic cleaner to ultrasonicate for 30 min at a frequency of 90% to form a translucent emulsion. The emulsion is added to a high-pressure homogenizer, and under the condition of a pressure of 100 MPa, overpressure is performed 5 times. Add the emulsion into the liposome extruder, under the pressure of 150MPa, overpressure 10 times ...

Embodiment 2

[0059] The preparation of embodiment 2 liposome pharmaceutical preparations

[0060] 1) Prepare blank liposomes: weigh 60 mg of phospholipid POPC, 24.74 mg of cholesterol and DSPE-PCB 10 50.88mg in a 100mL round bottom flask, add 30mL of chloroform to fully dissolve the solid, shake well. Using a rotary evaporator at a rotational speed of 100 rpm and a temperature of 40°C, the solvent chloroform was removed by rotary evaporation under reduced pressure to form a thin oil film, which was dried with a vacuum pump for 6 hours to ensure that the chloroform was completely removed. Add 10 mL of 200 mM ammonium sulfate solution into the flask, and use an ultrasonic cleaner to ultrasonicate for 15 min at a frequency of 50% to form a translucent emulsion. Add the emulsion into a high-pressure homogenizer, and under the condition of a pressure of 50 MPa, overpressure 3 times. Add the emulsion into the liposome extruder, and under the pressure of 100MPa, overpressure 3 times to prepare ...

Embodiment 3

[0062] The preparation of embodiment 3 liposome pharmaceutical preparations

[0063] 1) Prepare blank liposomes: weigh 60.00 mg of phospholipid POPC, 24.74 mg of cholesterol and DSPE-PCB 5016.43mg in a 100mL round bottom flask, add 30mL of chloroform to fully dissolve the solid, shake well. Using a rotary evaporator at a rotational speed of 200 rpm and a temperature of 80°C, the solvent chloroform was removed by rotary evaporation under reduced pressure to form a thin oil film, which was dried with a vacuum pump for 36 hours to ensure that all chloroform was removed. Add 15mL of 200mM ammonium sulfate solution into the flask, and use an ultrasonic cleaner to sonicate for 1 hour at a frequency of 150%, to form a translucent emulsion. Add the emulsion into a high-pressure homogenizer, and under the pressure of 150MPa, overpressurize 10 times. Add the emulsion into the liposome extruder, under the pressure of 200MPa, overpressure 15 times to prepare DSPE-PCB 20 Modified blank ...

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Abstract

The invention relates to a long-circulating liposome capable of avoiding an accelerated blood clearance (ABC) phenomenon, a medicine preparation containing the long-circulating liposome, and a preparation method and an application of the long-circulating liposome. The long-circulating liposome provided by the invention comprises phospholipid, auxiliary lipid and poly carboxyl betaine lipid, wherein the long-circulating liposome and the preparation thereof can be applied to medicines for treating related diseases. According to the long-circulating liposome for avoiding the ABC phenomenon provided by the invention, the defect that a common liposome is easily recognized by a reticular endothelium system is overcome; a long-circulating effect of blood is reached; meanwhile, the ABC phenomenon caused by multiple intravenous injections of the PEG-modified long-circulating liposome is avoided; the medicine effect of a therapeutic medicine is effectively improved; and the long-circulating liposome has a high application prospect in the field of medicines.

Description

technical field [0001] The present invention relates to long-circulation liposomes, in particular to a long-circulation liposome that avoids the phenomenon of accelerated blood clearance, more specifically to a liposome containing polycarboxybetaine lipids, pharmaceutical preparations containing it and their The preparation method and application of Background technique [0002] As a drug carrier, liposome has the advantages of good biocompatibility, reduced drug toxicity, increased drug stability, and enhanced drug targeting. As a drug carrier, liposomes have always attracted the attention of researchers. Drug carriers have been used in many ways. However, liposome-based pharmaceutical preparations are easily recognized by the reticuloendothelial system (RES), although this can improve the safety of some therapeutic drugs, it cannot effectively exert drug activity. The hydrophilic substructure of the liposome surface is changed by macromolecular substances to form liposom...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/34A61K47/24A61K31/704A61K31/4745A61P35/00A61P35/02A61P9/00A61P31/00A61P3/06A61P29/00A61P31/18A61P7/04
Inventor 张欣李燕刘瑞瑗
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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