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Novel cationic liposome nucleic acid pharmaceutical preparation as well as preparation method and application thereof

A technology of cationic liposomes and cationic lipids, which can be used in liposome delivery, other methods of inserting foreign genetic materials, drug combinations, etc.

Active Publication Date: 2013-07-10
INST OF PROCESS ENG CHINESE ACAD OF SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it was found in the application that although the cationic liposome gene transfection reagent based on DSPE-PEG modification has low cytotoxicity, good serum stability and simple operation, it still has the following disadvantages: (1) PEG modification affects the effect of cationic liposome on The compounding ability of the gene leads to poor gene compounding ability of the cationic liposome and a decrease in the embedding rate; (2) PEG modification affects the endosome escape process of the cationic liposome gene transfection reagent, resulting in the ineffective release of the gene into the cytoplasm, Reduced gene transfection efficiency
[0004] Another commonly used cationic liposome Lipofectamine TM 2000 (Invitrogen) has good gene complex ability and endosome escape ability, but its cytotoxicity is high (survival rate <50%), and its stability in serum is not good, so the transfection efficiency is also low. The medium needs to be replaced during the process, and the operation is more complicated

Method used

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  • Novel cationic liposome nucleic acid pharmaceutical preparation as well as preparation method and application thereof
  • Novel cationic liposome nucleic acid pharmaceutical preparation as well as preparation method and application thereof
  • Novel cationic liposome nucleic acid pharmaceutical preparation as well as preparation method and application thereof

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Embodiment 1

[0062] The preparation of embodiment 1 cationic liposome nucleic acid drug preparation

[0063] 1) Preparation of cationic liposomes: weigh cationic lipid DDAB (9.46 mg, 15 μmol), cholesterol (5.80 mg, 15 μmol) and DSPE-PCB 20 (32.86mg, 6μmol) 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 phosphate buffer saline (PBS, pH=7.4) containing 10% lactose to 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...

Embodiment 2

[0066] The preparation of embodiment 2 cationic liposome nucleic acid drug preparation

[0067] 1) Preparation of cationic liposomes: weigh cationic lipid DDAB (4.73 mg, 7.5 μmol), cholesterol (5.80 mg, 15 μmol) and DSPE-PCB 10 (16.83mg, 6μmol) 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 phosphate buffer saline (PBS, pH=7.4) containing 5% lactose to the flask, and use an ultrasonic cleaner to ultrasonicate for 15 minutes 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 liposo...

Embodiment 3

[0070]The preparation of embodiment 3 cationic liposome nucleic acid drug preparation

[0071] 1) Preparation of cationic liposomes: weigh cationic lipid DDAB (9.46 mg, 15 μmol), cholesterol (5.80 mg, 15 μmol) and DSPE-PCB 20 (16.43mg, 3μmol) 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 15 mL of phosphate buffered saline (PBS, pH=7.4) containing 20% ​​maltose to 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 pres...

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Abstract

The invention discloses a novel cationic liposome, a cationic liposome nucleic acid pharmaceutical preparation having the same as well as a preparation method and application thereof. The cationic liposome comprises cationic lipid, assisted lipo, polycarboxyl betaine lipid molecule and a freezing protective agent. The cationic liposome nucleic acid pharmaceutical preparation comprises cationic liposome modified by neutral lipid of polycarboxyl betaine and nucleic acid pharmaceutical preparation working solution. According to the cationic liposome, the defects of high toxicity, bad blood stability and low transfection efficiency are overcome and the pharmaceutical effects of the nucleic acid drugs are effectively improved; and at the same time, as the preparation is undisturbed by blood serum during the use, the operations in the experiment and the treatment are simplified.

Description

technical field [0001] The present invention relates to cationic liposomes, more specifically to cationic liposomes containing polycarboxybetaine neutral lipids, nucleic acid drug preparations containing them, their preparation methods and applications. Background technique [0002] Gene transfection is the transfer of nucleic acids with biological functions into cells, and the nucleic acids maintain their biological functions in cells. Because the naked nucleic acid molecules are easily degraded by ribozymes in tissues or cells, and the nucleic acid molecules themselves have negative charges, which are not conducive to the function of cell membranes and poor cell penetration. Therefore, researchers actively develop a variety of gene carriers, and continue to study and improve their selectivity, safety and high efficiency. At present, vectors commonly used in research and clinical applications are roughly divided into two categories: viral vectors and non-viral vectors. Vi...

Claims

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Application Information

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IPC IPC(8): C12N15/87A61K47/34A61K48/00A61K31/7052A61K9/127A61P7/04A61P43/00A61P3/06A61P35/00A61P9/00A61P31/00A61P29/00A61P31/18
Inventor 张欣梁子才梁兴杰代凤英李燕程强
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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