A kind of hyaluronic acid modified mitochondria targeting liposome and preparation method thereof

A technology of hyaluronic acid modification and targeting liposomes, which can be applied in the directions of liposome delivery, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of the anti-tumor effect of paclitaxel, etc., To avoid systemic side effects, increase circulation time, and increase drug concentration

Active Publication Date: 2021-09-24
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ordinary paclitaxel liposomes cannot target the tumor site, and due to the influence of multidrug resistance, the antitumor effect of paclitaxel has been greatly affected

Method used

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  • A kind of hyaluronic acid modified mitochondria targeting liposome and preparation method thereof
  • A kind of hyaluronic acid modified mitochondria targeting liposome and preparation method thereof
  • A kind of hyaluronic acid modified mitochondria targeting liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] A preparation method of hyaluronic acid-modified mitochondria-targeted paclitaxel liposomes

[0030] Dissolve egg yolk lecithin, cholesterol, paclitaxel and dequalinium chloride in a mixed solution of chloroform:methanol 1:1 according to the molar ratio of 95:5:10:20, evaporate to dryness with a rotary evaporator to form a thin film and continue vacuum drying 1h, then add 100ml of 0.02M phosphate buffer solution, hydrate in a water bath at 40°C, and disperse the lipid film evenly, and hydrate the liposomes at 40°C for 1h. The hydrated liposome suspension was passed through a film squeezer equipped with a 100nm polycarbonate film, and the film was squeezed 10 times at 50°C. The activated hyaluronic acid was added dropwise to the prepared liposomes at a mass ratio of 1:20, and reacted overnight in a shaker. The particle size, zeta and PDI of the sample were measured by a particle size analyzer, the paclitaxel concentration of the liposome was measured by high performance...

Embodiment 2

[0033] A preparation method of hyaluronic acid-modified mitochondria-targeted paclitaxel liposomes

[0034] Dissolve hydrogenated soybean phospholipid HSPC, dioleoylphosphatidylethanolamine DOPE, cholesterol, paclitaxel and dequalinium chloride in a mixed solution of chloroform:methanol 1:1 according to the molar ratio of 60:35:5:5:10, and use rotary evaporation Evaporate it into a thin film and continue vacuum drying for 1 hour, then add 100ml of 0.02M phosphate buffer solution, hydrate in a water bath at 40°C, and disperse the lipid film evenly, and hydrate the liposomes at 40°C for 1 hour. The hydrated liposome suspension was passed through a film squeezer equipped with a 100nm polycarbonate film, and the film was squeezed 10 times at 50°C. The activated hyaluronic acid was added dropwise to the prepared liposomes at a mass ratio of 1:20, and reacted overnight in a shaker. The particle size, zeta and PDI of the sample were measured by a particle size analyzer, the paclitax...

Embodiment 3

[0037] A preparation method of hyaluronic acid-modified mitochondria-targeted paclitaxel liposomes

[0038]Dissolve soybean lecithin, cholesterol, paclitaxel and dequalinium chloride in a mixed solution of chloroform:methanol 1:1 according to the molar ratio of 60:35:5:10:15, evaporate it to dryness with a rotary evaporator to form a thin film and keep vacuuming Dry for 1 hour, then add 100ml of 0.02M phosphate buffer solution, hydrate in a water bath at 40°C, and disperse the lipid film evenly, and hydrate the liposomes at 40°C for 1 hour. The hydrated liposome suspension was circulated 3 times at 300 bar at 50°C under the action of a homogenizer, and homogenized 10 times at 1100 bar. The activated hyaluronic acid was added dropwise to the prepared liposomes at a mass ratio of 1:20, and reacted overnight in a shaker. The particle size, zeta and PDI of the sample were measured by a particle size analyzer, the paclitaxel concentration of the liposome was measured by high perfo...

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Abstract

The invention discloses a hyaluronic acid modified mitochondria targeting liposome and a preparation method thereof. The mitochondria-targeted liposome of the present invention is composed of drug-loaded liposomes and hyaluronic acid modified on the outer layer, and the drug-loaded liposomes are liposomes loaded with hydrophobic drugs and dequalinium chloride, hydrophobic Sexual drugs are selected from any one of doxorubicin, paclitaxel, 10-hydroxycamptothecin, irinotecan or cisplatin. The beneficial effect of the present invention is that the hyaluronic acid-modified liposomes can effectively target receptors, increase the uptake of liposomes by tumor cells, and further target the mitochondria of cells in tumor cells, thereby achieving the goal of destroying mitochondria. function, promote the apoptosis of tumor cells, inhibit the growth of tumor cells, and achieve the ability to overcome the multidrug resistance of tumor cells.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a hyaluronic acid-modified mitochondria-targeted liposome and a preparation method thereof. Background technique [0002] Cancer is one of the diseases that are difficult to cure in modern medicine. One of the important reasons is that the multidrug resistance of tumors greatly reduces the effect of antitumor drugs. In recent years, the targeted delivery of drugs in tumor cells is a rapidly developing field. Mitochondria are the organelles in tumor cells that guarantee cell energy metabolism and regulate cell apoptosis. Targeting mitochondria can promote cell apoptosis and effectively To effectively overcome the multidrug resistance of tumor cells and enhance the anti-tumor effect of drugs has gradually become a research direction to effectively overcome the multidrug resistance of tumor cells. [0003] Paclitaxel (PTX) is a natural drug with broa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/61A61K31/4709A61P35/00A61K31/337
CPCA61K9/0019A61K31/337A61K31/4709A61K47/61A61K47/6911A61P35/00A61K2300/00
Inventor 甘莉田永丰张华秦艳梅李东
Owner SHANGHAI INST OF TECH
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