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Liposome composition capable of adjusting drug release and preparation method thereof

A liposome composition and an adjustable technology, which can be applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of complex reaction steps, low cell uptake efficiency, insensitivity to acid stimulation, etc. , to achieve mild conditions, high encapsulation efficiency, and lower production costs.

Active Publication Date: 2019-01-29
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The modifiers in these two patents need to be obtained by the reaction of polyaspartic acid and fatty chains, and the reaction steps are more complicated; in addition, due to the surface modification of polyaspartic acid, the surface potential of the obtained liposomes reaches about -40mV, Such higher negatively charged nanoformulations may achieve lower cellular uptake efficiency (cell surface is negatively charged); finally, such acid-induced release may be applicable to liposomes prepared by passive It may not be suitable for liposomes prepared by stealth liposomes or active drug loading methods (such as ammonium sulfate gradient method), because the drug release behavior in these liposomes is relatively insensitive to acid stimulation

Method used

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  • Liposome composition capable of adjusting drug release and preparation method thereof
  • Liposome composition capable of adjusting drug release and preparation method thereof
  • Liposome composition capable of adjusting drug release and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] The preparation of drug-loaded liposomes containing sodium polyaspartate (15mg / mL) in the inner aqueous phase:

[0064] Preparation of blank liposomes: Dissolve distearoylphosphatidylcholine (DSPC), cholesterol, distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-PEG) at a mass ratio of 3:1:0.36 in After fully dissolving in water ether, mix well after fully dissolving, then evaporate the organic solvent ether under reduced pressure, so that film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask, and then add 0.25M ammonium sulfate and 15mg / mL sodium polyaspartate (MW=9k) aqueous solution, hydration in 50°C water bath for 30 minutes, vortexed for 5 minutes, using liposome extrusion equipment, extruding the obtained liposome suspension through polycarbonate with a pore size of 200nm and 100nm membranes 10 times each to reduce the particle size of the blank liposomes.

[0065] Encapsulation of weakly basic drugs: the bla...

Embodiment 2

[0067] The preparation of drug-loaded liposomes containing sodium polyaspartate (30mg / mL) in the inner aqueous phase:

[0068] Preparation of blank liposomes: Dissolve distearoylphosphatidylcholine (DSPC), cholesterol, distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-PEG) at a mass ratio of 3:1:0.36 in In water ether, fully dissolve and mix evenly, then evaporate the organic solvent ether under reduced pressure, so that film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask, and then add 0.25M ammonium sulfate and 30mg / mL sodium polyaspartate (MW=9k) aqueous solution, hydration in 50°C water bath for 30 minutes, vortexed for 5 minutes, using liposome extrusion equipment, extruding the obtained liposome suspension through polycarbonate with a pore size of 200nm and 100nm membranes 10 times each to reduce the particle size of the blank liposomes.

[0069] Encapsulation of weakly basic drugs: the blank liposome obtained in t...

Embodiment 3

[0071] The preparation of drug-loaded liposomes containing sodium polyaspartate (100mg / mL) in the inner aqueous phase:

[0072] Preparation of blank liposomes: Dissolve distearoylphosphatidylcholine (DSPC), cholesterol, distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-PEG) at a mass ratio of 3:1:0.36 in In water ether, fully dissolve and mix evenly, then evaporate the organic solvent ether under reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask, and then add 0.25M ammonium sulfate and 100mg / mL sodium polyaspartate (MW=9k) aqueous solution, hydration in 50°C water bath for 30 minutes, vortexed for 5 minutes, using liposome extrusion equipment, extruding the obtained liposome suspension through polycarbonate with a pore size of 200nm and 100nm membranes 10 times each to reduce the particle size of the blank liposomes.

[0073] Encapsulation of weakly basic drugs: the blank liposome obtaine...

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Abstract

The invention relates to the field of pharmacy, and discloses a liposome composition capable of adjusting drug release and a preparation method thereof. The liposome composition includes liposome, media including a water phase encapsulated in the liposome and a compound; the media include at least one polyamino acid or salt thereof, and at least one therapeutic agent; and the compound can generateion gradient inside and outside of the liposome and make the therapeutic agent encapsulate the water phase in the liposome. Through the introduction of the polyamino acids or salts thereof into the water phase in the liposome, the release situations of drugs in the liposome can be adjusted, and the adjustment effect has a certain dose dependent. The preparation method mainly relates to an activedrug loading method which can form the ion gradient inside and outside of the liposome; and the polyamino acids or salts thereof can be directly taken as an internal water phase to introduce. The preparation method is simple in technology, convenient in operation and less in control parameter, so that the reduction of production costs can be realized, and the release of the drugs in the liposome can be effectively adjusted.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a liposome composition capable of regulating drug release and a preparation method thereof. Background technique [0002] Drug therapy that does not rely on drug delivery system (drug delivery system, DDS) is usually limited by the wide biodistribution of active ingredients and low specificity to diseased cells. This in vivo behavior will not only cause the drug to be ineffective at the lesion site Concentrations may also cause serious side effects. [0003] Liposome is widely used as a drug carrier. It can not only improve the distribution of drugs in vivo, but also has a certain long-term circulation and sustained release after stealth modification, and can reduce the toxicity to normal cells. Especially for tumor treatment, due to the high permeability and retention effect (enhanced permeability and retention effect, EPR) of solid tumors, after the drug is encapsulated in liposomes, i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4745
CPCA61K9/127A61K9/1277A61K31/4745A61K47/34
Inventor 高梦华黄惠锋徐兴王振环
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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