A liposome composition capable of regulating drug release and its preparation method

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., and can solve the problems of complex reaction steps, insensitivity to acid stimulation, low cell uptake efficiency, etc. , to achieve the effects of mild conditions, reduced production costs and simple preparation process

Active Publication Date: 2021-05-14
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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  • A liposome composition capable of regulating drug release and its preparation method
  • A liposome composition capable of regulating drug release and its preparation method
  • A liposome composition capable of regulating drug release and its preparation method

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 regulating drug release and a preparation method thereof. The liposome composition includes: liposome; a medium comprising an aqueous phase encapsulated within said liposome; a compound; said medium comprising: at least one polyamino acid or a salt thereof; at least one therapeutic agent; said compound It is a compound that can generate an ion gradient inside and outside the liposome and encapsulate the therapeutic agent in the aqueous phase of the liposome. The invention introduces the polyamino acid or its salt into the water phase in the liposome to regulate the release of the drug in the liposome, and the regulating effect has certain dose dependence. The preparation method of the liposome composition mainly relates to an active drug loading method that can constitute an ion gradient inside and outside the liposome, and the polyamino acid or its salt can be directly introduced as the inner water phase. Less, helps to reduce production costs, and can effectively regulate the release of drugs in liposomes.

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 Patents(China)
IPC IPC(8): A61K9/127A61K31/4745
CPCA61K9/127A61K9/1277A61K31/4745A61K47/34
Inventor 高梦华梁锦锋黄惠锋徐兴王振环
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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