Production of elaioplast

Abstract

A process for preparing the liposome of the medicine easy to be oxidized, hydrolyzed and modified includes such steps as dissolving the ester substance and the lipophilic substance to be coated in organic solvent to form oil phase, dissolving the hydrophilic substance to be coated in water to form internal water phase, mixing them, emulsifying to become W1 / O type emulsion, mixing it with proper aqueous solution, emulsifying to become W1 / O / W3 type complex emulsion, freeze drying, and hydrating to become liposome.

Description

Technical field: [0001] The invention relates to the technical field of biomedicine, in particular to a new liposome preparation method. Background technique: [0002] Liposomes are closed vesicle-like structures formed by phospholipid bilayers. Liposomes can be divided into unilamellar vesicles, multilamellar vesicles and multivesicular liposomes according to their structure. Liposomes were first discovered in 1965 by British Alec D.Bangham. Since then, it has been found that liposomes have great application value as material carriers, especially drug carriers, so liposomes have been systematically studied. [0003] After more than 20 years of exploration, researchers have proposed many valuable liposome preparation methods. At present, liposomes are mainly prepared by dispersion technique, which can be divided into three categories: 1) Based on mechanical dispersion technique. Such as the film dispersion method (filmdispersion), the phospholipids used to form liposomes...

AI Technical Summary

Problems solved by technology

[0006] (1) When the liposome is suspended in the water phase, it is a thermodynamically unstable dispersion system, and aggregation and fusion often occur, resulting in a larger particle size, and in severe cases, stratification may occur

[0007] (2) When phospholipids exist in the water phase, they are usually prone to hydrolysis and oxidation, and may form lysophospholipids. On the one hand, the toxicity of the preparation is increased, and on the other hand, liposomes are easily disintegrated, resulting in drug leakage.

[0008] (3) Liposomes are suspended in the water phase. During storage, the drug may leak, resulting in a change in the encapsulation rate, thereby affecting the efficacy of the preparation

If the drug itself is easily hydrolyzed, the stability problem of the formulation is more prominent

[0009] 2. Encapsulation rate problem

However, no matter the pH gradient or ammonium sulfate gradient active drug loading method, it is necessary to provide a large difference in pH environment inside and outside the liposome membrane, which is not only not suitable for drugs that are sensitive to acid and alkali, but also easily causes phospholipid decomposition and denaturation.

In addition, the active drug loading method is only suitable for ionizable drugs, and its application range is relatively limited

[0010] 3. Sterilization issues

This may not be possible with some liposome preparation processes

[0011] 4. Particle size control of liposomes

This in turn often leads to further leakage of the drug, affecting the quality of the formulation