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Preparation method of liposome for coating and carrying water soluble drugs

A technology of water-soluble drugs and liposomes, applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve complex problems, improve encapsulation efficiency, reduce leakage, and reduce complexity sexual effect

Active Publication Date: 2011-09-21
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the pH gradient method of the existing active drug loading technology all forms blank liposomes first, then utilizes the pH value of the external phase to be adjusted, and uses the pH gradient to transfer the drug from the external phase to the internal phase system. The operations are divided into preparing blank liposomes, adjusting After the pH value forms a pH gradient, the two processes of encapsulating the drug are relatively complicated.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: Irinotecan hydrochloride liposome

[0027] First embodiment of the present invention prepares the liposome of strong acid and weak base salt, adopts irinotecan hydrochloride as target drug, and liposome film-forming material selects distearoylphosphatidylcholine (DSPC), polyethylene glycol 2000 grafted distearoylphosphatidylethanolamine (DSPE-PEG2000), cholesterol and Tween 85, the organic phase solvent is ethanol, and the water phase is a phosphate buffer (pH7) containing water-soluble macromolecular polymer hydroxyethyl starch .5-8.0), preparing liposomes loaded with irinotecan hydrochloride.

[0028] Preparation method: 5mg irinotecan hydrochloride, 5mg distearoylphosphatidylcholine (DSPC), 0.5mg polyethylene glycol 2000 grafted distearoylphosphatidylethanolamine (DSPE-PEG2000), 2mg cholesterol and 2mg spit Wen 85 was added to 25ml of absolute ethanol, and heated in a 60°C water bath until completely dissolved to form an organic phase. Add 0.4 g of hy...

Embodiment 2

[0032] Embodiment 2: Diclofenac sodium liposome

[0033] The second embodiment of the present invention prepares the liposome of strong base and weak acid salt, adopts diclofenac sodium as target drug, liposome film-forming material selects hydrogenated soybean lecithin, cholesterol, Span 80 and cetyl alcohol, organic phase solvent It is ethanol, the water phase is acetic acid-sodium acetate buffer solution, and water-soluble polymer polyvinyl alcohol (PVA) is added to prepare liposomes encapsulating diclofenac sodium.

[0034]Preparation method: Add 5mg of diclofenac sodium, 40mg of hydrogenated soybean lecithin, 10mg of cholesteryl lipid and 3mg of Span 80 into 25ml of absolute ethanol, heat in a water bath at 60°C until completely dissolved, and form an organic phase. 0.1 g of propylene glycol and 0.5 g of polyvinyl alcohol (PVA) were added to 30 ml of 0.035 mol / L acetic acid-sodium acetate buffer solution with pH=5.5, and dissolved to form an aqueous phase. Draw the organ...

Embodiment 3

[0038] Embodiment 3: Adriamycin hydrochloride liposome

[0039] The first embodiment of the present invention prepares nanoscale liposome, adopts doxorubicin hydrochloride as target drug, liposome film-forming material selects hydrogenated egg yolk phospholipid, cholesterol, Tween 80, organic phase solvent is ethanol, water phase is Phosphate buffer solution (pH7.5-8.0) containing stabilizer propylene glycol and water-soluble polymer Poloxamer (Poloxamer 188), obtained by a high-pressure homogenization method with a particle size in the nanometer range of loaded doxorubicin hydrochloride unilamellar liposomes.

[0040] Preparation method: Add 5mg of doxorubicin hydrochloride, 10mg of hydrogenated egg yolk phospholipid, 5mg of cholesterol and 3mg of Tween 80 into 25ml of absolute ethanol, heat in a 60°C water bath until completely dissolved, and form an organic phase. 0.1 g of propylene glycol and 0.5 g of Poloxamer (Poloxamer 188) were added to 30 ml of 0.035 mol / L phosphate ...

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Abstract

The invention relates to a preparation method of liposome for coating and carrying water soluble drugs, comprising the following steps of: dissolving drugs in a salt form and a phospholipid material in an organic solvent to form an organic phase system; preparing a water solution buffer system with the pH value different from that of the organic phase system as a water phase system; and mixing the organic phase system with the water phase system by adopting an injection method to form liposome, wherein the solubility of the drugs is reduced due to the change of the pH value in the process of mixing the organic phase system into the water phase system, so that the drugs are coated and carried in the formed liposome. The preparation method provided by the invention combines the traditional ethanol injection method with the pH gradient method, the internal phase is injected into the external phase, and simultaneously, the liposome is prepared and the drugs are coated and carried in one step by utilizing the difference of pH between the internal phase and the external phase, thereby reducing the complexity of the traditional preparation method of liposome for coating and carrying water soluble drugs.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a preparation method of liposomes encapsulating water-soluble drugs. 【Background technique】 [0002] Liposomes are monolayer or multilayer microcapsules composed of ordered lipid bilayers. Liposome belongs to the colloidal system, has a cell-like structure, has a strong affinity with the cell membrane, and can increase the ability of the encapsulated drug to penetrate the cell membrane. Liposomes have good biocompatibility, can realize targeted delivery of drugs in vivo, and have many advantages such as prolonging drug action time, increasing drug stability in vivo and in vitro, reducing drug toxicity, and enhancing pharmacological effects. [0003] There are many methods for preparing liposomes, such as film dispersion method, reverse phase evaporation method, freeze-drying method, injection method, ultrasonic dispersion method, etc., ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/34
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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