Preparation method of drug-carrying liposome

A liposome and system technology, applied in the field of preparation of drug-loaded liposomes, can solve problems such as short action time, obvious drug burst effect, drug leakage, etc., to achieve a wide range of applicable dosage forms, reduce burst effect, improve The effect of encapsulation rate

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

Although there are reports of methods such as reverse phase evaporation to prepare liposomes loaded with water-soluble drugs, the drug burst release effect of this method is obvious and cannot meet the corresponding regulations of the Pharmacopoeia.
[0004] The active drug loading technology such as pH gradient method can increase the entrapment capacity of liposomes for water-soluble drugs, but the active drug loading technology is cumbersome to operate and has poor reproducibility, making it difficult to prepare in batches in an industrialized manner.
[0005] In addition, the liposomes obtained by most preparation methods are generally in a liquid state, which are difficult to store and transport, and are susceptible to problems such as flocculation, agglomeration, precipitation, and drug leakage due to changes in environmental conditions. The in vivo action time is short, which affects the effectiveness, safety and stability of the preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: Diclofenac sodium liposome

[0027] The first embodiment of the present invention adopts diclofenac sodium as the target drug, the amphiphilic macromolecular material selects povidone (PVP), and the liposome film-forming material selects hydrogenated soybean lecithin, cholesterol, Tween 80 and cetyl alcohol, Liposomes loaded with diclofenac sodium were prepared.

[0028] Experimental group: 20mg of povidone (PVP) was dissolved in 6ml of water, 8mg of diclofenac sodium was added to dissolve completely, packed in a vial, frozen at -30°C for 5 hours, freeze-dried (5×10 -4 Pa, 20h) to obtain diclofenac sodium solid freeze-dried product. 20mg of hydrogenated soybean lecithin, 6mg of cholesterol, 2mg of Tween 80 and 2mg of cetyl alcohol were dissolved in 20ml of tert-butanol, dissolved in a water bath at 65°C, and solid lyophilized product of diclofenac sodium was added, dissolved completely, and 120mg of mannitol (PVP) was added , dispersed evenly, packed in ...

Embodiment 2

[0034] Embodiment 2: Adriamycin hydrochloride liposome

[0035] The second embodiment of the present invention adopts doxorubicin hydrochloride as the target drug, the amphiphilic macromolecular material polyethylene glycol (PEG 2000), and the liposome film-forming material selects distearoylphosphatidylcholine (DSPC) , polyethylene glycol 2000 grafted distearoylphosphatidylethanolamine (DSPE-PEG2000) and Span 85 to prepare liposomes loaded with doxorubicin hydrochloride.

[0036] Experimental group: 15 mg of polyethylene glycol (PEG 2000) was dissolved in 6 ml of water, 5 mg of doxorubicin hydrochloride was added to dissolve completely, packed in a vial, frozen at -30°C for 5 hours, freeze-dried (5×10 -4 Pa, 20h) to obtain adriamycin hydrochloride solid freeze-dried product. Add 5mg of distearoylphosphatidylcholine (DSPC), 1mg of distearoylphosphatidylethanolamine (DSPE-PEG2000) grafted with polyethylene glycol 2000, and 2mg of Span 85 into 20ml of tert-butanol, in a water b...

Embodiment 3

[0042] Embodiment 3: recombinant human growth hormone liposome

[0043] The third embodiment of the present invention adopts protein drug recombinant human growth hormone as the object, the amphiphilic macromolecular material selects Poloxamer (Poloxamer 188), and the liposome film-forming material selects hydrogenated soybean lecithin, cholesterol, Tween 80 and propylene glycol to prepare liposomes loaded with recombinant human growth hormone.

[0044] Experimental group: Dissolve 20mg of Poloxamer (Poloxamer 188) in 6ml of water, add 1ml of recombinant human growth hormone (5mg / ml) and mix completely, put in a vial, freeze at -30°C for 5 hours, freeze-dry (5× 10 -4 Pa, 20h) to obtain a solid-state freeze-dried product of recombinant human growth hormone. 20mg of hydrogenated soybean lecithin, 6mg of cholesterol, 2mg of Tween 80 and 4mg of propylene glycol were dissolved in 20ml of tert-butanol, dissolved in a water bath at 65°C, and solid freeze-dried product of recombinan...

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Abstract

The invention relates to a preparation method of drug-carrying liposome. In the method, a two-step freeze-drying method is used for preparing the liposome for coating and carrying water soluble drugs, wherein a primary freeze drying process is performed in a water phase system, and a secondary freeze drying process is performed in an organic phase system. The water soluble drugs are evenly coated and carried in the liposome by the two-step freeze drying method, thus improving the envelopment rate of the drugs and reducing the initial burst release effect of the liposome for coating and carrying the water soluble drugs. The liposome prepared by the preparation method is suitable for coating various kinds of water soluble drugs and has a wide range of applicable dosage forms.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a preparation method of drug-loaded liposomes. 【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. At present, liposomes ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K45/00A61K47/34A61K47/32
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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