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Doxorubicin liposome and its preparation method

A kind of technology of doxorubicin lipid and liposome, which is applied in the field of medicine and achieves the effect of reasonable control of ethanol content

Inactive Publication Date: 2012-06-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Based on ethanol can cause lateral phase separation, resulting in increased permeability of lecithin / phosphatidylethanolamine liposome membrane, too much ethanol can easily cause liposome Aggregation, bilayer fusion and drug leakage affect the encapsulation efficiency, particle size and stability of liposomes, etc.

Method used

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  • Doxorubicin liposome and its preparation method
  • Doxorubicin liposome and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Preparation of doxorubicin hydrochloride liposomes (DOX-L) by pH gradient method

[0021] Preparation of blank liposomes

[0022] Weigh the lipid components, stir and dissolve them in a water bath at 65°C with an appropriate amount of absolute ethanol, evaporate the ethanol, add a citric acid-sodium citrate buffer solution with a certain concentration of pH=4.0, stir in a water bath at 65°C for 20 min, and obtain a blank lipid Primer. Sonicate the primary product probe for 8 min (200 w×2 min, 400 w×6 min), and pass through 0.8, 0.45, 0.22 μm microporous membranes in turn to obtain a blank liposome suspension (final phospholipid mass concentration 50 mg·mL -1 ).

[0023] Preparation and drug loading of gradient liposomes

[0024] Take 1.0 mL of the above blank liposome suspension, add a certain amount of 500 mmol L -1 Sodium phosphate solution to obtain gradient liposomes. Take a certain amount of gradient liposome and doxorubicin hydrochloride solution...

Embodiment 2

[0039] Embodiment 2 The influence of ethanol residue on liposome

[0040] prescription composition

[0041] Distearoylphosphatidylcholine (DSPC) 3g

[0042] Cholesterol (CH) 1g

[0043] Macrogol 1000 Cholesterol Hemisuccinate (mPEG1000-CHEMS) 0.5g

[0044] Weigh the prescription quantities of DSPC, CH, mPEG1000-CHEMS, and use 2.5%, 5.0%, 10%, 15%, 20%, 25%, 30% and 40% (volume ratio of ethanol to hydration medium) of absolute ethanol respectively Dissolve the membrane material, add 300 mmol·L of pH=4.0 -1 citric acid-sodium citrate buffer solution, the final concentration of phospholipids was 50 mg·mL -1 , and stirred in a water bath at 65°C for 20 min to obtain the primary blank liposome. Sonicate the primary product probe for 8 min (200 w×2 min, 400 w×6 min), then pass through the microporous membranes of 0.8, 0.45, and 0.22 μm in sequence to obtain a blank liposome suspension, which was measured by laser particle size The particle size of each liposome was measured by...

Embodiment 3

[0046] Embodiment 3 Adriamycin liposome preparation

[0047] Preparation of lipid mixture powder: mix HSPC, CHOL and PEG2000-DSPE according to the mass ratio (3:1:1), dissolve in ethanol to obtain a clear solution, and obtain lipid powder after spray drying (tert-butanol can also be used to dissolve each Lipid composition, lipid powder obtained by freeze-drying method).

[0048] Preparation of blank liposomes: the above-mentioned lipid powder was hydrated with 300 mM ammonium sulfate solution at 50-65° C., and sheared and dispersed to obtain multilamellar liposomes with uneven particle sizes. Add different amounts of absolute ethanol, use microfluidic equipment to reduce the particle size of liposomes (about 80nm), and prepare liposomes containing different concentrations of ethanol.

[0049] Preparation of gradient liposomes: use ion exchange resin / fiber to remove ammonium sulfate in the outer water phase of liposomes.

[0050] Drug loading: add adriamycin hydrochloride sol...

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Abstract

Belonging to the technical field of medicines, the invention discloses a doxorubicin liposome and its preparation method. The doxorubicin liposome is composed of doxorubicin, a phospholipid substance, cholesterol, and a PEG lipid derivative, etc. The doxorubicin liposome prepared by a pH gradient method in the invention has an encapsulation rate higher than 96%, ethanol content not greater than 10%, and almost constant related parameters. The preparation and its preparation method provided in the invention can control the ethanol content during liposome preparation, and ensures that the residual ethanol has no substantial influence on liposome property in the preparation process, thus providing reference for liposome preparation and ethanol content control in industrial production.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to adriamycin liposomes and a preparation method thereof. The preparation method can control the ethanol content in the liposome preparation process, and ensure that the residual ethanol in the preparation process has no significant effect on the liposome properties. sexual influence. Background technique: [0002] Doxorubicin (Doxorubicin) is a common classic antibiotic broad-spectrum antineoplastic drug. Its mechanism of action is mainly to inhibit the synthesis of RNA and DNA by affecting the activity of topoisomerase II, and its inhibitory effect on RNA is the strongest. It is a cycle non-specific drug, which can kill tumor cells in various growth cycles. Doxorubicin is a broad-spectrum antineoplastic drug, clinically used for the treatment of acute lymphoblastic leukemia, acute myelogenous leukemia, Hodgkin and non-Hodgkin lymphoma, breast cancer, lung cancer, ovarian cancer,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61K47/32A61K47/34A61P35/00A61P35/02
Inventor 邓意辉杨强
Owner SHENYANG PHARMA UNIVERSITY
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