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Preparation method of bortezomib liposome preparation

A technology of liposome preparation and bortezomib, which is applied in the fields of liposome delivery, pharmaceutical formula, boron compound active ingredients, etc. It can solve the problems of low encapsulation efficiency of bortezomib, large liposome particle size and complicated operation And other issues

Inactive Publication Date: 2021-06-08
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing bortezomib liposome preparation method is complicated to operate, the liposome particle size is relatively large, and the encapsulation efficiency of bortezomib is not high simultaneously, therefore, a kind of simple liposome preparation method is urgently needed to meet the requirements of boron. Administration of Tezomib

Method used

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  • Preparation method of bortezomib liposome preparation
  • Preparation method of bortezomib liposome preparation

Examples

Experimental program
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Embodiment 1

[0026] A preparation method of bortezomib liposome preparation, comprising the following steps:

[0027] (1) The liposome raw materials are mixed and dissolved in ethanol in the required amount in a round bottom flask, and the molar ratio of the three liposome raw materials is HSPC / cholesterol / DSPE-mPEG2000 (55:40:5);

[0028] (2) Then slowly inject the solvent into the phosphate buffer solution heated to 50°C through a syringe, and keep magnetic stirring until the ethanol is completely removed;

[0029] (3) Then liposome is extruded by 100nm polycarbonate membrane filter membrane, repeats 10 times;

[0030] (4) Dialyze with 12kDaMWCO dialysis membrane with 10mMPBS (pH7.0) for 48h at 25°C to remove ethanol, extralipid acetic acid and mannitol;

[0031] (5) Remote loading of BTZ in liposomes by incubating the liposome formulation with BTZ (400ug / ml) overnight;

[0032] (6) Then, at room temperature, dialyze once against 10 mMPBS (pH7.0) and dialyze three times against sucrose...

Embodiment 2

[0034] (1) The liposome raw materials are mixed and dissolved in ethanol in a required amount in a round bottom flask, and the molar ratio of the three liposome raw materials is HSPC / cholesterol / DSPE-mPEG2000 (50:45:6);

[0035] (2) Then slowly inject the solvent into the phosphate buffer solution heated to 55°C through a syringe, and keep magnetic stirring until the ethanol is completely removed;

[0036] (3) then liposome is extruded by 90nm polycarbonate membrane filter membrane, repeats 8 times;

[0037] (4) Dialyze with 14kDaMWCO dialysis membrane with 10mMPBS (pH7.0) at 30°C for 45h to remove ethanol, extralipid acetic acid and mannitol;

[0038] (5) Remote loading of BTZ in liposomes by incubating the liposome formulation with BTZ (350ug / ml) overnight;

[0039] (6) Then, at room temperature, dialyze once against 10 mMPBS (pH7.0) and dialyze three times against sucrose / phosphate buffer (9.5% sucrose, phosphate 10 mm; pH7.0) to remove free BTZ.

[0040] performance chec...

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Abstract

The invention discloses a preparation method of a bortezomib liposome preparation, which comprises the following steps: by taking hydrogenated soybean lecithin (HSPC), cholesterol and distearic acid phosphatidyl ethanolamine-polyethylene glycol (DSPE-mPEG2000) as raw materials, preparing liposome by an ethanol injection method, extruding the liposome through a polycarbonate membrane filter membrane to reduce the particle size of the liposome, removing ethanol, acetic acid and mannitol through dialysis, and incubating the liposome preparation and bortezomib (BTZ) overnight to obtain the bortezomib liposome preparation. An ethanol injection method is adopted to prepare the liposome, the operation is simple and convenient, two hydroxyl groups of mannitol in the liposome can be subjected to a covalent reaction with boric acid of BTZ, so that the BTZ encapsulation efficiency in the liposome preparation is improved, and the liposome is extruded through a 100 nm polycarbonate film filter membrane to reduce the particle size of the liposome.

Description

technical field [0001] The invention relates to the field of drug carriers, in particular to a preparation method of bortezomib liposome preparation. Background technique [0002] Bortezomib (BTZ) is a proteasome inhibitor, and its application in multiple myeloma (Multiplemyeloma, MM) can prolong the median survival period of MM from 3-5 years to 5-7 years. BTZ has become a class I recommended drug for the treatment of newly diagnosed multiple myeloma (Newlydiagnosed multiple myeloma, NDMM). However, adverse reactions such as peripheral neuropathy caused by BTZ seriously affect the survival and prognosis of patients. Since BTZ toxicity is caused by nonspecific interactions between BTZ and plasma proteins, it can be overcome by producing BTZ liposomes. Making liposome BTZ is an effective way to reduce the side effects of its medicine. [0003] Liposomes (or lipid bilayer vesicles) are round vesicles composed of concentric ordered lipid bilayers that encapsulate an aqueous ...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61K38/05A61K9/127A61K47/24A61K47/26A61K47/12A61P35/00
CPCA61K31/69A61K38/05A61K9/127A61K9/1277A61K47/24A61K47/26A61K47/12A61P35/00
Inventor 陈宝安周芳李新松王韬张浩张一周卢琨刘爽
Owner SOUTHEAST UNIV
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