Liposomal formulation of mitoxantrone

A technology of liposome preparation and mitoxantrone, which is applied in liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of toxicity limiting dose, limiting efficacy, etc.

Inactive Publication Date: 2004-01-21
NEOPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Toxicity of mitoxantrone limits dose of drug that can be given to patients
Furthermore, the development of broad-spectrum resistance in cells exposed to mitoxantrone limits its efficacy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] This example represents a liposomal mitoxantrone formulation. Mitoxantrone (3 μmol) was dissolved in chloroform together with cardiolipin (3 μmol). To this mitoxantrone mixture was added phosphatidylcholine (14 μmol) in hexane and 10 μmol cholesterol in chloroform with stirring. The solvent is evaporated in vacuo at or below about 30°C to obtain a thin dry lipid film and a dry lipid film of the drug. Liposomes were formed by adding 2.5 ml saline solution and mixing the ingredients vigorously, eg by vortexing. The flask was then vortexed to obtain multilamellar liposomes or sonicated to obtain unilamellar liposomes. Example 2

Embodiment 2

[0038] This example shows the preparation method of another liposomal mitoxantrone formulation. A solution of approximately 6 [mu]M mitoxantrone, 6 [mu]M cardiolipin, 28 [mu]M phosphatidylcholine and 20 [mu]M cholesterol is prepared in a suitable solvent and the solvent is evaporated. Dried lipid / drug films were dispersed in 7% trehalose in saline solution. The mixture was vortexed and sonicated. The liposomes are then dialyzed if necessary. The encapsulation rate of mitoxantrone was 80% or more as determined by HPLC. Example 3

Embodiment 3

[0039] This example shows the preparation method of another liposomal mitoxantrone formulation. Mitoxantrone was entrapped in liposomes by using 3 μM drug, 15 μM dipalmitoylphosphatidylcholine, 1 μM cardiolipin and 9 μM cholesterol in a volume of 2.5 ml. Evaporate the drug and lipid mixture in vacuo and resuspend it in an equal volume of saline solution. Liposomes were prepared as described in Example 1. In this system, the encapsulation efficiency of mitoxantrone was higher than 80%. Example 4

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Abstract

This invention pertains to liposomal formulations of mitoxantrone and methods for their manufacture and use. The compositions of the present invention include liposomal formulations of mitoxantrone in which the liposome contains any of a variety of neutral or charged liposome-forming materials in addition to a compound that is thought to bind mitoxantrone, such as cardiolipin. The liposomal compositions can be used advantageously in conjunction with secondary therapeutic agents other than mitoxantrone, including antineoplastic, antifungal, antibiotic among other active agents. Methods are provided in which a therapeutically effective amount of the formulation is administered to a mammal, such as a human.

Description

technical field [0001] The invention relates to a liposome preparation of mitoxantrone, a preparation method and application thereof. Background technique [0002] Mitoxantrone, especially its hydrochloride form, is a therapeutic agent used in the treatment of cancer and multiple sclerosis. U.S. Food and Drug Administration (FDA) first approved mitoxantrone hydrochloride to be sold in the U.S. as an injection in 1987, and its trade name was Novantrone®. Novantrone® is prepared as a sterile, pyrogen-free dark blue aqueous solution containing an amount equivalent to 2 mg / ml mitoxantrone free base hydrochloride form, and as an inactive component sodium chloride (0.80% w / v), sodium acetate (0.005% w / v) and acetic acid (0.046% w / v). [0003] Novantrone(R) is approved in combination with corticosteroids as early chemotherapy in the treatment of patients with pain associated with advanced hormone resistant prostate cancer. The recommended dose of Novantrone® is 12-14mg / m 2 , ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/133A61K9/19A61K31/136A61K45/06A61K47/22A61K47/28A61K47/44A61P25/00A61P35/00
CPCA61K31/136A61K9/127A61K45/06A61P25/00A61P35/00
Inventor 伊姆兰·艾哈迈德阿奎鲁尔·拉赫曼
Owner NEOPHARM CO LTD
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