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Preparation method and application of 2-methoxyestradiol albumin nano freeze-dried agent

A nanotechnology of methoxyestradiol and albumin, which is applied in the field of medicine, can solve the problems of affecting the therapeutic effect of 2-ME, strong liver first-pass metabolism, irregular oral absorption, etc., and achieves strong targeting and effective Fast, less toxic and side effects

Inactive Publication Date: 2015-04-29
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] There are still many problems in the actual clinical application of 2-ME, such as low solubility of the drug, irregular oral absorption, strong first-pass metabolism in the liver, short half-life, low bioavailability, etc., which greatly affect the therapeutic effect of 2-ME

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  • Preparation method and application of 2-methoxyestradiol albumin nano freeze-dried agent

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Embodiment 1

[0025] In the specific implementation of the present invention, it is realized by the following method, 2-methoxyestradiol is dissolved in absolute ethanol to make a concentration of solution A of 1 mg / ml, and bovine serum albumin is dissolved in ultrapure water , to make a bovine serum albumin aqueous solution B with a concentration of 20mg / ml, 30mg / ml, 50mg / ml, and 60mg / ml, adjust the pH of solution B to 9 with 0.1mol / L NaOH solution, and add to solution B Add the surfactant Tween-20 of 1 / 5000 of the weight of the solution B to the solution B, stir at a speed of 80r / min, after stirring for 5 minutes, use a constant flow pump to control the flow rate of the solution A to be 1ml / min and add it to the solution B. The volume ratio of solution A and solution B is 2:1 to form a mixed solution C, slowly add an aqueous glutaraldehyde solution with a mass concentration of 8% in the mixed solution C, and mix solution C with a mass concentration of 8% glutaraldehyde The volume ratio of...

Embodiment 2

[0027] When the present invention is implemented, it can also be realized by the following method. Get 2-methoxyestradiol and dissolve it in ethanol, and be mixed with a concentration of 1mg / ml, 2mg / ml, 4mg / ml, 5mg / ml. - The ethanol solution of methoxyestradiol, take bovine serum albumin and dissolve it in ultrapure water to make an albumin aqueous solution with a concentration of 30 mg / ml, fully dissolve it by ultrasonic waves, and dissolve the albumin with 0.1mol / L NaOH solution The solution was adjusted to a pH of 9, and a surfactant PEG-200 with a weight of 1 / 2000 of the albumin aqueous solution was added to the albumin aqueous solution, stirred at a speed of 80 r / min, and after stirring for 5 minutes, the 2-methoxyestradiol The ethanol solution of diol is added in the albumin aqueous solution at a flow rate of 1ml / min with a constant flow pump, and the volume ratio of the ethanol solution of 2-methoxyestradiol and the albumin aqueous solution is 3: 1 to form a mixed soluti...

Embodiment 3

[0029] The present invention can also be realized by the following method when the present invention is implemented: get 2-methoxyestradiol and dissolve it in ethanol, and be mixed with a concentration of 3mg / ml, 4mg / ml of a kind of 2-methoxyestradiol Ethanol solution, take bovine serum albumin and dissolve it in ultrapure water to make an albumin aqueous solution with a concentration of 50mg / ml, dissolve it fully by ultrasonic, adjust the albumin solution to pH 9 with 0.1mol / L NaOH solution, and Add surfactant poloxamer and PEG-400 of 1 / 3000 weight of albumin aqueous solution to the albumin aqueous solution, the mass ratio of poloxamer and PEG-400 is 1:1, and stir at a speed of 80r / min , after stirring for 5 minutes, the ethanol solution of 2-methoxyestradiol was added to the albumin aqueous solution with a constant flow pump to control the flow rate of 1ml / min, the ethanol solution of 2-methoxyestradiol and the albumin aqueous solution The volume ratio is 2.5: 1 to form a mi...

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Abstract

The invention relates to a preparation method and an application of a 2-methoxyestradiol albumin nano freeze-dried agent, and effectively solves the problems in preparation of the 2-methoxyestradiol albumin nano freeze-dried agent and application of the freeze-dried agent to preparation of medicines for treating tumors. The method comprises the following steps: dissolving 2-methoxyestradiol albumin in an organic solvent-absolute ethanol to prepare a solution A; dissolving bovine serum albumin in ultra-pure water to prepare a solution B, adding a surfactant, and adjusting the pH value to be 8-10 by an NaOH solution; adding the solution A into the solution B to prepare a mixed solution C; adding glutaraldehyde into the mixed solution C, stirring evenly, standing and solidifying; performing rotary evaporation to remove the organic solvent to prepare a nano solution D; adding a freeze-drying protective agent into the nano solution D, and performing freeze-drying to prepare the 2-methoxyestradiol albumin nano freeze-dried agent. The 2-methoxyestradiol albumin nano freeze-dried agent is simple in method, easy to produce and prepare, good in stability, long in medicine effect, high in targeting property, rapid in acting, small in negative effect, low in administration frequency, high in bioavailability and simple to prepare; the medicines can be protected from being affected by an environment.

Description

technical field [0001] The invention relates to medicine, in particular to a preparation method and application of 2-methoxyestradiol albumin nano freeze-dried agent. Background technique [0002] 2-methoxyestradiol (2-methoxyestradiol, 2-ME) is a natural metabolite of estradiol found in the human body during the study of estrogen metabolism in the 1970s. It is a new type of hormone anti-tumor drug. Recently, studies on its pharmacological effects have shown that 2-ME can induce apoptosis of endothelial cells, disturb the formation of microvessels, and inhibit the formation of new blood vessels, so it is a better inhibitor of new blood vessel formation. Further studies have shown that it has a good inhibitory effect on various tumors in vivo and in vitro, and has been used in the treatment of multiple myeloma, prostate cancer and breast cancer. At the same time, the compound does not depend on estrogen receptors and has no estrogen effect. At present, the research of 2-ME o...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/565A61K47/42A61P35/00
Inventor 张楠王培张振中徐霞郭晓静鲁春云侯瑞瑞李佳张红岭夏亚丹王维嘉陈燕牛利锋高书林
Owner ZHENGZHOU UNIV
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