Vascular occlusive agent, application thereof and preparation method

A technique for vascular embolizing agent and contrast agent, which is applied in the field of vascular embolizing agent to achieve the effects of high recovery rate, good biodegradability and good biocompatibility

Inactive Publication Date: 2012-11-07
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no relevant patent literature mentioning the use of multivesicular liposomes as embolization agents for interventional therapy

Method used

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  • Vascular occlusive agent, application thereof and preparation method
  • Vascular occlusive agent, application thereof and preparation method
  • Vascular occlusive agent, application thereof and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of multivesicular liposomes is as follows:

[0044] (1) Weigh 41 mg of phosphatidylcholine dimyristate (phase transition temperature: 23°C), 40 mg of cholesterol, 4.86 mg of phosphatidylglycerol distearate (phase transition temperature: 55°C), three 11.25 mg of glyceryl oleate was dissolved in 1 ml of chloroform to form a lipid solution;

[0045] (2) Mix the lipid solution and the first water phase (1ml ultrapure aqueous solution), and emulsify on an ultrasonic cell crusher for 1-3 minutes to form W / O colostrum; the emulsification temperature is 20°C;

[0046] (3) Pour the W / O type colostrum into the second water phase of equal volume (glucose with a mass percentage concentration of 4% and lysine with a concentration of 20mM, and the volume ratio of the two is 1:1). On the cutter, adjust the shearing speed and time to form a W / O / W type double emulsion with an average particle size of 5-40 μm; the emulsification temperature is 35°C;

[0047] (4) Redispe...

Embodiment 2

[0050] Preparation of visualized multivesicular liposomes containing antineoplastic drugs, such as figure 1 Shown:

[0051] (1) Weigh 41mg hydrogenated soybean lecithin (phase transition temperature 50°C), 40mg cholesterol, 4.86mg dipalmitate phosphatidylglyceride (phase transition temperature 40°C) and 11.25mg tripalmitin in proportion Dissolve in 1ml of chloroform to form lipid solution;

[0052] (2) 320 mg of contrast agent iohexol and 1 mg of antineoplastic drug doxorubicin were dissolved in 1 ml of ultrapure water to form the first aqueous phase (aqueous drug solution);

[0053] (3) Mix the lipid solution and the aqueous solution, and emulsify on an ultrasonic cell crusher for 1 to 3 minutes to form W / O colostrum; the emulsification temperature is 37°C;

[0054] (4) Pour the W / O type colostrum into the second water phase of equal volume (glucose with a mass percentage concentration of 4% and lysine with a mass percentage of 20mM, the volume ratio of the two is 1:1), and...

Embodiment 3

[0059] Preparation of visualized multivesicular liposomes containing antineoplastic drugs, such as figure 1 Shown:

[0060] (1) Weigh 35.23mg dipalmitate phosphatidylcholine (phase transition temperature: 40°C), 29.1mg cholesterol, and 7.9mg dipalmitate phosphatidylglyceride (phase transition temperature: 23°C) in proportion 30.96 mg of glyceryl trioleate was dissolved in 1 ml of chloroform to form a lipid solution;

[0061] (2) Dissolve 320mg of iodofluhydrin as a contrast agent and 100mg of gemcitabine as an antineoplastic drug in 1ml of ultrapure water to form the first aqueous phase (aqueous drug solution);

[0062] (3) Mix the lipid solution and the aqueous solution, and emulsify on an ultrasonic cell crusher for 1 to 3 minutes to form W / O colostrum; the emulsification temperature is 37°C;

[0063] (4) Pour the W / O colostrum into an equal volume of the second aqueous phase (10% glucose by mass and 50mM lysine, the volume ratio of the two is 1:2). On the high-speed shea...

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Abstract

The invention discloses a vascular occlusive agent, application thereof and a preparation method. The vascular occlusive agent is a multivesicular liposome formed by accumulating non-concentric cells, the cells are connected with one another through lipid membranes and are externally coated by lipid membranes with proper surface areas, the multivesicular liposome can be scattered into single liposomes at a vascular embolization position, the particle size of the multivesicular liposome ranges from 5 micrometers and 100 micrometers, and a contrast agent, an antitumor drug or combination of the contrast agent and the antitumor drug can be wrapped in the multivesicular liposome. The occlusive agent wrapping the contrast agent and the antitumor drug simultaneously has the functions of embolization, development and tumor resistance and can be used for realizing target vascular embolization in interventional therapy, the developable multivesicular liposome containing the antitumor drug can be directionally deposited in a tumor blood supply vessel by the aid of transcatheter arterial chemoembolization, peripheral vascular embolization is realized as the cells are gradually disintegrated, and CT (computerized tomography) development at the embolization position can be realized.

Description

technical field [0001] The invention relates to a blood vessel embolism agent and its application and preparation method. Background technique [0002] Transcatheter arterial chemoembolization (TACE) is an effective local treatment method in the non-surgical treatment of liver cancer, and it is also an important means of adjuvant treatment before surgery, which can effectively prolong the survival period. At present, in the clinical application of TACE, the commonly used drug loading method of embolic preparations is simply mixing. Tumors with rich blood supply are uncontrollable due to the complexity of the tumor vascular structure and the impact of blood flow; the water-in-oil emulsion of water-soluble drugs will reverse the liquid phase after entering the blood, and the drugs will quickly enter the body fluid; The process of precipitation in the phase is also extremely unstable; the above-mentioned processes all easily cause a large amount of drug loss, fail to reach the...

Claims

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Application Information

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IPC IPC(8): A61L31/14A61L31/16A61L31/18
Inventor 徐宇虹魏晓慧唐海玲陈群力
Owner SHANGHAI JIAO TONG UNIV
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