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Preparation method and applications of gambogic acid self-assembled polymer nanoparticles

A technology of gambogic acid and self-assembly, applied in the field of medicine and chemical industry, can solve the problems of poor stability, low drug loading, low encapsulation rate, etc., and achieve good stability, good biocompatibility, and high encapsulation rate. Effect

Active Publication Date: 2016-07-27
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of the present invention is to overcome the shortcomings of existing gambogic acid preparations such as poor stability, low encapsulation efficiency and low drug loading, and provide a high encapsulation efficiency, high drug loading, stable gambogic acid self-assembly polymerization Preparation method and application of nanoparticle

Method used

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  • Preparation method and applications of gambogic acid self-assembled polymer nanoparticles
  • Preparation method and applications of gambogic acid self-assembled polymer nanoparticles
  • Preparation method and applications of gambogic acid self-assembled polymer nanoparticles

Examples

Experimental program
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Effect test

Embodiment 1

[0026] The preparation method of embodiment 1 gambogic acid self-assembled polymer nanoparticle

[0027] The preparation method is as follows:

[0028] 1) Polymer material preparation: 0.04mol polyethylene glycol 6000, 0.001mol ε-caprolactone, 0.0001mol stannous octoate and 5ml toluene were added to a three-necked bottle, stirred under mechanical stirring and N 2 Under protection, react in an oil bath at 130°C for 12 hours; after the reaction, the reaction product is naturally cooled to room temperature, and the toluene is spun out; the product is dissolved in dichloromethane, and after the product is completely dissolved, it is slowly dropped into a large amount of cold petroleum ether. Precipitate, filter with suction, dissolve the precipitate with dichloromethane, slowly drop into petroleum ether, repeat the operation, and filter to obtain a white product, which is vacuum-dried at 40°C to obtain a polymer material.

[0029] 2) Put 40mg of gambogic acid into eggplant-shaped...

Embodiment 2

[0033] The preparation of embodiment 2 gambogic acid self-assembled polymer nanoparticles

[0034] The method is the same as in Example 1, the ultrasonic power is selected to be 315W, but the number of ultrasonic waves is changed to 1 time, 2 times, 3 times, 4 times, 5 times, 6 times, and each time is 2 minutes, and the gambogic acid self-assembled polymer nanoparticles are measured The particle size, PDI, encapsulation efficiency, and drug loading are shown in Table 2.

[0035] Table 2

[0036]

[0037] It can be seen from Table 2 that when the ultrasonic time is increased from 2 min to 4 min, the encapsulation efficiency and drug loading are the highest. Continuing to increase the ultrasonic time, the encapsulation efficiency decreased instead. Moreover, if the ultrasonic time is too long, the polymer skeleton will be broken, the particles will be broken, the solution will be unstable, and some coagulation will occur. Therefore, the optimal time is 4 minutes.

Embodiment 3

[0038] The preparation of embodiment 3 gambogic acid self-assembled polymer nanoparticles

[0039] The method is the same as in Example 1, the ultrasonic power is selected to be 315W, and the hydration time is changed to 2h, 4h, 6h, and 8h respectively, and the particle size, PDI, encapsulation efficiency, and drug loading of gambogic acid self-assembled polymer nanoparticles are measured As in Table 3.

[0040] table 3

[0041]

[0042] As can be seen in Table 3, the hydration time increased from 2h to 8h. At 4h, the encapsulation efficiency and drug loading reached the highest, and the hydration time was 4h.

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Abstract

The invention relates to a preparation method and applications of gambogic acid self-assembled polymer nanoparticles. The preparation method comprises the following steps: adding polyethylene glycol, epsilon-caprolactone, stannous octoate and methylbenzene into a three-necked bottle, and carrying out oil bath reaction at 130 DEG C for 12h under the stirring state and under the protection of N2; after the reaction, removing methylbenzene through rotary evaporation; dissolving the product by adopting dichloromethane, slowly dropwise adding the obtained solution into plenty of cold petroleum ether for precipitation, operating repeatedly, and carrying out suction filtration to obtain a polymer material; taking gambogic acid, placing gambogic acid into an eggplant-shaped bottle, adding acetonitrile for dissolving gambogic acid, adding the polymer material into the obtained solution for dissolving, removing acetonitrile through rotary evaporation, after removing of acetonitrile, a layer of medicinal film is formed on the wall of the bottle, placing the bottle into a vacuum drying oven, removing trace amount of acetonitrile, adding purified water into the bottle, carrying out hydration treatment under 65 DEG C, placing the obtained solution into an ice-water bath, carrying out ultrasound treatment for twice under the power of 315W, wherein each time of ultrasound treatment lasts for 2 min, and after the ultrasound treatment, filtering the obtained solution by a 0.45 [mu] m filter membrane. The prepared nanoparticles are high in encapsulation efficiency, high in drug loading capacity, and good in stability.

Description

technical field [0001] The invention relates to a gambogic acid self-assembled polymer nanoparticle with high encapsulation rate and a preparation method and application thereof, which belong to the technical field of medicine and chemical industry. Background technique [0002] Gambogic acid (gambogicacid, GA) is the main active ingredient of Gambogia, which can selectively induce tumor cell apoptosis, exhibits a wide range of strong anti-tumor effects in vivo and in vitro, and has a relatively strong effect on a variety of tumor cells. Strong inhibitory effect, but no obvious inhibitory effect on normal hematopoietic system and immune function. The anti-tumor mechanism of gambogic acid may be related to blocking cell cycle, inducing apoptosis, inhibiting angiogenesis, binding to transferrin receptor (TfR), and affecting the expression of related genes and proteins. Due to the extremely low solubility of gambogic acid in water (less than 0.5 μg / mL), rapid plasma clearance,...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/34A61K31/352A61P35/00
CPCA61K9/5146A61K31/352
Inventor 陈立江刘宇王芳张国林梁啸王欣李丽张金凤王朝勃
Owner LIAONING UNIVERSITY
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