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A kind of preparation method of halloysite nanotube drug carrier and halloysite nanotube carrier drug

A halloysite nanotube and nanotube technology, which can be used in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc. The effect of reducing serious toxic and side effects and avoiding drug leakage

Inactive Publication Date: 2020-05-19
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] In recent years, cancer has become one of the main causes of human death "Global Cancer Report 2014", but the current clinical anticancer drugs generally have shortcomings such as low selectivity, large toxic and side effects, and short half-life

Method used

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  • A kind of preparation method of halloysite nanotube drug carrier and halloysite nanotube carrier drug
  • A kind of preparation method of halloysite nanotube drug carrier and halloysite nanotube carrier drug
  • A kind of preparation method of halloysite nanotube drug carrier and halloysite nanotube carrier drug

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Experimental program
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Effect test

Embodiment 1

[0060] (1) Thiolation modification of halloysite nanotubes

[0061] Ultrasonic dispersion of 5.0g of halloysite powder in 50ml of hydrochloric acid solution with a mass fraction of 25%, magnetic stirring at 70°C for 2h, centrifugation and washing with a large amount of distilled water until pH 6-7, vacuum drying at 100°C, grinding and passing through 100 mesh Sieve and collect for later use. 2.0 g of the purified halloysite powder was ultrasonically dispersed in 100 ml of anhydrous toluene, 20 ml of 3-mercaptopropyltrimethoxysilane was added dropwise, and the mixture was refluxed for 24 hours at 120° C. under the protection of argon. After cooling to room temperature, it was centrifuged, washed several times with anhydrous toluene and absolute ethanol, and dried under vacuum at 60°C to obtain thiolated halloysite nanotubes (HNTs-SH), see image 3 .

[0062] (2) Synthesis of mercapto oligosaccharide-folic acid

[0063] Take 1g of chitosan oligosaccharide (COS), 1g of element...

Embodiment 2

[0074] (1), (2) step with embodiment 1.

[0075] (3) Loading and drug loading test of anticancer drugs

[0076] 300mg of mercapto halloysite powder was ultrasonically dispersed in 10ml of 5-fluorouracil (5-FU) PBS solution with a concentration of 3mg / ml, vacuumed several times, and the air in the system was exhausted as much as possible, and stirred for 48 hours in the dark. Keep vacuuming to make 5-fluorouracil loaded into the inner cavity of the halloysite nanotube as much as possible. After the reaction was completed, it was centrifuged and washed several times with PBS, and the supernatant was collected to test the ultraviolet absorption of 5-fluorouracil at 266 nm, and the drug loading was calculated to be 6.7% according to the standard curve of 5-fluorouracil. After drying, the 5-fluorouracil-loaded halloysite powder was obtained, described as 5-FU@HNTs-SH.

[0077] (4) Assembly of multifunctional halloysite nanotube drug-loading system

[0078] The halloysite powder ...

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Abstract

The invention discloses an indianite nano-tube medicine carrier and a method for preparing indianite nano-tube carrier medicines. A plurality of mercapto chitosan oligosaccharide-folic acid molecular chains are combined with the surfaces of mercapto-modified indianite nano-tubes by disulfide bonds in a wrapping manner to obtain the indianite nano-tube medicine carrier. The indianite nano-tube medicine carrier and the method have the advantages that the structures of the indianite nano-tube medicine carrier are innovated, mercapto chitosan oligosaccharide chains with a plurality of folic acid targeting molecules are combined with the surfaces of the indianite nano-tubes in the wrapping manner, anticancer medicines can be loaded in mercapto-substituted indianite inner cavities, the mercapto chitosan oligosaccharide chains are combined with the surfaces of the indianite nano-tubes in the wrapping manner, accordingly, leakage of the medicines can be prevented as much as possible, and the targeting efficiency further can be enhanced by the multiple folic acid targeting molecules combined with the outsides of the indianite nano-tubes; chitosan oligosaccharide chains can be removed by the aid of glutathione breakage disulfide bonds which are reducing agents in tumor cells, and accordingly medicine release can be controlled; multifunctional indianite nano-tube medicine carrying systems with integrated targeting and stimulating responsiveness are assembled, accordingly, severe toxic and side effects of the anticancer medicines can be effectively reduced, and effects of recognizing the tumor cells in a targeting manner and controlling medicine release can be realized.

Description

technical field [0001] The invention belongs to the field of targeted controlled release drug nanomaterials, and in particular relates to a multifunctional halloysite nanotube drug loading system, a preparation method and research on controlled release performance. Background technique [0002] In recent years, cancer has become one of the main causes of human death "Global Cancer Report 2014", but the current clinical anticancer drugs generally have shortcomings such as low selectivity, large toxic and side effects, and short half-life. [0003] Studies have found that folic acid receptors on the surface of tumor cells are overexpressed, much higher than normal cells, and folic acid is a basic component of cell metabolism, DNA synthesis and repair, and the rapid growth of tumor cells requires sufficient folic acid to maintain DNA synthesis. How to make full use of the targeting effect of folic acid to maximize the delivery of anticancer drugs to the tumor site and stimulate...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K47/02A61K31/704A61K31/513A61P35/00
CPCA61K31/513A61K31/704A61K47/02A61K47/36
Inventor 钟世安胡雨薇吴瀚顾皓陈建李秀芳孙燕华黄燊李雨晴刘慧许江峰李建兵任涛
Owner CENT SOUTH UNIV