Nanometer chitosan ultrasonic microbubble targeting prostate cancer cells and preparation and application thereof

A nano-chitosan, ultrasonic microbubble technology, applied in echo/ultrasonic imaging agents, preparations for in vivo tests, medical preparations with non-active ingredients, etc., can solve the problem of low tissue penetration, ultrasonic microbubble targets Low tropism and other problems, to achieve the effect of strong tissue penetration, high tissue targeting, and strong penetration

Active Publication Date: 2017-05-31
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to provide a targeted nano-chitosan with high targeting and strong tissue penetrat...

Method used

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  • Nanometer chitosan ultrasonic microbubble targeting prostate cancer cells and preparation and application thereof
  • Nanometer chitosan ultrasonic microbubble targeting prostate cancer cells and preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] 1) 40 parts by weight of chitosan, 20 parts by weight of methacryloyloxyethyltrimethylammonium chloride, and 20 parts by weight of 3-maleimidopropionic acid hydroxysuccinimide ester are mixed, 60 React at ℃ for 6 hours to obtain quaternized modified chitosan; add 30 parts by weight of prostate-specific antibody PSA antibody (Shanghai Ruiqi Technology Co., Ltd., model Rsm-1625M) to the modified chitosan, add Potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with pH=6.5, make the pH of the system=6.5, and react at 60°C for 4 hours to obtain the chitosan-prostate specific antibody complex;

[0039] 2) Mix 10 parts by weight of dodecafluoropentane, 5 parts by weight of chitosan-prostate specific antibody complex and 10 parts by weight of distilled water, and react for 1.5 hours to form colostrum;

[0040] 3) Add 10 parts by weight of Tween 60 to 40 parts by weight of castor oil and dropwise add 10 parts by weight of n-butanol as the organic phase...

Embodiment 2

[0044] 1) 50 parts by weight of chitosan, 30 parts by weight of methacryloyloxyethyltrimethylammonium chloride, and 20 parts by weight of 3-maleimidopropionic acid hydroxysuccinimide ester are mixed, 60 React at ℃ for 6 hours to obtain quaternized modified chitosan; add 30 parts by weight of prostate specific antibody PSA antibody (Shanghai Ruiqi Technology Co., Ltd., model is Rsm-1625M) to modified chitosan, add Potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with pH=6.5, make the pH of the system=6.5, and react at 60°C for 4 hours to obtain the chitosan-prostate specific antibody complex;

[0045] 2) Mix 40 parts by weight of nitrogen, 10 parts by weight of chitosan-prostate specific antibody complex and 20 parts by weight of distilled water, and react for 1.5 hours to form colostrum;

[0046] 3) Add 10 parts by weight of Tween 60 to 40 parts by weight of castor oil and dropwise add 10 parts by weight of n-butanol as the organic phase, stir evenly...

Embodiment 3

[0050] 1) 60 parts by weight of chitosan, 20 parts by weight of methacryloyloxyethyltrimethylammonium chloride, and 20 parts by weight of 3-maleimidopropionic acid hydroxysuccinimide ester are mixed, 60 Reaction under ℃ for 6 hours, obtains the modified chitosan of quaternization; In modified chitosan, add 30 weight parts prostate-specific antibody PSMA antibody (commercial drug reagent, Shanghai Rui Qi Technology Co., Ltd., model is Rsm- 1625M), adding potassium dihydrogen phosphate-dipotassium hydrogen phosphate buffer solution with pH=6.5, making the pH of the system=6.5, and reacting at 60°C for 4 hours to obtain the chitosan-prostate specific antibody complex;

[0051] 2) Mix 40 parts by weight of octafluoropropane, 5 parts by weight of chitosan-prostate specific antibody complex and 25 parts by weight of distilled water, and react for 1.5 hours to form colostrum;

[0052] 3) Add 10 parts by weight of Tween 60 to 40 parts by weight of castor oil and dropwise add 10 parts ...

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Abstract

The invention belongs to the technical field of medical preparations, and discloses nanometer chitosan ultrasonic microbubble targeting prostate cancer cells and preparation and application thereof. A method comprises the following steps of (1) mixing chitosan, methacryloyloxyethyl trimethyl ammonium chloride and N-succinimidyl 3-maleimidopropionate, and heating to react, so as to obtain modified chitosan; adding a prostate antigen, adjusting the pH (potential of hydrogen) value of a system, and continuing to react, so as to obtain a complex; (2) stirring and mixing an inert matter with low boiling point, the complex and water, so as to obtain primary emulsion; (3) adding a dispersant and an additive into an oil-phase solvent, uniformly mixing, adding the primary emulsion, stirring at high speed, adding a crosslinking agent to cure, adding a precipitating agent to precipitate, washing, centrifuging at high speed, and drying particles, so as to obtain the ultrasonic microbubble. The nanometer chitosan ultrasonic microbubble has the advantages that the targeting property is good, the tissue penetration ability is strong, the affinity is high, and the nanometer chitosan ultrasonic microbubble is suitable for the ultrasonic developing of the prostate cancer cells.

Description

technical field [0001] The invention belongs to the field of medical preparations, and in particular relates to a nano-chitosan ultrasonic microbubble targeting prostate cancer cells, a preparation method and application thereof. Background technique [0002] Ultrasound contrast agents (UCAs) have been continuously developed since Gramiak's first discovery of tiny air bubbles that enhanced ultrasound imaging in 1967, and ultrasound detection techniques have evolved with them. With the development of ultrasound contrast agents, ultrasound contrast agents are no longer limited to ultrasound imaging, but have begun to develop towards drug delivery. Therefore, ultrasound molecular imaging technology based on ultrasound contrast agents combined with drug delivery systems has been developed. It is clinically used in the diagnosis, treatment and evaluation of certain diseases. [0003] At present, nano-microbubbles can enter the extravascular space and perform ultrasound imaging o...

Claims

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Application Information

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IPC IPC(8): A61K49/22A61K9/51A61K47/36A61K47/42A61K47/04A61K47/06A61K47/20A61P35/00
CPCA61K9/5115A61K9/5123A61K9/5161A61K9/5169A61K49/223
Inventor 黄岳山邓惠良劳永华郭圣文黄育铭
Owner SOUTH CHINA UNIV OF TECH
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