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Targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation as well as preparation method and applications thereof

A mesoporous polydopamine, multifunctional technology, applied in the field of biomedical materials, can solve the problems of lack of targeting, achieve the effect of increasing drug loading, easy operation, and improving tumor treatment effect

Active Publication Date: 2019-01-29
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most manganese contrast agents lack targeting in the process of circulation in the body

Method used

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  • Targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation as well as preparation method and applications thereof
  • Targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation as well as preparation method and applications thereof
  • Targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Synthesis of targeted drug carrier MPDA-PEG-FA

[0041] Specific steps are as follows:

[0042] (1) Preparation of MPDA: Dissolve 0.15 g of dopamine and 0.1 g of Puronic F127 in a mixed solvent of 10 mL of water and ethanol, add 0.16 mL of 1,3,5-trimethylbenzene under ultrasonic conditions in a water bath, continue ultrasonication for 2 minutes, add 0.760 mL of ammonia water, stirred for 3 h, centrifuged and washed to obtain MPDA with a particle size of 200±10 nm.

[0043] (2) Synthesis of MPDA-PEG-FA: 2 mg PEG-FA was weighed and dissolved in 1 mL dimethyl sulfoxide, 1 mg MPDA was dissolved in 2 mL ultrapure water, and dimethyl sulfoxide was slowly added dropwise into ultrapure water , adjusted the pH of the mixed solution to 8.5, stirred for 24 h, centrifuged at 5000 rpm for 10 min, washed three times with ultrapure water, and the resulting precipitate was MPDA-PEG-FA, which was resuspended in water.

Embodiment 2

[0044] Example 2 Synthesis of targeted drug carrier MPDA-PEG-FA

[0045] Specific steps are as follows:

[0046] (1) Preparation of MPDA: Dissolve 0.15 g of dopamine hydrochloride and 0.1 g of Pluronic F127 in a mixed solvent of 10 mL of water and ethanol, add 0.16 mL of 1,3,5-trimethylbenzene under ultrasonic conditions in a water bath, continue ultrasonication for 2 min, and add 0.375mL ammonia water, stirred for 2h, centrifuged and washed to obtain MPDA with a particle size of 200±10 nm.

[0047] (2) Synthesis of MPDA-PEG-FA: 5 mg PEG-FA was weighed and dissolved in 1 mL dimethyl sulfoxide, 1 mg MPDA was dissolved in 2 mL ultrapure water, and dimethyl sulfoxide was slowly added dropwise into ultrapure water , adjust the pH of the mixed solution to 9, stir for 24 hours, centrifuge at 5000rpm for 10 minutes, wash twice with ultrapure water, and the resulting precipitate is MPDA-PEG-FA, which is resuspended in PBS (pH 7.4) solution.

Embodiment 3

[0048] Example 3 Synthesis of targeted nano-therapeutic agent RF@MPDA(Mn)-PEG-FA

[0049] Specific steps are as follows:

[0050] (1) Synthesis of MPDA-PEG-FA (Mn): take 1 mg of MPDA-PEG-FA synthesized in Example 1 and resuspend in ultrapure water, add 2 mg of MnSO4 to it, stir for 12 h, centrifuge at 5000 rpm for 10 min, Wash 3 times with ultrapure water, and the obtained precipitate is MPDA(Mn)-PEG-FA.

[0051] (2) Synthesis of RF@MPDA(Mn)-PEG-FA: Dissolve 1 mg MPDA(Mn)-PEG-FA synthesized above in 1 mL THF, 2 mg regorafenib in 1 mL THF, and mix the two , put it still in a vacuum drying oven, and when the volume of the solvent evaporated to 500 μL, take it out and centrifuge it at 4500 rpm for 8 min, and wash it twice with water. 7.4) in solution.

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Abstract

The invention discloses a targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation as well as a preparation method and applications of the targeting mesoporous polydopamine multi-purpose nanometer diagnosis and treatment preparation. The targeting mesoporous polydopamine multi-purse nanometer diagnosis and treatment preparation is composed of a water-soluble folic-acid-targeting mesoporous polydopamine medicine carrier, hydrophobic regorafenib and manganese sulfate, wherein the mass ratio of regorafenib to the folic-acid-targeting mesoporous polydopamine medicine carrier is (0.5-4): 1, and the mass ratio of manganese sulfate to the folic-acid-targeting mesoporous polydopamine medicine carrier is (1-6):1. The targeting mesoporous polydopamine diagnosis and treatment preparation can recognize positive tumor cells of a folic acid receptor, so that a targeting effect is achieved during treatment. For the diagnosis and treatment preparation, the chemotherapy under the guidance of MRI imaging is realized, the tumor treatment effect is expected to be improved, meanwhile, the biocompatibility is good, and therefore, the targeting mesoporous polydopaminemulti-purpose nanometer diagnosis and treatment preparation has the clinical application potential.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a targeted mesoporous polydopamine multifunctional nanometer diagnosis and treatment agent and a preparation method thereof. Background technique [0002] Cancer is one of the major diseases that endanger human health at present. There are about 14 million new cancer patients and about 8.2 million deaths in the world every year. There are about 3.5 million new cases of cancer and about 2.5 million deaths in my country every year. Due to the aging of the social population structure, environmental pollution, and the impact of unhealthy living behaviors such as smoking, the situation of cancer in my country is becoming more and more serious, and the treatment of cancer is facing great challenges. Therefore, the development of diagnostic and therapeutic agents with good biocompatibility and functions of diagnosis, monitoring, and treatment has important clinical appl...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/44A61K47/54A61K49/10A61K49/12A61K49/18A61P35/00
CPCA61K47/545A61K47/6949A61K49/101A61K49/126A61K49/189A61P35/00A61K31/44
Inventor 曹众管青青郭宇郭若汨
Owner SUN YAT SEN UNIV
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