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Targeted nano diagnosis and treatment agent with glutathione activation based on light click reaction strategy as well as preparation method and application of targeted nano diagnosis and treatment agent

A light click reaction and glutathione technology, applied in the field of biomedicine, can solve problems such as drug leakage and rapid metabolism

Pending Publication Date: 2022-04-05
南方医科大学皮肤病医院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although these systems are beneficial to increase the effective dose of drugs at the lesion site and alleviate the side effects of drugs, hydrophilic drugs such as rifampin often suffer from drug leakage and rapid metabolism, making the development of nano-delivery systems still a long way to go
In particular, most of the current delivery systems lack the functions of image tracing diagnosis and treatment monitoring of tuberculosis lesions, making the diagnosis and treatment of tuberculosis still a challenging scientific topic

Method used

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  • Targeted nano diagnosis and treatment agent with glutathione activation based on light click reaction strategy as well as preparation method and application of targeted nano diagnosis and treatment agent
  • Targeted nano diagnosis and treatment agent with glutathione activation based on light click reaction strategy as well as preparation method and application of targeted nano diagnosis and treatment agent
  • Targeted nano diagnosis and treatment agent with glutathione activation based on light click reaction strategy as well as preparation method and application of targeted nano diagnosis and treatment agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: Synthesis of RIF@HA-NG, RIF@Cy5.5-HA-NG nanoparticles

[0043] (1) Synthesis of HA-Cys-MA, a macromolecular monomer HA-Cys-MA with a photo-click reaction group and a double bond group Methacryloyl (MA) and glutathione-responsive cysteine ​​Cysteine ​​(Cys), which has a photo-click reaction The polymer monomer HA-Lys-Tet of the group Tetrazolium (Tet) and Lysine (Lys);

[0044] The specific steps of synthesizing HA-Cys-MA:

[0045] Such as figure 1 As shown, first di-tert-butyl dicarbonate (Boc 2 O, DiBoc) and NH 2 -Cys-NH 2 Co-dissolved in dimethylformamide and reacted at room temperature, di-tert-butyl dicarbonate (Boc 2 O) and NH 2 -Cys-NH 2 The molar ratio is 1.0:1.0, and the reaction time is 6 hours; the amino group at one end is protected to obtain Boc-Cys-NH 2 .

[0046] Methacryloyl chloride and Boc-Cys-NH 2 Reaction at room temperature in anhydrous dichloromethane to generate Boc-Cys-MA, methacryloyl chloride and Boc-Cys-NH 2 The molar r...

Embodiment 2

[0053] Embodiment 2: Characterization of RIF@HA-NG, RIF@Cy5.5-HA-NG nanoparticles

[0054] Particle size and potential characterization: The particle size distribution and zeta potential of RIF@HA-NG were measured with a dynamic light scattering analyzer (DLS).

[0055] Morphology analysis: The morphology of RIF@Cy5.5-HA-NG was characterized by TEM.

[0056] Determination of drug release rate: The drug release efficiency of RIF@Cy5.5-HA-NG with or without GSH was measured by mass spectrometry.

[0057] Such as image 3 As shown in A, it was found that the average particle size of RIF-loaded HA-NG was about 100 nm.

[0058] At the same time, if image 3 As shown in B, the zeta potential was measured, and it was found that the zeta potential was -27.5mV and -32.5mV before and after loading RIF, indicating that the nanoparticle RIF@HA-NG has good stability.

[0059] Such as image 3 The TEM results of C show that the nanoparticles RIF@Cy5.5-HA-NG are spherical particles with...

Embodiment 3

[0061] Embodiment 3: Determination of targeting ability of RIF@Cy5.5-HA-NG nanoparticles

[0062] In order to be able to perform image tracing in vivo and in vitro later, the nano-therapeutic agent RIF@HA-NG is functionally modified, and the fluorescent dye Cy5.5 is linked to the surface of the nano-therapeutic agent RIF@HA-NG through a chemical bond to obtain the nano-therapeutic agent RIF@ Cy5.5-HA-NG. In this example, confocal laser microscopy was used to evaluate the targeting ability of RIF@Cy5.5-HA-NG.

[0063] In this example, macrophages containing Mycobacterium tuberculosis were used for experiments, and three experimental groups were set up: the control group, the Cy5.5 group and the RIF@Cy5.5-HA-NG group, and PBS and Cy5.5 were added according to the grouping requirements. 5 (final concentration 10 μM), RIF@Cy5.5-HA-NG (final concentration 10 μM), respectively co-incubated with macrophages containing Mycobacterium tuberculosis for 1 h, then washed 3 times with PBS,...

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Abstract

The invention discloses a targeted nano diagnosis and treatment agent based on a light click reaction strategy and having glutathione activation characteristics as well as a preparation method and application of the targeted nano diagnosis and treatment agent. The preparation method comprises the following steps: synthesizing a macromolecular monomer HA-Cys-MA and a macromolecular monomer HA-Lys-Tet; a high-molecular monomer HA-Cys-MA, a high-molecular monomer HA-Lys-Tet and rifampicin are subjected to a light click biological orthogonal reaction to form the nano diagnosis and treatment agent RIF (at) HA-NG; the dye Cy5.5 is modified to the nano diagnosis and treatment agent RIF (at) HA-NG through an amidation reaction, and the nano diagnosis and treatment agent RIF (at) Cy5.5-HA-NG with the image tracing capacity is obtained. The invention has the following advantages: a biocompatible and multifunctional composite nano diagnosis and treatment agent containing hyaluronic acid, rifampicin, even Cy5.5 and other functional components is constructed, and it is verified that the composite nano diagnosis and treatment agent can be used as an effective mycobacterium tuberculosis targeting nano material and is used for targeted chemotherapy of tuberculosis.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a tuberculosis drug. Background technique [0002] Tuberculosis (TB) is highly contagious and has been a major global public health problem. This chronic disease is caused by Mycobacterium Tuberculosis (M.tb) and most commonly affects the lungs. At present, surgery combined with multiple anti-tuberculosis drugs is the routine treatment for tuberculosis. Although drugs such as rifampicin (RIF) and isoniazid have been used as the first choice of clinical anti-tuberculosis drugs because of their good therapeutic effect and reasonable price, the short half-life of these chemotherapy drugs in the body and the unavoidable side effects are increasingly The outstanding problems have brought a lot of suffering to patients, and have received great attention from clinical medical researchers and scholars in the field of basic scientific research. Therefore, designing and developing ef...

Claims

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Application Information

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IPC IPC(8): A61K49/00
Inventor 廖玉辉郑举敦陈晓东伍启康杨荣华黄佳林王胜男林伟强
Owner 南方医科大学皮肤病医院
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