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Nano diagnosis and treatment agent, preparation method and application thereof

A nanometer and nanoparticle technology, applied in the direction of nanotechnology, nano optics, nanotechnology, etc., can solve the problems of low drug loading, polymer structure hindering transformation, and premature release of drugs, etc.

Pending Publication Date: 2021-03-12
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the developed systems often face the problems of low drug loading and premature drug release, and the complexity of their polymer structures may hinder their further clinical translation

Method used

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  • Nano diagnosis and treatment agent, preparation method and application thereof
  • Nano diagnosis and treatment agent, preparation method and application thereof
  • Nano diagnosis and treatment agent, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Synthesis and Characterization of a Reactive Oxygen Responsive Heterodimeric Prodrug

[0047] First, the heterodimeric prodrug HRC was synthesized from commercially available CPT and HPPH via a two-step reaction route. in BF 3 Et 2 Under the catalysis of O (110mmol, 13ml), the precursor of compound 1 was synthesized by condensation of methyl thioglycolate (70mmol, 6.26ml) and acetone (34mmol, 2.55ml) (yield: 90%). 1 H NMR (300 MHz, MeOD) 3.718 (6H, s), 3.463 (4H, s), 1.603 (6H, s). The precursor of compound 1 (1 g) was dissolved in anhydrous tetrahydrofuran (150 mL) and cooled in an ice-water bath, then LiAlH 4 (1.52 g, 40.1 mmol) was slowly added to the reaction mixture. After 30 minutes, the mixture was slowly heated to reflux for 2 hours. Water (1 mL) was then added to quench the reaction. The mixture was filtered and the solvent in the filtrate was evaporated by rotary evaporator. Purification by silica column chromatography gave Compound 1 as a yellow liquid...

Embodiment 2

[0050] Preparation and Characterization of Nanotherapeutic Agents Based on Heterodimer Prodrugs

[0051] By nanoprecipitation method, dissolve HRC and F127 in a small amount of DMSO, and then add appropriate amount of water, then spontaneously form nanoparticles HRC@F127 nanoparticles, at the feed weight ratio of HRC:F127=0.2, the nanoparticles have about Hydrated particle size of 23nm ( figure 2 ), the resulting nanoparticles have high loading efficiencies exceeding 95%. When the feed ratio was changed to 0.1 or 0.4, nanoparticles with similar sizes were obtained. The obtained HRC@F127 nanoparticles were stable, and no obvious precipitation and obvious size change were found after one week. In contrast, CPT@F127 nanoparticles obtained by the same method had a size larger than 200 nm and were unstable, with precipitation occurring within hours. At the same time, the drug-loading efficiencies of CPT and HPPH are only 55% to 76%. We further investigated the drug release fro...

Embodiment 3

[0055] Nanotherapeutics for selective cancer cell imaging and treatment

[0056] Two cell lines, cancer cells (HCT116 cells) with high endogenous reactive oxygen species levels and normal cells with high endogenous reactive oxygen species levels (mouse fibroblast cell line L929) were selected for the experiment. Fluorescent imaging analysis was performed after HRC@F127 was incubated with cells for 24 hours. like image 3 As shown, the results showed that under the same incubation time, HCT116 cells showed higher fluorescence intensity than L929, indicating that HRC@F127 was activated and released more HPPH under the action of higher ROS levels in cancer cells, producing Stronger fluorescence.

[0057] At the same time, the results of experiments evaluating cell viability by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) method showed that ( Figure 4 ), in the absence of light, HRC@F127 showed higher cytotoxicity to HCT116 cells with high ROS levels: at a co...

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Abstract

The invention discloses a nano diagnosis and treatment agent, a preparation method and application thereof, wherein the nano diagnosis and treatment agent comprises nano particles, and the nano particles comprise an inner core of a small molecular prodrug responsive to active oxygen, and a shell formed by coating the surface of the inner core with an amphiphilic polymer. The nano diagnosis and treatment agent is formed by depositing a small molecular prodrug and an amphiphilic polymer in water, and nano particles are simple in component and good in stability, have tumor response imaging and treatment effects and have good application prospects in the field of tumor diagnosis and treatment.

Description

technical field [0001] The invention relates to the field of medical nano-materials, in particular to a nano-diagnostic agent and its preparation method and application. Background technique [0002] Cancer treatment has come a long way in the past few decades. The realization of precision medicine in the future is an important development trend of cancer treatment, but it is still challenging to achieve this goal. The current main method of cancer treatment is still conservative chemotherapy, but this method usually has problems such as rapid blood clearance, drug resistance and serious side effects. In order to alleviate side effects and improve the therapeutic selectivity of cancer cells, the concept of prodrugs has been proposed. Prodrugs usually refer to those compounds that can release active drugs through enzymatic or non-enzymatic stimulation in vivo and exert their medicinal effects. Less active. [0003] At present, in the common design of prodrugs, the active ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K41/00A61K47/55A61K49/00A61P35/00A61P35/02B82Y5/00B82Y20/00B82Y30/00B82Y40/00A61K31/4745
CPCA61K41/0071A61K47/55A61K9/5146A61K9/0019B82Y5/00B82Y30/00B82Y40/00B82Y20/00A61P35/00A61P35/02A61K31/4745A61K49/0021A61K49/0093
Inventor 黄鹏江美娟林静陈小元
Owner SHENZHEN UNIV
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