Nanometer medicine loading system, method for preparing same and application of nanometer medicine loading system

A nano-drug loading and nano-particle technology, which is applied in the field of nano-drug loading system and its preparation, can solve the problems of oxygen consumption, poor treatment effect, poor stability of catalase, etc., and achieve reduced oxygen consumption and good system safety performance, good biocompatibility

Inactive Publication Date: 2018-09-14
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its main defect is that the anticancer effect of PDT is highly dependent on the oxygen concentration in the cancer cells, and the treatment process is constantly consuming oxygen
[0003] The main disadvantages of the above means: (1) Carrying oxygen: Oxygen is a small gas molecule, which is easy to leak out of the carrier and has low efficiency; (2) Catalase has poor stability and is easily inactivated. (3) The catalytic efficiency of near-infrared photolysis of water is low, and the penetration of near-infrared light is poor, so that the activity of photosensitizer molecules is poor, and the therapeutic effect is not good.

Method used

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  • Nanometer medicine loading system, method for preparing same and application of nanometer medicine loading system
  • Nanometer medicine loading system, method for preparing same and application of nanometer medicine loading system
  • Nanometer medicine loading system, method for preparing same and application of nanometer medicine loading system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] [Example 1] Preparation of nano drug loading system (CHC-PZM@HA)

[0047] 1. Porphyrin metal-organic framework structure of zirconium

[0048] The tetrakis(4-carboxyphenyl)porphyrin ligand was synthesized in two steps (refer to Feng DW et al, J.Am.Chem.Soc.2013, 135, 17105-17110 for details). First, add 6.9 (5.5, 6.9, 8) g methyl p-formylbenzoate to a 500 mL three-neck round bottom flask containing 100 mL propionic acid, drop 3.0 g pyrrole into the flask after the mixture is refluxed, and mix the solution React for 12 hours in the dark. After the mixture was cooled to room temperature, the crystals were collected by centrifugation and washed 3-5 times to obtain purple crystals. Then, the obtained crystals were dispersed in a mixed solvent consisting of 25 mL of tetrahydrofuran (THF) and 25 mL of methanol (MeOH), then transferred to an aqueous solution of 2.6 g of KOH (2.6 g of KOH was dissolved in 25 mL) for dispersion, and then the mixture was refluxed for 12 hours ...

Embodiment 2

[0055] [Example 2] Preparation of nano drug loading system (CHC-PZM@HA)

[0056] The porphyrin metal-organic framework structure of zirconium in this example is derived from Example 1.

[0057] 1. Loading α-cyano-4-hydroxycinnamate into zirconium porphyrin metal-organic framework

[0058] Preparation of CHC@PZM: The small molecule inhibitor (α-cyano-4-hydroxycinnamate, CHC) was loaded into PZM. 300 mg of α-cyano-4-hydroxycinnamate was dissolved in 8 mL of DMF, which was then added to a solution of PZM (40 mg) in DMF (4 mL) and stirred at room temperature for 24 hours. at 1.1×10 4 Excess CHC was removed by centrifugation at rpm for 30 minutes and washed with fresh DMF. Then the PZM loaded with CHC was washed with distilled water for 3-5 times and then dispersed in distilled water for later use.

[0059] 2. Coating hyaluronic acid on the porphyrin metal-organic framework of zirconium loaded with α-cyano-4-hydroxycinnamate

[0060] Preparation of CHC-PZM@HA: CHC-loaded PZM w...

Embodiment 3

[0061] [Example 3] Preparation of nano drug loading system (CHC-PZM@HA)

[0062] The porphyrin metal-organic framework structure of zirconium in this example is derived from Example 1.

[0063] 1. Loading α-cyano-4-hydroxycinnamate into zirconium porphyrin metal-organic framework

[0064] Preparation of CHC@PZM: The small molecule inhibitor (α-cyano-4-hydroxycinnamate, CHC) was loaded into PZM. 600 mg of α-cyano-4-hydroxycinnamate was dissolved in 12 mL of DMF, which was then added to a solution of PZM (60 mg) in DMF (6 mL) and stirred at room temperature for 24 hours. at 1.1×10 4 Excess CHC was removed by centrifugation at rpm for 30 minutes and washed with fresh DMF. Then the PZM loaded with CHC was washed with distilled water for 3-5 times and then dispersed in distilled water for later use.

[0065] 2. Coating hyaluronic acid on the porphyrin metal-organic framework of zirconium loaded with α-cyano-4-hydroxycinnamate

[0066] Preparation of CHC-PZM@HA: CHC-loaded PZM ...

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Abstract

The invention discloses a nanometer medicine loading system, a method for preparing the same and application of the nanometer medicine loading system, and belongs to the field of nanometer biomedicine. The nanometer medicine loading system, the method and the application have the advantages that a lactic acid protein inhibitor CHC (alpha-cyano-4-hydroxycinnamate) is carried into cells by the aid of porphyrinic zirconium metal organic framework materials for the first time, targeting polymers are coated, the intratumor oxygen consumption can be reduced after the CHC is released, equivalently, the intratumor oxygen concentration is increased, accordingly, the shortcomings of photodynamic cancer therapy in the prior art can be overcome by the aid of the nanometer medicine loading system, andphotodynamic antitumor effects can be greatly improved; the nanometer medicine loading system is excellent in biocompatibility and system safety.

Description

technical field [0001] The invention belongs to the field of nano-biomedicine, and relates to a nano-drug loading system and its preparation method and application. Background technique [0002] In recent years, many scholars have carried out photodynamic therapy (PDT) cancer research. Photodynamic therapy is a non-invasive anti-cancer method, which specifically refers to: under a certain wavelength of light radiation, the photosensitizer converts triplet oxygen (3O2) in tumor cells into active oxygen ( ROS), so as to achieve the anti-tumor effect. Its main defect is that the anticancer effect of PDT is highly dependent on the oxygen concentration in the cancer cells, and the treatment process consumes oxygen continuously. The tumor microenvironment is inherently hypoxic. With the progress of PDT, the hypoxia of the tumor becomes more serious, which greatly limits the therapeutic effect of PDT. Therefore, researchers have devoted themselves to increasing the oxygen concen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K31/216A61K9/51A61K47/22A61K47/36A61P35/00
CPCA61K9/5123A61K9/5161A61K31/216A61K41/0076A61P35/00A61K2300/00
Inventor 张先正钟振林陈朝霞刘妙登曾旋
Owner WUHAN UNIV
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