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Oxygen-carrying nano photosensitive preparation as well as preparation method and application thereof

A technology of nano light and photosensitizer, applied in the field of medicine, can solve the problems of oxygen consumption and aggravation of hypoxia, etc., and achieve the effect of improvement effect, simple preparation process, good stability and biocompatibility

Pending Publication Date: 2022-03-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, a large amount of oxygen will be consumed during photodynamic therapy, which will further aggravate hypoxia.

Method used

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  • Oxygen-carrying nano photosensitive preparation as well as preparation method and application thereof
  • Oxygen-carrying nano photosensitive preparation as well as preparation method and application thereof
  • Oxygen-carrying nano photosensitive preparation as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Synthesis of Amphiphilic Photosensitive Polymer Material PEG-Poly(Ser-Ce6)

[0031] Step 1, synthesis of O-acetyl-L-serine-N-carboxy anhydride: Disperse 5 g of O-acetyl-L-serine-hydrochloride in 200 mL of anhydrous THF. Dissolve 3.92 g of triphosgene in a small amount of anhydrous tetrahydrofuran, then add it into the stirred O-acetyl-L-serine-hydrochloride solution, and stir in an oil bath at 48°C for 2 hours. After the reaction cleared, the temperature control was turned off and the reaction was allowed to cool to room temperature. The solvent was removed by vacuum rotary evaporation, followed by product purification using a silica gel column. The silica gel was vacuum-dried at 140 °C for 12 hours in advance, and the eluent was petroleum ether / ethyl acetate (volume ratio: 2:1 and then 1:1). After rotary evaporation, the light yellow oily product O-acetyl-L- Serine-N-carboxy anhydride.

[0032] Step 2, 0.389 g PEG2000-NH 2 Dissolve in 30 mL of anhydrous dimethyl su...

Embodiment 2

[0038] Preparation and Characterization of Self-carrying Oxygen Nanophotosensitizer (PSCe6-PFH)

[0039]Nanoparticles were prepared by phacoemulsification. A certain amount of PSCe6, namely PEG-Poly(Ser-Ce6), was weighed and dissolved in tetrahydrofuran to prepare a 1 mg / mL solution. After centrifugation (5000 rpm, 10 min), the supernatant was taken for later use. Slowly add 1 mL of the PSCe6 solution to the stirred 4 mL of deionized water. Then 20 µL of perfluorohexane (PFH) was added and ultrasonically emulsified at 30% ultrasonic power for 40 minutes, with a pause of 2 s for every 1 s of ultrasonication. The sonicated solution was dialyzed against distilled water (MWCO 3500Da) for 24 hours to obtain PSCe6-PFH, which was stored at 4°C. Since PFH has the ability to carry oxygen, an oxygen cylinder was connected through a catheter before use, and oxygen was blown through the PSCe6-PFH solution for 15 minutes to prepare a self-carrying oxygen nanophotosensitive preparation PS...

Embodiment 3

[0046] Changes of Dissolved Oxygen Content of Self-Carrying Oxygen Nanophotosensitizer (PSCe6-PFH) in Deoxygenated Solution

[0047] The dissolved oxygen (Dissolve Oxygen, DO) content was detected with a pen-type dissolved oxygen detector. First, blow the distilled water in the vial with nitrogen for 30 minutes to obtain deoxygenated water. Use a dissolved oxygen detector to detect the dissolved oxygen content in the solution, and record it every 5 s for a total of 600 s. During the whole process, the rest of the bottle mouth is sealed. , to create anaerobic conditions, as a blank control group. After blowing oxygen for 15 minutes to PSCe6-PFH, PSCe6 and distilled water by connecting the oxygen bottle through the catheter, take 1 mL each and inject it into the above-mentioned vial, and use the dissolved oxygen detector to detect the content of dissolved oxygen in the solution in the same way.

[0048] Figure 7 The dissolved oxygen content changes for the prepared nanopartic...

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Abstract

The invention discloses an oxygen self-carrying nano photosensitive preparation as well as a preparation method and application thereof, and belongs to the technical field of medicines. The preparation is prepared from an amphiphilic photosensitive polymer entrapped with a fluorocarbon compound with oxygen carrying capacity; the amphiphilic photosensitive polymer is a diblock copolymer modified by a photosensitizer, and the photosensitizer is selected from indocyanine green, a chlorin derivative, chlorophyll or heme; the fluorocarbon compound with the oxygen carrying capacity is selected from perfluorohexane, perfluoropentane, perfluorodecane, perfluorodecane or perfluorobromooctane. The oxygen self-carrying nano photosensitive preparation disclosed by the invention can obviously improve the oxygen level of a tumor by conveying oxygen to a tumor part, and enhances the killing effect of photodynamic; meanwhile, the preparation is combined with a cell mitochondrial respiration inhibitor, so that the hypoxia level of tumors can be further improved, and the treatment effect of photodynamic in a hypoxia area is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a self-carrying oxygen nanometer photosensitive preparation and its preparation method and application. Background technique [0002] Photodynamic therapy as a clinical approach has proven to be an effective option for the treatment of a variety of localized and superficial cancers. The basic principle is to irradiate the photosensitizer at a specific part with light of a specific wavelength to make it absorb light energy and transition to an excited state, and then transfer the energy to the surrounding molecular oxygen during the process of returning from the excited state to the ground state, thereby producing a large number of molecules with a lethal effect. reactive oxygen species (Reactive Oxygen Species, ROS), thereby killing tumor cells. Compared with traditional treatment methods, photodynamic therapy has the characteristics of high selectivity and less tox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00
CPCA61K41/0071A61K47/595A61K9/5146A61K33/00A61K47/06A61K45/06A61P35/00B82Y5/00B82Y20/00B82Y40/00A61K2300/00
Inventor 钱程根江雯怡戴园欣汤迎琦
Owner CHINA PHARM UNIV
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