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Pure photosensitizer self-assembled nanoparticles and preparation and application thereof

A self-assembled nanoparticle and photosensitizer technology, applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of drug leakage, poor PPa hydrophobicity, poor toxicity related to excipients, etc., and achieve high-efficiency encapsulation, good stability, Simple and easy preparation method

Active Publication Date: 2020-09-04
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows creation of stable and effective drug carriers that can be used safely by deliver them through blood vessels or other body cavities without causing damage during their use. It also includes methods for studying how these materials behave under various conditions such as exposure to specific substances like glucose, oxidizing enzymes, reducing drugs, etc., which are important factors affecting its effectiveness at treating diseases caused due to abnormal cells' behavioral patterns within the human body.

Problems solved by technology

The technical problem addressed in this patented text relates to improving the effectiveness of light oncology during medical procedures while minimizing side effects caused by current techniques like radiation exposure. Current approaches involve administering high dosages of chemical compounds which often cause adverse events. A new method called photoimmunization involves delivering photosensorium dyes directly onto target areas instead of injecting them locally could improve patient outcomes but they lack sufficient retention time inside tissues after being delivered over hours. This challenge needs further study because conventional ways cannot effectively transport pharmacologists' medications accurately enough within specific locations.

Method used

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  • Pure photosensitizer self-assembled nanoparticles and preparation and application thereof
  • Pure photosensitizer self-assembled nanoparticles and preparation and application thereof
  • Pure photosensitizer self-assembled nanoparticles and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1: Preparation of PPa self-assembled nanoparticles and PEG-modified PPa self-assembled nanoparticles

[0044] Accurately weigh 1 mg of PPa, dissolve it with 200 μL of a mixed solution of ethanol and tetrahydrofuran (3:2), and slowly add the solution dropwise to 2 mL of deionized water under stirring, to spontaneously form uniform nanoparticles of PPa nanoparticles. The organic solvent in the nano-preparation was removed by dialysis with deionized water at 25°C.

[0045] (1) The preparation method of non-PEGylated PPa self-assembled nanoparticles: Dissolve a certain amount of PPa in an appropriate amount of ethanol and tetrahydrofuran (3:2), and slowly add the solution dropwise to water under stirring, and the PPa spontaneously Form uniform nanoparticles. Ethanol and tetrahydrofuran in the preparation are removed by dialysis to obtain a nano colloid solution without any organic solvent.

[0046] (2) The preparation method of PEG-modified PPa self-assembled n...

Embodiment 2

[0055] Embodiment 2: The self-assembly mechanism analysis of PPa

[0056] Through simple computer simulations, the mechanism of PPa self-assembly was explored, and the molecular docking calculation was completed using the Vina program of the Yinfu cloud computing platform. The compound PPa was energy minimized under the MMFF94 force field to obtain a 3D structure and form a stable nanoassembly. AutoDock Vina program was used for semi-flexible docking, the results are as follows figure 2 As shown, the unique multiple pyrrole ring structures of PPa molecules, as well as the intermolecular π-π stacking and hydrophobic interactions have made great contributions to the self-assembly of PPa molecules.

Embodiment 3

[0057] Embodiment 3: Colloidal stability test of PPa self-assembled nanoparticle

[0058] 1 mL of the PEG-modified self-assembled nanoparticles prepared in Example 1 was taken out, added to 20 mL of phosphate buffered saline (PBS, pH 7.4) containing 10% FBS, incubated at 37° C. for 24 hours, and At predetermined time points (0, 1, 2, 4, 6, 8 and 12 hours), the particle size change was measured by dynamic light scattering. The result is as image 3 As shown, compared with other groups, PPa / PCL-PEG 2K Nanoparticles and PPa / PPa-PEG 2K The nanoparticle colloid has good stability, and the particle size does not change significantly within 24 hours. Further preferred is Pa / PCL-PEG 2K Nanoparticles and PPa / PPa-PEG 2K nanoparticles.

[0059] 1 mL of the PEG-modified self-assembled nanoparticles prepared in Example 1 was taken out and added to 20 mL of PBS. Under different laser irradiation times, the changes in the particle size of the nanoparticles were observed, and the result...

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Abstract

The invention belongs to the technical field of medicine and pharmacy, and relates to pure photosensitizer self-assembled nanoparticles so as to achieve the effects of being high in medicine loading quantity, good in stability and low in toxic and side effects, and capable of performing specific disintegration on tumor locations, retarding aggregation-caused quenching (ACQ) effects, and improvingantitumor activity. The pure photosensitizer self-assembled nanoparticles provided by the invention are prepared through separate self-assembly of a photosensitizer, or prepared through self-assemblyof the photosensitizer and a PEG modifier through core-sheath matching, wherein the photosensitizer is one or more of pheophorbide a, chlorophyll a, pheophorbide a, 2-[1-hexyloxyethyl]-2-devinyl pyropheophorbide-a and chlorin e6, the PEG modifier is an amphiphilic polymer of an amphipathic PEG modifier, PEG and the photosensitizer, and the weight ratio of the photosensitizer to the PEG modifier is(10:0.5)-(10:3). A new strategy and more choices are provided for developing a pure medicine self-assembled delivery system, and urgent requirements for efficient chemotherapy preparations in clinical application are met.

Description

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Claims

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Application Information

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Owner SHENYANG PHARMA UNIVERSITY
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