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Title:
PHOTOSENSITIZER MOLECULE AND USE THEREOF IN INCREASE OF RETENTION TIME THEREOF IN TUMOR AND ENHANCEMENT OF THERAPY FOR LARGE-VOLUME TUMORS
Document Type and Number:
WIPO Patent Application WO/2023/061194
Kind Code:
A1
Abstract:
Disclosed in the present invention are a photosensitizer molecule and the use thereof in the increase of the retention time thereof in a tumor and the enhancement of the therapy for large-volume tumors, which belong to the field of nano-materials. According to the present invention, AN-BDP is synthesized by means of introducing anthracene into BODIPY-meso, and due to the strong intermolecular π-π interaction of anthracene, AN-BDP and an amphiphilic block copolymer DSPE-PEG 2000 are self-assembled into stable nanoparticles AN-BDP NPs. In addition, by means of anthracene, AN-BDP can be excited to a triplet excited state under light irradiation and acts with O 2 to generate 1O2. AN-BDP NPs are enriched at the tumor site and retained for around 10 days after tail vein injection. In a mouse tumor model having a conventional volume tumor, AN-BDP NPs can completely inhibit the growth of the tumor by means of one-time tail vein injection and one-time photoirradiation therapy; and in a large-volume tumor model, only a tumor growth inhibition rate of 12% is observed under the same therapy conditions. Due to the fact that the retention time thereof in a tumor is long, photoirradiation therapy can be carried out three times after a single injection of the AN-BDP NPs, and the therapeutic effect is remarkably improved.

Inventors:
SUN WEN (CN)
XI DONGMEI (CN)
PNEG XIAOJUN (CN)
FAN JIANGLI (CN)
Application Number:
PCT/CN2022/121296
Publication Date:
April 20, 2023
Filing Date:
September 26, 2022
Export Citation:
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Assignee:
UNIV DALIAN TECH (CN)
International Classes:
C07F5/02; A61K9/51; A61K41/00; A61K47/24; A61P35/00; B82Y5/00; B82Y40/00
Foreign References:
CN113861229A2021-12-31
CN111440206A2020-07-24
CN110950899A2020-04-03
CN110407864A2019-11-05
Other References:
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Attorney, Agent or Firm:
DALIAN EAST PATENT AGENT LTD. (CN)
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