Title:
ACID-RESPONSIVE NANO-MICELLE ON BASIS OF CHERENKOV EFFECT, AND PREPARATION METHOD AND USE THEREFOR
Document Type and Number:
WIPO Patent Application WO/2023/001317
Kind Code:
A1
Abstract:
Disclosed in the present invention are an acid-responsive nano-micelle on the basis of the Cherenkov effect, and a preparation method and use therefor. The nano-micelle uses pyropheophorbide a as the photosensitizer main body, and modifies N,N-diisopropylamine, 131I labeled tyrosine or any one of 68Ga, 177Lu, 89Zr labeled tetraazacyclododecane tetraacetic acid, and polyethylene glycol to functionalize, and connects by means of N-Alpha-Fmoc-N-Epsilon-t-Boc-L-Lysine. According to the present invention, a micelle is prepared by a plurality of sequential amide coupling reactions, and can be passively targeted to a tumor site. In normal tissues, due to the aggregation-induced quenching effect, the photodynamics of the micelle is suppressed, and there is no phototoxicity. The micelle can respond to decomposition, recover photodynamically at the tumor site, generate active oxygen species by means of photoexcitation to kill tumors, have Cherenkov self-illumination, can avoid the limited penetration capability of the conventional exogenous light, and finally achieve selective photodynamic therapy of a deep tumor.
Inventors:
SUN XIAOLIAN (CN)
GUO JINGRU (CN)
FENG KAI (CN)
GUO JINGRU (CN)
FENG KAI (CN)
Application Number:
PCT/CN2022/116525
Publication Date:
January 26, 2023
Filing Date:
September 01, 2022
Export Citation:
Assignee:
UNIV CHINA PHARMA (CN)
International Classes:
A61K9/107; A61K41/00; A61K47/54; A61K47/60; A61K51/04; A61K51/06; A61K51/12; A61K101/02; A61P35/00; C07K1/107; C07K1/13; C07K5/065
Domestic Patent References:
| WO2017045192A1 | 2017-03-23 | |||
| WO2017019520A1 | 2017-02-02 |
Foreign References:
| CN113546042A | 2021-10-26 | |||
| CN114010598A | 2022-02-08 | |||
| CN105267966A | 2016-01-27 |
Attorney, Agent or Firm:
NANJING SUGAO PATENT AND TRADEMARK FIRM ( ORDINARY PARTNERSHIP ) (CN)
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