mt0c00386_si_001.pdf (689.18 kB)
Hypocrellin-Based Multifunctional Phototheranostic Agent for NIR-Triggered Targeted Chemo/Photodynamic/Photothermal Synergistic Therapy against Glioblastoma
journal contribution
posted on 2020-05-31, 12:03 authored by Chuangli Zhang, Jiasheng Wu, Weimin Liu, Xiuli Zheng, Wenjun Zhang, Chun-Sing Lee, Pengfei WangA huge
challenge exists in the diagnosis and treatment of malignant
glioblastoma (GBM) due to the presence of the blood–brain barrier
(BBB). Herein, a multifunctional phototheranostic agent is designed
on the basis of an octadecane-modified temozolomide (TMZ-C18) for chemotherapy, a dicysteamine-modified hypocrellin derivative
(DCHB) as a natural-origin photosensitizer with a singlet
oxygen (1O2) quantum yield of 0.51, and a cyclic
peptide (cRGD) as a targeting unit against glioblastoma. Co-encapsulated DCHB and TMZ-C18 assembly with cRGD decoration,
referred to as DTRGD NPs, shows a wide absorption at
the NIR region peaked at 703 nm, an NIR emission peak at 720 nm, good
photostability, high photothermal conversion efficiency (33%), and
effective degradation of TMZ-C18. More importantly, DTRGD NPs can efficiently break through the blood–brain
barrier and enrich in the orthotopic glioblastoma. The treatment of
subcutaneous U87MG tumor beard mice demonstrates that DTRGD
NPs present remarkable anticancer efficiency and the targeted
chemo/photodynamic/photothermal synergistic therapy can be achieved
with almost no toxicity. This multifunctional phototheranostic agent
shows great potential for the diagnosis and treatment of glioblastoma.