Photodynamic
therapy (PDT) is a clinically approved minimally invasive
therapy for malignant diseases. Indocyanine green (ICG) is a prominent
photosensitive agent for PDT, but it has intrinsic drawbacks such
as aggregation, instability, and photolytic degradation. Although
numerous nanoparticle-based approaches have been studied to overcome
such issues, there are still limitations such as potential immunogenicity
and unprecise and inefficient delivery to the tumor. In this study,
we disclosed a nanoformulation (SIWV-pSiNP(ICG)), SIWV peptide-functionalized
glioblastoma (GBM) homing, and ICG-incorporated porous silicon nanoparticles
(pSiNPs). The nanoformulation demonstrated an enhanced photodynamic
property under NIR light irradiation with improved stability of the
incorporated ICG. The SIWV-pSiNP(ICG) also showed significant targeting
ability to the GBM cells with nontoxicity and laser-triggered ROS
generation in situ. As a result, the SIWV-pSiNP(ICG) showed superior
therapeutic efficacy (anticancer efficiency) with excellent biocompatibility
in the GBM xenograft mice. This work presents a novel and efficient
strategy to enhance PDT efficacy for the targeted GBM therapy.