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.

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