Novel 1-phenylethyl-containing aza-BDOIPY for phototherapy and simultaneous monitoring of tumor immune microenvironment reprogramming

Therapy-induced modulation of the tumor microenvironment (TME) to overcome the immunosuppressive TME is considered to be a chance for cancer treatment. Herein, we prepared near-infrared absorbing aza-BODIPY PhEt-azaBDP with 1-phenylethyl group at 1,7-sites, a type I photodynamic-photothermal therapy (PDT-PTT) agent. Self-assembly PhEt-azaBDP nanoparticles (NPs) can provide combined phototherapeutic effects under light irradiation and simultaneously induce inflammatory TME, by monitoring tumor-associated macrophages (TAMs) repolarization. Utilizing cluster of differentiation 86 (CD86) and CD163 as the M1-type marker and M2-type marker respectively, PhEt-azaBDP NPs resulted in the increasement of the expression of CD86 and the decreasement of the expression of CD163 in TAMs under near-infrared (NIR) light irradiation, promoting TAMs to switch from M2-phenotype to M1-phenotype. Inflammatory cytokines, interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α), could be the key cytokine involved in the phototherapy-induced TME reprogramming. PhEt-azaBDP NPs could be a potential theranostic scaffold for the simultaneous induction and detection of TME reprogramming triggered by phototherapy. Self-assembly PhEt-azaBDP NPs as type I PDT-PTT agents can provide combined phototherapeutic effects under light irradiation and simultaneously induce inflammatory tumor microenvironment (TME), promoting tumor-associated macrophages (TAMs) to switch from M2-phenotype to M1-phenotype. [Display omitted]