1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-PC is a phospholipid-porphyrin conjugate that is composed of phosphatidylcholine containing palmitic acid at the sn-1 position and the photosensitizer pyropheophorbide a at the sn-2 position. Lipid nanoparticles (LNPs) containing 1-palmitoyl-2-pyropheophorbide a-sn-glycero-3-PC and encapsulating FAM-labeled siRNA are dissociated under irradiation with near-infrared light (NIR) in PC3-Luc6 cells. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-PC then enters the endolysosomal membrane and generates reactive oxygen species (ROS), which disrupt the membrane and allow the release of FAM-labeled siRNA into the cytosol. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-PC-stabilized nanoemulsions loaded with the mitotic inhibitor paclitaxel, combined with laser irradiation, reduce tumor growth and increase survival in a KB squamous cell carcinoma mouse xenograft model.
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