Selective cancer-killing ability of new efficient porphyrin-based nanophotosensitizer in Lab-on-a-chip system

•Biocompatible multilayer oil core nanocapsules were successfully synthesized.•Tumor targeted capability of nanocapsules was observed.•Selective photodynamic activity against A549 cancer cells was revealed.•ROS generation in A549 cells treated with nanophotosensitizer was observed.•A novel Lab-on-a-chip system has been demonstrated. The oil core nanocapsules platform holds great potential to enhance the efficiency and accuracy of anticancer therapies. In this work, we describe the preparation of well-defined multilayer oil core nanocapsules built of oppositely charged polyelectrolytes via a layer-by-layer (LbL) assembly strategy and their use as advanced drug delivery systems for photodynamic therapy (PDT). The prepared nanocapsules show great stability in a physiological environment with uniform morphology and diameters of around 120 nm as disclosed by stability investigation, TEM and DLS analysis. By in vitro cellular experiments based on MTT assays, CLSM, FACS analysis and ROS detection, we confirmed that tetraphenylporphyrin TPP-loaded multilayer nanocapsules were selectively PDT-active against A549 cancer cells (human lung adenocarcinoma). Cellular uptake results showed that TPP NCs were readily taken up by A549 cells and enhanced TPP uptake was detectable in the NCs-treated cells in comparison to carrier free drug. TPP NCs also elicited intracellular ROS generation, which leads to enhanced toxicity in A549 cells. Toxicological impact of developed nanocapsules was further investigated using newly designed microfluidic Lab-on-a-chip system enabling photodynamic activity studies on three types of cell culture. Our results demonstrate a major potential of TPP-loaded multilayer oil core nanocapsules for PDT therapeutic treatment of a lung cancer.