Theranostic Nanoscaffold for Targeted Delivery of Cisplatin

High Resolution Image Download MS PowerPoint Slide The development of multifunctional nanoscaffolds offers a promising approach for the simultaneous diagnosis and therapy of various diseases. In this study, we designed and evaluated a multifunctional theranostic nanoscaffold termed FLAB, which consists of four integrated components: nanoparticles of iron oxide (Fe 3 O 4 ) functionalized with polyethylenimine (F), liposomes (L), a targeting aptamer (A), and the fluorescent dye [2-(4-(5,5-difluoro-5 H 4λ 4,5λ 4 -dipyrrolo[1,2-c:2′,1′-f][1,3,2]diazaborinin-10-yl)phenoxy)ethan-1-ol] (BODIPY, B). Upon encapsulation of the chemotherapeutic agent cisplatin (c), the nanoscaffold is referred to as FLABc. This nanomodular design enables both targeted drug delivery and imaging capabilities, making FLAB and FLABc promising candidates for theranostic applications. While cisplatin was selected as a model chemotherapeutic agent for lung cancer treatment, the nanoscaffold can be readily adapted to deliver alternative drugs for other pathological conditions. The targeting aptamer, which can be substituted to recognize different molecular biomarkers, enables disease-specific delivery and enhances therapeutic precision. Physicochemical characterization confirmed successful assembly and stability of the nanoscaffold. Cytotoxicity assays performed on MRC-5 (normal lung fibroblasts) and H1299 (nonsmall cell lung carcinoma) demonstrated that FLABc effectively reduced cancer cell viability while minimizing the cytotoxicity typically associated with free cisplatin. Flow cytometry revealed high apoptosis induction in H1299 lung cancer cells, and fluorescence microscopy confirmed efficient cellular uptake and localization. BODIPY-labeled FLAB nanoscaffolds are partially internalized in vesicles of H1299 cells, indicating trafficking to late endosomes/lysosomes. This distribution may facilitate intracellular cisplatin release and enhance therapeutic activity. These findings support the potential of FLAB as a flexible and targeted theranostic tool, capable of integrating drug delivery and diagnostic capabilities in a single nanosystem for cancer and beyond.