Co-Loading of Black Phosphorus Nanoflakes and Doxorubicin in Lysolipid Temperature-Sensitive Liposomes for Combination Therapy in Prostate Cancer.

Black phosphorus (BP) is one of the most promising nanomaterials for cancer therapy. This 2D material is biocompatible and has strong photocatalytic activity, making it a powerful photosensitiser for combined NIR photothermal and photodynamic therapies. However, the fast degradation of BP in oxic conditions (including biological environments) still limits its use in cancer therapy. This work proposes a facile strategy to produce stable and highly concentrated BP suspensions using lysolipid temperature-sensitive liposomes (LTSLs). This approach also allows for co-encapsulating BP nanoflakes and doxorubicin, a potent chemotherapeutic drug. Finally, we demonstrate that our BP/doxorubicin formulation shows per se high antiproliferative action against an in vitro prostate cancer model and that the anticancer activity can be enhanced through NIR irradiance.

High-Yield 99mTc Labeling of Gold Nanoparticles Carrying Atropine and Adrenaline.

This work focuses on the synthesis, purification, and analytical characterization of novel multifunctional Au NPs radiolabeled with 99mTc. These mixed-ligand shell Au NPs represent pharmacologically relevant samples for potential application in theragnostics. A ligand using a plain linker with a rather long chain consisting of 10 CH2 groups and a thiol moiety along with the PADA chelator has been used for both the attachment to the Au NP surface and for the 99mTc(CO)3+ complexation. We have combined this with our approach of stabilizing Au NP without any PEG or other stabilizing groups. Thus, monoligand shell Au NPs were radiolabeled by different strategies (prelabeling and postlabeling). Additionally, pharmacologically relevant Au NPs were synthesized carrying both a biofunctionalization with either atropine or adrenaline and the 99mTc radiolabel. All samples were obtained in very good yields (up to 80% of the total activity loaded onto the column) and completely/particularly purified using desalting columns. Detailed analytical characterization of the Au NPs before and after radiolabeling has proven the NPs' robustness throughout the process. Their intact functionalization, shape, and stability was confirmed by transmission electron microscopy (TEM), ultraviolet/visible (UV/vis) spectroscopy, dynamic light scattering (DLS), and infrared (IR) spectroscopy. The presented strategy represents a versatile building block system that can be adapted to a variety of bioactive molecules and may be of high relevance for theragnostic applications.