The fusion of technology and medicine, embodied by Magnetic Resonance Imaging (MRI), has transformed healthcare. Our review highlights the novel integration of SPIONs, tracing their journey from research to advanced clinical applications.
In recent times, researchers have aimed for new strategies to combat cancer by the implementation of nanotechnologies in biomedical applications. This work focuses on developing protein-based nanoparticles loaded with a newly synthesized NIR emitting and absorbing phthalocyanine dye, with photodynamic and photothermal properties. More precisely, we synthesized highly reproducible bovine serum albumin-based nanoparticles (75% particle yield) through a two-step protocol and successfully encapsulated the NIR active photosensitizer agent, achieving a good loading efficiency of 91%. Making use of molecular docking simulations, we confirm that the NIR photosensitizer is well protected within the nanoparticles, docked in site I of the albumin molecule. Encouraging results were obtained for our nanoparticles towards biomedical use, thanks to their negatively charged surface (−13.6 ± 0.5 mV) and hydrodynamic diameter (25.06 ± 0.62 nm), favorable for benefitting from the enhanced permeability and retention effect; moreover, the MTT viability assay upholds the good biocompatibility of our NIR active nanoparticles. Finally, upon irradiation with an NIR 785 nm laser, the dual phototherapeutic effect of our NIR fluorescent nanoparticles was highlighted by their excellent light-to-heat conversion performance (photothermal conversion efficiency 20%) and good photothermal and size stability, supporting their further implementation as fluorescent therapeutic agents in biomedical applications.
Nowadays, extensive research is being carried out to find innovative solutions for the development of stable, reproductible, and highly efficient fluorescent contrast agents with the ability of targeting specific cells, which can be further implemented for fluorescent-guided surgery in a real clinical setting. The present study is focused on the development of fluorescent dye-loaded protein nanoparticles (NPs) to overcome the drawbacks of the standard administration of free organic fluorophores, such as cytotoxicity, aqueousinstability, and rapid photo-degradation. Precisely, human serum albumin (HSA) NPs loaded with two different FDA approved dyes, namely indocyanine green (ICG) and fluorescein isothiocyanate (FITC), with a fluorescence response in the near-infrared and visible spectral domains, respectively, have been successfully designed. Even though the diameter of fluorescent HSA NPs is around 30 nm as proven by dynamic light scattering and transmission electron microscopy investigations, they present good loading efficiencies of almost 50% for ICG, and over 30% for FITC and a high particle yield of over 75%. Molecular docking simulations of ICG and FITC within the structure of HSA confirmed that the dyes were loaded inside the NPs, and docked in Site I (subdomain IIA) of the HSA molecule. After the confirmation of their high fluorescence photostability, the NPs were covalently conjugated with folic acid (HSA-FA NPs) in order to bind specifically to the folate receptor alpha (FRα) protein overexpressed on NIH:OVCAR3 ovarian cancer cells. Finally, fluorescence microscopy imaging investigations validate the improved internalization of folate targeted HSA&FITC NPs compared to cells treated with untargeted ones. Furthermore, TEM examinations of the distribution of HSA NPs into the NIH:OVCAR3 cells revealed anincreased number of NP-containing vesicles for the cells treated with HSA-FA NPs, compared to the cells exposed to untargeted HAS NPs, upholding the enhanced cellular uptake through FRα-mediated potocytosis.
9 February 2023 in International Journal of Pharmaceutics
Oxidative stress is linked to a series of diseases; therefore, the development of efficient antioxidants might be beneficial in preventing or ameliorating these conditions. Based on the structure of a previously reported compound with good antioxidant properties and on computational studies, we designed several catechol derivatives with enhanced antioxidant potential. The compounds were synthesized and physicochemically characterized, and their antioxidant activity was assessed through different antiradical, electron transfer and metal ions chelation assays, their electrochemical behavior and cytotoxicity were studied. The results obtained in the in vitro experiments correlated very well with the in silico studies; all final compounds presented very good antioxidant properties, generally superior to those of the reference compounds used. Similarly, the results obtained from studying the compounds’ electrochemical behavior were in good agreement with the results of the antioxidant activity evaluation assays. Regarding the compounds’ cytotoxicity, compound 7b had a dose-dependent inhibitory effect against all cell lines. In conclusion, through computer-aided design, we developed several catechol thiazolyl-hydrazones with excellent antioxidant properties, of which compound 7b, with two catechol moieties in its structure, exhibited the best antioxidant activity.