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To fight against cancer, smarter drugs and drug delivery systems are required both to boost the efficiency of current treatments while reducing deleterious side effects, and combine diagnosis/monitoring with therapy (theranosis) in the search for the final goal of personalized medicine. This work presents the design, preparation, and proof‐of‐principle validation of a novel hybrid organic–inorganic nanocomposite joining together non‐invasive imaging capabilities through magnetic resonance imaging and externally actuated therapeutic properties through a combination of chemo‐ and thermotherapy. The lipidic matrix of the nanocomposite was composed of carnauba wax, which was simultaneously dual loaded with magnetite nanoparticles and the anticancer drug Oncocalyxone A. Obtained formulations were fully characterized and showed outstanding performances as T2‐contrast agents in magnetic resonance imaging (r2>800 mm−1 s−1), heat generating sources in magnetic hyperthermia (specific absorption rate, SAR>200 W g−1Fe), and magnetically responsive drug delivery vehicles. The potential of the designed formulations as theranostic agents was validated in vitro and results indicated a synergistic thermo/chemotherapeutic effect derived from heat generation and controlled drug delivery to cancer growth. Thereby, this external control over the drug delivery profile and the integrated imaging capability open the door to personalized cancer medicine and real‐time monitoring of tumor progression. [ABSTRACT FROM AUTHOR]

Keywords: hybrid nanocomposites; magnetic hyperthermia; magnetic nanoparticles; MRI; thermo/chemotherapy EN hybrid nanocomposites magnetic hyperthermia magnetic nanoparticles MRI thermo/chemotherapy 4434 4434 1 04/08/20 20200406 NES 200406 B Theranostic magnetic wax nanocomposite vehicles b were synthesized through a safe-by-design approach which simultaneously incorporated magnetic nanoparticles and the anticancer drug Oncocalyxone A. The obtained formulation showed outstanding performance as a T SB 2 sb -contrast agent in MRI and offered a synergistic thermo/chemotherapeutic effect in vitro derived from heat generation by magnetic hyperthermia and controlled drug delivery over cancer growth. This external control over the drug delivery profile and the integrated imaging capability open the door to personalized cancer medicine and real-time monitoring of tumor progression. [Extracted from the article]

Self-assembled peptide hydrogels have emerged in recent years as the new paradigm in biomaterials research. We have contributed to this field the development of hydrogels based on dehydrodipeptides N-capped with naproxen. The dehydrodipeptide hydrogels can be loaded with drugs, thus being potential nanocarriers for drug delivery. In this work novel dehydrodipeptides containing tyrosine and aspartic acid amino acid residues N-capped with naproxen and C-terminal dehydrophenylalanine were prepared and characterized. Superparamagnetic iron oxide nanoparticles (SPIONs) were incorporated into the dehydrodipeptide-based hydrogels and their effect on the self-assembly, structure and rheological and magnetic properties of the hydrogels was studied. Magnetic hydrogels, with incorporated SPIONs, displayed concentration-dependent T2-MRI contrast enhancement. Moreover, upon magnetic excitation (alternating magnetic field –AMF–) the SPIONs were able to generate a significant amount of heat. Hence, magnetic hyperthermia can be used as a remote trigger for release of drug cargos and SPIONs incorporated into the self-assembled dehydrodipeptide hydrogels. [ABSTRACT FROM AUTHOR]

[Display omitted] Triple-negative breast cancer (TNBC) represents 15–25 % of the new breast cancer cases diagnosed worldwide every year. TNBC is among the most aggressive and worst prognosis breast cancer, mainly because targeted therapies are not available. Herein, we developed a magnetic theranostic hybrid nanovehicle for targeted treatment of TNBC through pH-triggered tumour associated macrophages (TAMs) targeting. The lipid core of the nanovehicle was composed of a Carnaúba wax matrix that simultaneously incorporated iron oxide nanoparticles and doxorubicin (DOX) - a chemotherapeutic drug. These drug-loaded wax nanovehicles were modified with a combination of two functional and complementary molecules: (i) a mannose ligand (macrophage targeting) and (ii) an acid-sensitive sheddable polyethylene glycol (PEG) moiety (specificity). The TAMs targeting strategy relied on the mannose − mannose receptor recognition exclusively after acid-sensitive " shedding " of the PEG in the relatively low tumour microenvironment pH. The pH-induced targeting capability towards TAMs was confirmed in vitro in a J774A.1 macrophage cell line at different pH (7.4 and 6.5). Biocompatibility and efficacy of the final targeted formulations were demonstrated in vitro in the TNBC MDA-MB-231 cell line and in vivo in an M-Wnt tumour-bearing (TNBC) mouse model. A preferential accumulation of the DOX-loaded lipid nanovehicles in the tumours of M-Wnt-tumour bearing mice was observed, which resulted both on an efficient tumour growth inhibition and a significantly reduced off-target toxicity compared to free DOX. Additionally, the developed magnetic hybrid nanovehicles showed outstanding performances as T 2 -contrast agents in magnetic resonance imaging (r 2 ≈ 400–600 mM−1·s−1) and as heat generating sources in magnetic hyperthermia (specific absorption rate, SAR ≈ 178 W·g−1 Fe). These targeted magnetic hybrid nanovehicles emerge as a suitable theranostic option that responds to the urgent demand for more precise and personalized treatments, not only because they are able to offer localized imaging and therapeutic potential, but also because they allow to efficiently control the balance between safety and efficacy. [ABSTRACT FROM AUTHOR]