Alginate–lavender nanofibers with antibacterial and anti-inflammatory activity to effectively promote burn healing

One of the current challenges in wound care is the development of multifunctional dressings that can both protect the wound from external agents and promote the regeneration of the new tissue. Here, we show the combined use of two naturally derived compounds, sodium alginate and lavender essential oil, for the production of bioactive nanofibrous dressings by electrospinning, and their efficacy for the treatment of skin burns induced by midrange ultraviolet radiation (UVB). We demonstrate that the engineered dressings reduce the risk of microbial infection of the burn, since they stop the growth of Staphylococcus aureus. Furthermore, they are able to control and reduce the inflammatory response that is induced in human foreskin fibroblasts by lipopolysaccharides, and in rodents by UVB exposure. In particular, we report a remarkable reduction of pro-inflammatory cytokines when fibroblasts or animals are treated with the alginate-based nanofibers. The down-regulation of cytokines production and the absence of erythema on the skin of the treated animals confirm that the here described dressings are promising as advanced biomedical devices for burn management

Design, Synthesis, Structure–Activity Relationship Studies, and Three-Dimensional Quantitative Structure–Activity Relationship (3D-QSAR) Modeling of a Series of <i>O</i>‑Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase

We recently reported molecules designed according to the multitarget-directed ligand paradigm to exert combined activity at human fatty acid amide hydrolase (FAAH) and dopamine receptor subtype D3 (D3R). Both targets are relevant for tackling several types of addiction (most notably nicotine addiction) and other compulsive behaviors. Here, we report an SAR exploration of a series of biphenyl-<i>N</i>-[4-[4-(2,3-substituted-phenyl)­piperazine-1-yl]­alkyl]­carbamates, a novel class of molecules that had shown promising activities at the FAAH–D3R target combination in preliminary studies. We have rationalized the structural features conducive to activities at the main targets and investigated activities at two off-targets: dopamine receptor subtype D2 and endocannabinoid receptor CB_1. To understand the unexpected affinity for the CB₁ receptor, we devised a 3D-QSAR model, which we then prospectively validated. Compound <b>33</b> was selected for PK studies because it displayed balanced affinities for the main targets and clear selectivity over the two off-targets. <b>33</b> has good stability and oral bioavailability and can cross the blood–brain barrier