Human neutrophil elastase (HNE) is a serine protease that degrades matrix proteins. An excess of HNE may trigger several pathological conditions, such as psoriasis. In this work, we aimed to synthesize, characterize and formulate new HNE inhibitors with a 4-oxo-β-lactam scaffold with less toxicity, as well as therapeutic index in a psoriasis context. HNE inhibitors with 4-oxo-β-lactam scaffolds were synthesized and characterized by NMR, FTIR, melting point, mass spectrometry and elemental analysis. In vitro cytotoxicity and serine protease assays were performed. The compound with the highest cell viability (AAN-16) was selected to be incorporated in an emulsion (AAN-16 E) and in a microemulsion (AAN-16 ME). Formulations were characterized in terms of organoleptic properties, pH, rheology, droplet size distribution, in vitro drug release and in vivo psoriatic activity. All compounds were successfully synthesized according to analytical methodology, with good yields. Both formulations presented suitable physicochemical properties. AAN-16 E presented the most promising therapeutic effects in a murine model of psoriasis. Overall, new HNE inhibitors were synthesized with high and selective activity and incorporated into topical emulsions with potential to treat psoriasis.

The by-products of olive oil industry are a major ecological issue due to their phenolic content, highly toxic organic load, and low pH. However, they can be recovered and reused, since their components have antioxidant, anti-inflammatory, and photoprotector properties. In this work, oil-in-water creams containing three different olive oil industry by-products extracts were produced without the use of organic solvents. First, the extracts were thoroughly characterized in vitro for cytotoxicity, inhibition of skin enzymes, and antioxidant and photoprotection capacities. Safety studies were then performed, including ocular and skin irritation tests, ecotoxicity evaluation, and in vivo Human Repeat Insult Patch Test. The results obtained in this initial characterization supported the incorporation of the extracts in the cream formulations. After preparation, the creams were characterized for their organoleptic, physicochemical, droplet size and rheological properties, and microbial contamination. The results showed that all formulations were semi-solid creams, with stable pH, compatible with the skin, without microbial contamination, and with the expected droplet size range. The rheological analysis showed shear-thinning behavior with yield stress, with the viscosity decreasing with increasing shear rate. The oscillatory results suggest that the creams have a strong network structure, being easily rubbed into the skin. Finally, compatibility, acceptability and antioxidant efficacy were evaluated in vivo, in human volunteers. No adverse reactions were observed after application of the formulations on skin and the cream with the highest concentrations of phenolic compounds showed the highest antioxidant efficiency. In conclusion, the results suggest that olive oil industry by-products extracts have valuable properties that favor their re-use in the cosmetic industry. The example presented here showed their successful incorporation into creams and their impact in these formulations’ appearance, pH, and rheological performance, as well as their in vivo compatibility with skin and antioxidant efficiency.

Pickering emulsions are systems composed of two immiscible fluids stabilized by solid organic or inorganic particles. Pickering emulsions are particularly useful in cosmetics, where the surfactants are unwanted, as well as in the pharmaceutical field, where transdermal and/or dermal drug delivery is difficult to achieve and controlled drug release is desired. Here, we studied calcium carbonate particles as stabilizers of Pickering emulsions for topical use. An optimized formulation was obtained using a Quality by Design approach. First, a screening experiment was performed to identify the formulation and process critical variables that affect the quality properties of the Pickering emulsion. The optimization of the production was then studied by establishing the design space. The final formulation was hereinafter investigated regarding the pH, rheological properties, and in vitro cytotoxicity assays. The results showed the formulation had a pH compatible with human skin and a shear thinning behavior. Moreover, this formulation showed a strong network structure, with a suitable spreadability on the skin, allowing an easy application. The in vitro assays were performed to assess the potential cytotoxicity of the calcium carbonate-stabilized emulsion and the particles themselves, and the results revealed that the formulation did not significantly affect the cell viability. In conclusion, the use of calcium carbonate particles as a stabilizer ingredient contributed to achieve an eco-friendly Pickering emulsion.

Keywords:CO 2 valorization cyclic carbonates tetrabutylammonium halide salts organocatalysis ordered mesoporous silica A B S T R A C T The conversion of CO 2 into cyclic carbonates in the presence of epoxides is one of the most promising methods to valorize this important C 1 building block. Tetrabutylammonium halide salts are known to catalyze this reaction with moderate activity, and often a co-catalyst is added to increase efficiency. Herein, the influence of the addition of ultra-large pore SBA-15 silica on the catalytic activity of tetrabutylammonium halide salts for this reaction has been investigated in detail. Whereas a negative effect of silica was observed for the NBu 4 Cl catalyst, surface silanols were shown to strongly improve the yield of the reaction when NBu 4 Br and NBu 4 I were used as catalysts. The catalytic activity of the NBu 4 I salt could be increased by a factor of ten when a relevant amount of mesoporous silica was added. This latter catalytic system leads to high yields and selectivity for a wide variety of substrates under mild condition (80°C). Measurement of the activation parameters demonstrated that the rate enhancement is entropically driven: the pre-organization of the reactants and catalyst on the surface leads to a marked decrease of the activation energy of the reaction. A direct comparison between yield improvement induced by the addition of either an amorphous or a mesostructured silica highlights the crucial role played by the shape and concavity of the support.

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Olea europaea L. is one of the most important fruit trees in the Mediterranean countries due to its products, olive oil and table olives. However, the olive oil extraction industry produces large amounts of byproducts, such as olive pomace, leaves and olive mill wastewater, which are considered harmful to the environment, having negative impacts on soil, aquatic and air ecosystems. The olive oil industry byproducts are a major ecological issue mainly due to their phenolic components, such as oleuropein, hydroxytyrosol and tyrosol. However, olive oil industry by-products can be recovered, treated and studied for their health-promoting properties, holding great potential for the cosmetic and pharmaceutical industries. Furthermore, the recovery and treatment processes contribute to an efficient waste management and sustainability of the olive oil industry, leading to important economic benefits. The phenolic compounds extracted and obtained from these by-products present numerous health properties and can be used as antioxidant, photoprotector, anti-inflammatory and/or antimicrobial agents in wellness and therapeutics of the skin. This review highlights issues related to olive oil industry by-products and then proceeds to discuss how their beneficial biological activities make them reusable, particularly their high positive impact in treating skin disorders.

Naturally derived surfactants in hair care products are a trend in cosmetic technology. This study aimed to formulate and fully characterize the performance of shampoos with sugar‐derived surfactants, namely, the alkyl polyglucosides decyl glucoside and coco‐glucoside. In addition, different thickeners and conditioning ingredients were added to improve the formulation properties. A sodium laureth sulfate (SLES) formulation was used as control. Rheology, pH, foaming, contact angles on a keratin surface, and surface tensions were determined. The safety of the formulations was evaluated by in vitro cytotoxicity studies using the human keratinocyte HaCaT cell line and human retinal pigment epithelial cells ARPE‐19. The efficacies were studied by in vitro hair combing force assays and in vivo sensorial analysis. The formulated sugar surfactant‐based shampoos showed the following properties: (i) pH values higher than those of SLES (which were posteriorly lowered with lactic acid); (ii) higher foamability than SLES, and high wettability; (iii) Newtonian behavior and predominance of liquid state with a suitable viscosity; (iv) low cytotoxicity in both human keratinocytes and retinal cell lines (in contrast to SLES); (v) easier hair combing than SLES, when Polyquaternium‐7 was used as conditioner; (vi) efficient and gentle hair washing; and (vii) favorable sensorial analysis confirming the previous washing properties. In conclusion, the sugar surfactants had a considerable impact in the properties of the shampoo formulations, in terms of both hair cleansing properties and efficacy, as demonstrated here. These favorable outcomes clearly support the use of these ingredients in shampoo formulation design.

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