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Objectives: Bioactive molecules derived from natural products combine the ability to absorb UV light and act as antioxidants. We developed an oil‐based sucupira (native species of the Brazilian cerrado) nanoemulsion (NE) using a high‐energy emulsification method and assessed its effectiveness in vitro. Methods: An easily scalable high‐pressure homogenization method was used to prepare the formulation. NE droplets mean diameter, pH, stability, conductivity and morphology were analysed. Formulation bioactivity was assessed using HaCaT cells. Key findings: The formulation presented suitable pH and size for topic administration and was stable for over 90 days upon storage at 4, 25 and 45°C. The NE showed protective effect against oxidative stress and reduced levels of UVA‐induced pro‐inflammatory cytokines IL‐6 and IL‐8. Conclusions: A novel, stable and easily prepared formulation was obtained for encapsulation of sucupira oil. The protective effect of the formulation by cytokine inhibition in the early stage of the inflammatory process was shown in vitro. Combined with the antioxidant effect by inhibition of reactive oxygen species, the use of sucupira oil NE for prevention and treatment of UVA‐induced stress could contribute to decrease the effects of UV radiation on skin ageing. [ABSTRACT FROM AUTHOR]

To design nanoparticle (NP)-based drug delivery systems for pulmonary administration, biodegradable materials are considered safe, but their potential toxicity is poorly explored. We here explore the lung toxicity in mice of biodegradable nanoparticles (NPs) and compare it to the toxicity of non-biodegradable ones. NP formulations of poly(d,l-lactide-co-glycolide) (PLGA) coated with chitosan (CS), poloxamer 188 (PF68) or poly(vinyl alcohol) (PVA), which renders 200 nm NPs of positive, negative or neutral surface charge respectively, were analyzed for their biodistribution byin vivofluorescence imaging and their inflammatory potential after single lung nebulization in mice. After exposure, analysis of bronchoalveolar lavage (BAL) cell population, protein secretion and cytokine release as well as lung histology were carried out. The inflammatory response was compared to the one induced by non-biodegradable counterparts, namely, TiO2of rutile and anatase crystal form and polystyrene (PS). PLGA NPs were mostly present in mice lungs, with little passage to other organs. An increase in neutrophil recruitment was observed in mice exposed to PS NPs 24 h after nebulization, which declined at 48 h. This result was supported by an increase in interleukin (IL)-6 and tumor necrosis factor α (TNFα) in BAL supernatant at 24 h. TiO2anatase NPs were still present in lung cells 48 h after nebulization and induced the expression of pro-inflammatory cytokines and the recruitment of polymorphonuclear cells to BAL. In contrast, regardless of their surface charge, PLGA NPs did not induce significant changes in the inflammation markers analyzed. In conclusion, these results point out to a safe use of PLGA NPs regardless of their surface coating compared to non-biodegradable ones. [ABSTRACT FROM PUBLISHER]

Context: Ketoprofen is a non-steroid anti-inflammatory drug (NSAID) used in the treatment of rheumatic diseases and in mild to moderate pain. Ketoprofen has a short biological half-life and the commercially available conventional release formulations require dosages to be administered at least 2-3 times a day. Due to these characteristics, ketoprofen is a good candidate for the preparation of controlled release formulations. Objectives: In this work, a multiparticulate-sustained release dosage form containing ketoprofen in a carnauba wax matrix was developed. Methods: Particles were prepared by an emulsion congealing technique. System variables were optimized using fractional factorial and response surface experimental design. Characterization of the particles included size and morphology, flow rate, drug loading and in vitro drug release. Results: Spherical particles were obtained with high drug load and sustained drug release profile. The optimized particles had an average diameter of approximately 200 µm, 50% (w/w) drug load, good flow properties and prolonged ketoprofen release for more than 24 h. Conclusions: Carnauba wax microspheres prepared in this work represent a new multiparticulate-sustained release system for the NSAID ketoprofen, exhibiting good potential for application in further pharmaceutical processes. [ABSTRACT FROM AUTHOR]