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Design and Characterization of a New Quercus Suber-Based Pickering Emulsion for Topical Application

Publication . Carriço, Catarina; Pinto, Pedro; Graça, Angélica; Gonçalves, Lídia; Ribeiro, Helena; Marto, Joana

Quercus Suber Bark from Quercus suber L. is a natural, renewable and biodegradable biomaterial with multifunctional proprieties. In this study, we used it as solid particles to stabilize a Pickering emulsion. The main goal was to produce an optimized topical formulation using biocompatible organic particles as stabilizers of the emulsion instead of the common surfactants, whilst benefiting from Quercus suber L. proprieties. In this work, a Quality by Design (QbD) approach was successfully applied to the production of this emulsion. A screening design was conducted, identifying the critical variables of the formula and process, affecting the critical quality attributes of the emulsion (droplet size distribution). The optimization of the production was made through the establishment of the design space. The stability was also investigated during 30 days, demonstrating that Quercus Suber Bark-stabilized emulsions are stable since the droplet size distribution lowers. In vitro studies were performed to assess antioxidant and antiaging efficacy, which revealed that the formulation had indeed antioxidant proprieties. A physicochemical characterization demonstrated that the formulation presents a shear-thinning fluid, ideal for topical administration. The in vivo compatibility study confirmed that the final formulation is not skin irritant, being safe for human use. A sensorial analysis was also performed, using a simple sensory questionnaire, revealing very positive results. Thus, the use of Quercus Suber Bark particles as a multifunctional solid ingredient contributed to achieve a stable, effective and innovative Pickering emulsion with a meaningful synergistic protection against oxidative stress.

2019-03Journal article

Open access

Pickering Emulsions Stabilized by Calcium Carbonate Particles: A New Topical Formulation

Publication . Marto, Joana; Nunes, Andreia; Martins, Ana Margarida; Carvalheira, João; Prazeres, Pedro; Gonçalves, Lídia; Marques, Alexandre; Lucas, António; Ribeiro, Helena Margarida

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.

2020-07-31Journal article

Open access

Novel and Modified Neutrophil Elastase Inhibitor Loaded in Topical Formulations for Psoriasis Management

Publication . Nunes, Andreia; Marto, Joana; Gonçalves, Lídia; Simões, Sandra; Félix, Rita; Ascenso, Andreia; Lopes, Francisca; Ribeiro, Helena

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.

2020-04-14Journal article

Open access