Development, characterization and bioactivity of EPP-AF® propolis loaded microcapsules

Andresa Aparecida Berretta, Jéssica Aparecida Lima, Isabella Salgado Gonçalves, Soraia I. Falcão, Ricardo Calhelha, Lilian Barros, Nathália Ursoli Ferreira, Nathaly Amorim Alcazar, Juliana Correa, Hernane da Silva Barud, Miguel Vilas-Boas, David De Jong, Jairo Kenupp Bastos.

The organic and functional food market grows every year. Organic food comes from sustainable and ecofriendly production, while functional foods provide some health benefits. Bees produces propolis from bioactive plant substances aiming to protect the hive and its inhabitants. Various biological activities for this material have been described, justifying interest in this product for health promotion. However, propolis generally has poor bioavailability, as it is relatively insoluble in water. Its most common form of presentation has the disadvantages of ethanol content and a strong and striking taste. Consequently, technological alternatives that can increase solubility with efficacy and safety, and that meet organic production specifications, are a challenge. We examined the possibility of organic propolis-loaded microcapsules as a functional health-food ingredient. Microcapsules were obtained using spray-dryer technology, with an emulsion based on propolis (EPP-AF®) and acacia gum (40:60). The propolis-loaded microcapsules were characterized using FT-IR, SEM, TGA, HPLC and spectrophotometric techniques, along with the determination of antimicrobial, antioxidant, antitumor, anti-inflammatory, and antihypercholesterolemic activities in in vitro models. Propolis-loaded microcapsules were successfully obtained, with spherical shape and encapsulation efficiency of 93.7±0.7%, presenting IC50 of 2.654±0.062 and 7.342±0.058 μg/mL by FRAP and DPPH antioxidant methods respectively; they had superior antimicrobial activity against gram-positive strains. Antitumor activity was calculated based on the concentration that inhibited 50% of cellular growth (GI50) in AGS, Caco2 and MCF-7 strains, giving results of 154.0±1.0, 117±1.0 and 271.0±25 μg/mL, respectively. Propolis-loaded microcapsules reduced the permeation of cholesterol by 53.7%, demonstrating antihypercholesterolemic activity and gave an IC50 of 59.0±0.1 μg/mL for NO production in RAW264.7 cells. These results demonstrate the potential of this new disposition to be offered as a food and pharmaceutical ingredient, though additional studies are recommended in order to validate the safety of proposed dosages.

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