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Open AccessArticle

Phytosomes with Persimmon (Diospyros kaki L.) Extract: Preparation and Preliminary Demonstration of In Vivo Tolerability

1
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal
2
Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. Universidad Complutense, 28871 Alcalá de Henares, Spain
3
Departamento de Ciências e Tecnologia de Biomassa, Mechanical Engineering and Resource Sustainability Centre, Faculdade de Ciências e Tecnologia, UNL, Quinta da Torre, 2829-516 Monte da Caparica, Portugal
4
National Institute for Agricultural and Veterinary Research (INIAV), Vairão, 4485-655 Vila do Conde, Portugal
5
Centre for Study in Animal Science (CECA), ICETA, University of Oporto, 4099-002 Oporto, Portugal
6
JCS, Dr. Joaquim Chaves, Laboratory of Clinical Analysis, 1495-068 Lisbon, Portugal
7
ITQB, Estação Agronómica Nacional, Av. da República, 2780-157 Oeiras, Portugal
8
IBET, Avenida da República, Quinta-do-Marquês, Estação Agronómica Nacional, 2780-157 Oeiras, Portugal
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(6), 296; https://doi.org/10.3390/pharmaceutics11060296
Received: 1 May 2019 / Revised: 19 June 2019 / Accepted: 20 June 2019 / Published: 22 June 2019
(This article belongs to the Special Issue Bioinspired Design in Drug Delivery)
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PDF [1484 KB, uploaded 22 June 2019]
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Abstract

Persimmon (Diospyros kaki L.), a fruit rich in phenolic compounds (PCs), has been considered effective in mitigating oxidative damage induced by an excess of reactive oxygen species. Due to large molecular weight and intrinsic instability in some physiological fluids, PCs’ passage through biological membranes is very limited. Carriers like phytosomes are promising systems to optimize oral absorption of encapsulated extracts. This work prepared and fully characterized phytosomes containing bioactive phenolic extracts from persimmon in terms of size, surface charge, encapsulation efficiency and stability over six months. These phytosomes were orally dosed to Wistar rats during a 15-day period. Afterwards, haematological and biochemical analyses were performed. Monodisperse phytosomes were successfully prepared, with size less than 300nm (PI < 0.3) and high encapsulation efficiency (97.4%) of PCs. In contrast to free extract, extract-loaded phytosomes had higher antioxidant activity after 6 months storage. Oral administration of extract-loaded phytosomes and free extract did not lead to lipidic profile changes and were within referenced normal ranges, as well as glycaemia levels and urine parameters. The results highlighted the potential of persimmon PCs as food supplements or pharmacological tools, suggesting a promising and safe phytosomal formulation containing bioactive agents of persimmon that could lead to health benefits. View Full-Text
Keywords: Persimmon; Diospyros kaki; phenolic compounds; phytosomes; food supplement; antioxidant; encapsulation efficiency; in vivo assessment Persimmon; Diospyros kaki; phenolic compounds; phytosomes; food supplement; antioxidant; encapsulation efficiency; in vivo assessment
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Direito, R.; Reis, C.; Roque, L.; Gonçalves, M.; Sanches-Silva, A.; Gaspar, M.M.; Pinto, R.; Rocha, J.; Sepodes, B.; Rosário Bronze, M.; Eduardo Figueira, M. Phytosomes with Persimmon (Diospyros kaki L.) Extract: Preparation and Preliminary Demonstration of In Vivo Tolerability. Pharmaceutics 2019, 11, 296.

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