TY - JOUR
T1 - Phytosomes with persimmon (Diospyros kaki l.) extract
T2 - Preparation and preliminary demonstration of in vivo tolerability
AU - Direito, Rosa
AU - Reis, Catarina
AU - Roque, Luís
AU - Gonçalves, Margarida
AU - Sanches-Silva, Ana
AU - Gaspar, Maria Manuela
AU - Pinto, Rui
AU - Rocha, João
AU - Sepodes, Bruno
AU - Bronze, Maria Rosário
AU - Figueira, Maria Eduardo
N1 - This research was funded by Universidade de Lisboa PhD grant: REITORIA/BD/FF01/2015.
supported in part through Grant UID/DTP/04138/2019 from Fundação para a Ciência e a Tecnologia (FCT), Portugal.
PY - 2019/6/1
Y1 - 2019/6/1
N2 - 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.
AB - 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.
KW - Antioxidant
KW - Diospyros kaki
KW - Encapsulation efficiency
KW - Food supplement
KW - In vivo assessment
KW - Persimmon
KW - Phenolic compounds
KW - Phytosomes
UR - http://www.scopus.com/inward/record.url?scp=85069871346&partnerID=8YFLogxK
U2 - 10.3390/pharmaceutics11060296
DO - 10.3390/pharmaceutics11060296
M3 - Article
C2 - 31234548
AN - SCOPUS:85069871346
SN - 1543-8384
VL - 11
JO - Pharmaceutics
JF - Pharmaceutics
IS - 6
M1 - 296
ER -