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

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.

From Diospyros kaki L. (Persimmon) Phytochemical Profile and Health Impact to New Product Perspectives and Waste Valorization

“…The concentrations of the phenolic compounds (caffeic acid, catechin, chlorogenic acid, epicatechin, fisetin, ferulic acid, gallic acid, p-coumaric acid, and protocatechuic acid) were determined by the ultra-high performance liquid chromatography (UHPLC-DAD) method ( Table 2 ). In an aqueous persimmon fruit extract, gallic acid was found to be the most plentiful phenolic compound (2.794 ± 0.263 mg/100 g FW) detected [ 75 ], which is also in accordance with Pu and colleagues who found a concentration of 2.789 mg/100 g FW in the variety D. kaki var. silvestris M [ 76 ].…”

“…As a matter of fact, if we consider the work done by Jang and co-authors performed on homogeneous samples of the non-astringent cultivar Fuyu, the smallest concentration of soluble polyphenols was 454 mg GAE/100 g FW with ethanol extraction, about half the maximum concentration determined through extraction with water (860 mg GAE/100 g FW) [ 37 ]. Denev and colleagues determined 916.8 mg GAE/100 g FW [ 74 ], and Direito and colleagues determined 641 ± 51.96 mg GAE/100 g FW [ 75 ]. The inconsistency detected in these assays can be illuminated by considering the edaphoclimatic conditions, analysis of distinct opossum cultivars, and maturation phases, even when the fruit is more suitable for eating.…”

“…The concentrations of the three hydroxycinnamic acids (caffeic acid, ferulic acid, and chlorogenic acid) in the study done by Direito and colleagues were below 0.1 mg/100 g FW, except for the chlorogenic acid content, as was illustrated by Pu and colleagues [ 76 ]. The chlorogenic acid concentration in the work presented by these authors was 0.171 ± 0.016 mg/100 g FW D. kaki extract [ 75 ]. Published results of 0.274 mg/100 g FW in the variety of D. kaki var.…”

“…silvestris M, with a value of 0.048 ± 0.004 mg/100 g FW [ 76 ], roughly less than twice the concentration reported by Direito and colleagues of 0.097 ± 0.004 mg/100 g FW [ 75 ], in accordance with the concentration reported by Esteban-Muñoz and colleagues, where p-coumaric acid was the hydroxycinnamic acid with the greatest levels in both persimmon varieties (not statistically different) with ranges from 0.088 to 0.113 mg/100 g FW [ 20 ]. According to these authors’ work, protocatechuic acid had a concentration of 0.013 ± 0.010 mg/100 g in the Rojo Brillante variety, which was greater than those attained for the Triumph sample (0.004 mg/100 g), which is in agreement with the concentration reported by Direito and colleagues (0.005 mg/100 g FW) [ 75 ]. Greater concentrations were observed in various persimmon extracts acquired with various solvents [ 77 ], but the use of a HPLC equipped with ECD (electron capture detector) detection might overemphasize the concentration, and lower concentrations have also been described [ 75 ].…”

Phenolic Compounds Impact on Rheumatoid Arthritis, Inflammatory Bowel Disease and Microbiota Modulation

“…These new strategies of completely green nanotechnologies, such as phytosomes, can be employed to make the bioavailability of bioactive phenolic compounds more efficient [ 343 ], increasing the beneficial health effects of phenolic compounds that they carry, and may also be supportive of traditional pharmacological therapies in the context of disease [ 344 , 345 ].…”