Nanoencapsulation Improves Scavenging Capacity and Decreases Cytotoxicity of Silibinin and Pomegranate Oil Association

Abstract

Silibinin (SB) and pomegranate oil (PO) present therapeutic potential due to antioxidant activity, but the biological performance of both bioactives is limited by their low aqueous solubility. To overcome this issue, the aim of the present investigation was to develop nanocapsule suspensions with PO as oil core for SB encapsulation, as well as assess their toxicity in vitro and radical scavenging activity. The nanocapsule suspensions were prepared by interfacial deposition of preformed polymer method. SB-loaded PO-based nanocapsules (SBNC) showed an average diameter of 157 ± 3 nm, homogenous size distribution, zeta potential of -14.1 ± 1.7 mV, pH of 5.6 ± 0.4 and SB content close to 100%. Similar results were obtained for the unloaded formulation (PONC). The nanocapsules controlled SB release at least 10 times as compared with free SB in methanolic solution. The SBNC scavenging capacity in vitro was statistically higher than free SB (p < 0.05). Cell viability in monocytes and lymphocytes was kept around 100% in the treatments with SBNC and PONC, while the SB and the PO caused a decrease around 30% at 50 μM (SB) and 724 μg/mL (PO). Protein carbonyls and DNA damage were minimized by SB and PO nanoencapsulation. Lipid peroxidation occurred in nanocapsule treatments regardless of the SB presence, which may be attributed to PO acting as substrate in reaction. The free compounds also caused lipid peroxidation. The results show that SBNC and PONC presented adequate physicochemical characteristics and low toxicity against human blood cells. Thereby, this novel nanocarrier may be a promising formulation for therapeutic applications.

Diphenyl Diselenide and Clotrimazole Co-loaded into Eudragit® RS 100 Nanocapsules Formulation Has Superior Antioxidant Potential and Promising Anti-candida Activity

“…Furthermore, all nanocapsules suspensions were more effective than the free forms (MCT CD and CO CD). This result can be explained due to the superior contact provided by the nanometer scale of the particles in suspension, facilitating the hydrogen donation to the radical site [41]. Besides, our results corroborate with other studies that showed the improved radical scavenging activity provided by the nanoparticles [21,22].…”

Increased Loading, Efficacy and Sustained Release of Silibinin, a Poorly Soluble Drug Using Hydrophobically-Modified Chitosan Nanoparticles for Enhanced Delivery of Anticancer Drug Delivery Systems

“…It suggested that the pCNP system is a great carrier candidate that can increase the loading of hydrophobic load. The study of Marchiori et al [ 33 ], performed nanoencapsulation by using interfacial deposition of the preformed polymer method with pomegranate oil as an oil core for the encapsulation of SLB. In their study, a high % E.E was achieved, credited to the higher affinity of SLB with the oil core than the aqueous phase.…”

Hydrogels for the Delivery of Plant-Derived (Poly)Phenols

“…In the design of this original HG system, the authors took also into account the additional biological activity of the oily component of the nanocapsules, as both SB and pomegranate seed oil exert anti-inflammatory activity, mostly by the inhibition of the NF-κB pathway [ 77 , 78 ]. The SB-loaded nanocapsules (formed by an oily core surrounded by a polymeric membrane) were prepared as a suspension according to a method carried out by the same research group, that is, the interfacial deposition of preformed polymer method [ 79 ]. Then, the final HG system was obtained by slow dispersion of this suspension into the co-polymer by using triethanolamine and imidazolidinyl urea (0.6%) for pH adjustment and preservative purposes, respectively.…”