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.
Objetivo: O óleo de linhaça apresenta diversas propriedades terapêuticas, principalmente devido à presença de ácidos poli-insaturados em sua composição. Para melhor eficácia e/ou aumento da estabilidade de óleos vegetais farmacologicamente ativos, sistemas nanoestruturados são desenvolvidos para veiculação deste tipo de substância. Este estudo objetivou desenvolver e caracterizar sistemas nanoestruturados contendo óleo de linhaça. Foram preparadas nanocápsulas poliméricas e nanoemulsões, avaliando-se duas concentrações de óleo (1,5% e 3,0%) em ambas as formulações e dois polímeros, Poli(ε-caprolactona) e Eudragit ® RL100, no desenvolvimento das nanocápsulas. Ambas as formulações apresentaram características adequadas para sistemas coloidais. Em relação às nanoemulsões, houve diferença significativa das características entre as quantidades de óleo, sendo que 1,5% de óleo de linhaça foi a concentração mais satisfatória. Em relação à presença dos polímeros, houve variação apenas dos valores de potencial zeta e pH. Concluindo, as formulações foram consideradas adequadas para o encapsulamento do óleo de linhaça, sendo carreadores promissores para outras substâncias ativas.Descritores: Óleos Vegetais; Óleo de Linhaça; Nanoemulsões: Nanocápsulas Poliméricas.
Cristina
ABSTRACTObjective: Linseed oil has several therapeutic properties, mainly due to the presence of polyunsaturated acids in its composition. For best efficiency and/or increasing the stability of vegetable oils pharmacologically active, nanoestructured systems are developed to vehicle this type of substance. This study aimed to develop and characterize nanostructured systems containing linseed oil. Polymeric nanocapsules, and nanoemulsions were prepared, evaluating two oil concentrations (1.5% and 3.0%) in both formulations and two polymers, Poli(ε-caprolactona) e Eudragit ® RL100, of the nanocapsules development. Both formulations showed appropriate properties for colloidal systems. Regarding the nanoemulsions, there was a significant difference in characteristics between the amounts of oil, while 1.5% linseed oil was the most satisfying concentration. About presence of polymers, there was variation only of zeta potential and pH values. In conclusion, the formulations were considered suitable for the encapsulation of the linseed oil, being promising carriers for other active substances.
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