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

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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.

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Acknowledgements

The authors wish to thank C. B. da Silva for Zetasizer access and CNPq (Process number: 456863/2014-1) for the financial support.

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Authors and Affiliations

  1. Laboratório de Tecnologia Farmacêutica, Programa de Pós-graduação em Ciências Farmacêuticas, Centro de Ciências da Saúde, Departamento de Farmácia Industrial, Universidade Federal de Santa Maria, Santa Maria, 97105-900, Brazil

    Marila C. L. Marchiori, Cristina Rigon & Letícia Cruz

  2. Centro Universitário Franciscano, Santa Maria, Brazil

    Priscila M. Copetti & Michele R. Sagrillo

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  1. Marila C. L. Marchiori
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  2. Cristina Rigon
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Correspondence to Letícia Cruz.

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Marchiori, M.C.L., Rigon, C., Copetti, P.M. et al. Nanoencapsulation Improves Scavenging Capacity and Decreases Cytotoxicity of Silibinin and Pomegranate Oil Association. AAPS PharmSciTech 18, 3236–3246 (2017). https://doi.org/10.1208/s12249-017-0810-5

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  • DOI: https://doi.org/10.1208/s12249-017-0810-5

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