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Nanoemulsions Containing a Coumarin-Rich Extract from Pterocaulon balansae (Asteraceae) for the Treatment of Ocular Acanthamoeba Keratitis

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Abstract

This study describes the incorporation of a coumarin-rich extract from Pterocaulon balansae into nanoemulsions intended for the local treatment of ocular keratitis caused by Acanthamoeba. The n-hexane dewaxed extract of P. balansae was characterized by HPLC/PDA and UPLC/MS. The presence of four major coumarins was detected, where 5-methoxy-6,7-methylenedioxycoumarin was selected as a chemical marker. This extract was then incorporated into nanoemulsions composed of medium chain triglycerides and egg-lecithin, through spontaneous emulsification. Such a procedure yielded the formation of monodisperse nanoemulsions in a sub-300-nm range, regardless of the amount of extract incorporated (1.0–5.0 mg/mL). The amoebicidal activity against Acanthamoeba castellanii was both dose-dependent and incubation time-dependent. A reduction of 95% of trophozoite viability was detected after 24 h of incubation with a nanoemulsion at 1.25 mg/mL of coumarins, being a similar effect detected for chlorhexidine. These results suggest a potential of the formulations developed in this study as a new strategy for the treatment of ocular keratitis caused by Acanthamoeba.

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Acknowledgments

The authors want to thank the Brazilian Federal Agency for the Support and Evaluation of Graduate Education (CAPES) and National Council for Scientific and Technological Development (CNPq) for the financial support. L.P. wishes to thank CAPES for her Graduate fellowship. G.Z. wishes to thank the CNPq (Programa Jovens Talentos—grant number 028/2012) for his postdoctoral grant.

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Authors and Affiliations

  1. Faculty of Pharmacy, Federal University of Rio Grande do Sul, 2752 Ipiranga, 90610-000, Porto Alegre, Brazil

    Lua Ferreira Panatieri, Nathalya Tesch Brazil, Kathrin Faber, Bruna Medeiros-Neves, Gilsane Lino von Poser, Giovanni Konat Zorzi & Helder Ferreira Teixeira

  2. Institute of Basic Health Sciences, 500 Sarmento Leite, 90050-170, Porto Alegre, Brazil

    Marilise Brittes Rott

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  1. Lua Ferreira Panatieri
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Correspondence to Helder Ferreira Teixeira.

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Panatieri, L.F., Brazil, N.T., Faber, K. et al. Nanoemulsions Containing a Coumarin-Rich Extract from Pterocaulon balansae (Asteraceae) for the Treatment of Ocular Acanthamoeba Keratitis. AAPS PharmSciTech 18, 721–728 (2017). https://doi.org/10.1208/s12249-016-0550-y

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