4.3 Article

Nanostructuring lipid carriers using Ridolfia segeturn (L.) Moris essential oil

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ELSEVIER
DOI: 10.1016/j.msec.2019.109804

关键词

Essential oil; Ridolfia segetum; Nanostructured lipid carriers; Hydrogel; Dermal delivery; Cytotoxicity

资金

  1. Fundacao para a Ciencia e a Tecnologia (FCT), Portuguese Agency for Scientific Research [016648, POCI-01-0145-FEDER-016648, Pest UID/NEU/04539/2013, POCI-01-0145-FEDER-007440, UID/NEU/04539/2013]

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The therapeutic potential of essential oils is widely recognized since antiquity, due to their antibacterial, anti fungal, anti-inflammatory and immuno-modulatory properties. In particular, their physicochemical characteristics, such as lipophilicity and permeation enhancement effect have sparked attention for the development of innovative lipid nanosystems. The present work aimed at developing a differentiated nanostructured lipid carrier (NLC) based formulation for topical application, using the Ridolfia segetum essential oil (REO), isolated by hydrodistillation from this Portuguese aromatic plant, with a dual key function, as active and simultaneously nanostructuring component of the nanoparticles. The incorporation of the essential oil in the solid lipid matrix, followed by the respective hot high-pressure homogenization, led to particles with a size of 143 +/- 5 nm, along with a polydispersity index of 0.21, a zeta potential of -16.3 +/- 0.6 mV, encapsulation efficacy of ca. 100% and loading capacity of 1.4%. A comprehensive physicochemical characterization of the lipid nanosystem, including morphology, structural, thermal and accelerated stability analysis confirmed its nanostructured nature. REO-NLC was further jellified for designing an appropriate semisolid topical dosage form. In vitro release, permeation and skin retention studies evidenced a sustained release behaviour and a reservoir-like effect, suitable for a prolonged topical delivery. Cytotoxicity studies, performed in fibroblasts and keratinocytes, revealed the biocompatibility of the developed formulations. This work highlights the critical role of REO as a multiaddressable compound, both as active pharmaceutical ingredient and nanostructuring agent, able to tailor the permeation enhancement profile of nanoparticles towards topical delivery purposes and concomitantly presenting a safety profile for cosmetic and/or pharmaceutical purposes.

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