Abstract

Essential oils are odorant liquid oily products consisting of a complex mixture of volatile compounds obtained from a plant raw material. They have been increasingly proven to act as potential natural agents in the treatment of several human conditions, including diabetes mellitus (DM). DM is a metabolic disorder characterized by chronic hyperglycemia closely related to carbohydrate, protein and fat metabolism disturbances. In order to explore novel approaches for the management of DM our group proposes the encapsulation of sucupira essential oil, obtained from the fruits of the Brazilian plants of the genus Pterodon, in nanostructured lipid carriers (NLCs), a second generation of lipid nanoparticles which act as new controlled drug delivery system (DDS). Encapsulation was performed by hot high-pressure homogenization (HPH) technique and the samples were then analyzed by dynamic light scattering (DLS) for mean average size and polydispersity index (PI) and by electrophoretic light scattering (ELS) for zeta potential (ZP), immediately after production and after 24 h of storage at 4 °C. An optimal sucupira-loaded NLC was found to consist of 0.5% (m/V) sucupira oil, 4.5% (m/V) of Kollivax® GMS II and 1.425% (m/V) of TPGS (formulation no. 6) characterized by a mean particle size ranging from 148.1 ± 0.9815 nm (0 h) to 159.3 ± 9.539 nm (at 24 h), a PI from 0.274 ± 0.029 (0 h) to 0.305 ± 0.028 (24 h) and a ZP from −0.00236 ± 0.147 mV (at 0 h) to 0.125 ± 0.162 (at 24 h). The encapsulation efficiency and loading capacity were 99.98% and 9.6%, respectively. The optimized formulation followed a modified release profile fitting the first order kinetics, over a period of 8 h. In vitro cytotoxicity studies were performed against Caco-2 cell lines, for which the cell viability above 90% confirmed the non-cytotoxic profile of both blank and sucupira oil-loaded NLC.

Highlights

  • Essential oils (EOs) are odorant liquid oily products, consisting of a complex mixture of lipophilic and volatile compounds obtained from a plant raw material by one of three distinct procedures: Dry distillation, driving by steam of water or suitable mechanical method without heating [1,2,3,4,5,6]

  • A suitable lipid blend requires (i) the solubility of the active compound in lipid matrix to attempt lipid incorporation into lipid nanoparticles, ensuring proper drug loading capacity and encapsulation efficiency; (ii) a major spatial incompatibility of liquid and solid lipids molecules, wherein the oil molecules have no active participation in the solid crystalline matrix of the solid lipid and solid lipid crystals, in turn, are not dissolved in the oil; (iii) stability of lipid phase to chemical degradation; (iv) biodegradable lipids, capable to produce nanometric particles; and (v) an acceptable toxicological profile, with no production of toxic residues along nanostructured lipid carriers (NLCs) production process [36,39]

  • We found out that lipid mixtures having sucupira oil and Imwitor® 900 K or Kollivax® GMS II may be used in sucupira oil-loaded NLC

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Summary

Introduction

Essential oils (EOs) are odorant liquid oily products, consisting of a complex mixture of lipophilic and volatile compounds obtained from a plant raw material by one of three distinct procedures: Dry distillation, driving by steam of water or suitable mechanical method without heating [1,2,3,4,5,6] Among their most abundant constituents, terpenes, sesquiterpenes and flavonoids are receiving increasing attention as potential natural agents for the treatment of several human diseases [7,8,9,10,11,12,13,14,15] (e.g., rheumatoid arthritis and other inflammatory diseases, cardiovascular diseases, diabetes and metabolic syndrome [16,17,18]). DM type 1 or insulin-dependent diabetes mellitus (T1DM or IDDM)

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