Characterization of solid lipid nanoparticles produced with carnauba wax for rosmarinic acid oral delivery

Abstract

In the last decade, research studies have increased on the development of delivery systems for polyphenols, for protection, improvement of stability and increase of their bioavailability. Rosmarinic acid is a polyphenol with described bioactivities, such as antioxidant, anti-mutagenic, anti-bacterial and anti-viral capabilities. Thus, the aim of this research work was to produce stable solid lipid nanoparticles (SLN) using carnauba wax as lipidic matrix, for delivery of rosmarinic acid, to be further incorporated into food matrices.Hence, different concentrations of wax (0.5, 1 and 1.5%, w/v) and percentages of surfactant (1, 2 and 3%, v/v) were tested. Physical properties, surface morphology and association efficiencies were studied at time of production and after 28 day at refrigerated storage. Thermal properties and the nature of the chemical interactions between the lipids waxes and rosmarinic acid were also evaluated. The particles showed range size between 35-927 nm and zeta potentials of ca. À38 to 40, showing high stability, with no risk of aggregation due to electric repulsion of SLN. High association efficiencies % (ca. 99%) were obtained. FTIR analyses proved the association of rosmarinic acid and lipidic matrix. The low lipid and high surfactant concentrations leads to small SLN. The surfactant, polysorbate 80 decreases the interfacial tension in the SLN surfaces, preventing aggregation, leading to the development of small particles. These properties were maintained throughout the 28 day of refrigerated storage, and no rosmarinic acid was released by the particles during refrigeration, indicating good compatibility between rosmarinic acid and the waxy core of SLN. The optimum range values to obtain the desirable features for incorporation in a functional food suggest formulations containing 1.0 and 1.5% (w/v) of lipid and 2% (v/v) of surfactant.

Safety profile of solid lipid nanoparticles loaded with rosmarinic acid for oral use: in vitro and animal approaches

“…First, the values related to the physical properties of SLN were in accordance to those obtained in previous works, [6][7][8] showing that the entrapment of RA and herbal extract in SLN induced an increase in particle size. The polydispersity index and zeta potential indicate SLN stability in solution and absence of agglomeration.…”

“…High AE percentages in SLN were found, in accordance with the ones obtained in previous works. [6][7][8] The RA Figure 6 Representative TEM images of spleen, EWAT, small intestine, and cecum tissue samples of rats after 14 d of oral treatments: control (vehicle-treated) rats; rats treated with Witepsol (WSLN-RA10) and with Carnauba (WSLN-RA10) SLN loaded with RA (10 mg/kg bw/d).…”

“…[6][7][8] Witepsol and Carnauba waxes were used to produce these systems. Witepsol is a synthetic wax usually not only used in the pharmaceutical industry as excipient but also approved for human consumption; Carnauba wax (also named Brazilian wax) is naturally extracted from the leaves of a particular palm tree known as Copernicia cerifera, a plant native to the northeast of Brazil.…”

Superoxide Dismutase-Loaded Solid Lipid Nanoparticles Prepared by Cold Homogenization Method: Characterization and Permeation Study Through Burned Rat Skin

“…All formulations demonstrated CI% below 30%. Hence, low value of CI% leads to slower drug release and means that lower energy is required to melt the crystal lipids (22). Therefore, low amount of CI% is sufficiently low to ensure the sustained release of SOD, yet isn't sufficiently high to make sure SLN stability.…”

Olive-oil nanocapsules stabilized by HSA: influence of processing variables on particle properties

“…Liquid lipid nanocapsules (LLN) constitute a new generation of nanoparticulate drug-delivery systems offering major advantages such as higher degree of biocompatibility and versatility (Roger et al 2009;Madureira et al 2015;Anton et al 2008). These nanocarriers can load drugs, vaccines, diagnostics, and nutraceuticals to be administered by different routes (topical, oral, pulmonary, or parenteral).…”