Abstract

Rutin is a flavonoid compound obtained from different vegetables and fruits; specifically, it is found in the seeds of buckwheat and in fruit peels, particularly citrus. It is also an important constituent of red wine. Rutin exhibits various biological properties including antiviral, vasoprotective, anti-inflammatory, and anticarcinogenic activities. However, its antioxidant activity is the most well studied. Despite the potential for in vitro applications, rutin presents low oral bioavailability that affects its biological activities. Nanoparticles composed of polymers, protein, or lipids are of great importance in the pharmaceutical and nutraceutical areas due to their physicochemical properties, which improve the pharmacokinetics of the drug which is loaded within. This study presents the production of bovine serum albumin (BSA) nanoparticles containing rutin by nano spray drying. Nanoparticles were characterized in terms of mean particle size, size distribution, morphology, zeta potential, and drug content; as well as their antioxidant activity. The optimized spray-drying conditions produced spherical particles with a mean size of 316 nm, zeta potential of −32 mV, and encapsulation efficiency around 32%. Moreover, when antioxidant activity toward the ABTS+ radical was assayed, nanoencapsulation increased the IC50 of rutin by 2-fold. The nano spray-drying process proved to be suitable for the production of rutin-loaded BSA nanoparticles with potential antioxidant activity.

Highlights

  • Rutin (3,3’,4’,5,7-Pentahydroxyflavone 3-rutinoside) is a naturally occurring flavonoid found in the floral buds of Sophora japonica L. and in buckwheat and fruit peels, especially those of citrus fruits

  • Ethanol (99.8%) was purchased from Vetec-QuímicaFina (Brazil), methanol was purchased from Merck® (Germany), phosphate buffered saline (PBS) pH 7.4 was obtained from Sigma-Aldrich

  • The Nanospray-Dryer B-90 used in this study is one of a new generation of spray dryers developed for nanoparticle formulation (Lee et al, 2011; Panda et al, 2016; Pérez-Masiá et al, 2015)

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Summary

Introduction

Rutin (3,3’,4’,5,7-Pentahydroxyflavone 3-rutinoside) is a naturally occurring flavonoid found in the floral buds of Sophora japonica L. and in buckwheat and fruit peels, especially those of citrus fruits (orange, grapefruit, lemon, and lime). This compound is an important constituent of red wine. Various nanoencapsulation techniques have been reported, including emulsification, nanoprecipitation, desolvation, and spray drying. It is often used for dehydration of samples, spray drying can be used as a method of encapsulation in order to trap active materials within an inert matrix (Tewa-Tagne, Briançon, Fessi, 2007).

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