Abstract

Context: Nanotechnology can be applied to deliver and protect antioxidants in order to control the oxidative stress phenomena in several chronic pathologies. Chitosan (CS) nanoparticles are biodegradable carriers that may protect antioxidants with potent biological activity such as rosmarinic acid (RA) in Salvia officinalis (sage) and Satureja montana (savory) extracts for safe and innovative therapies.Objective: Development and characterization of CS nanoparticles as a stable and protective vehicle to deliver RA for medical applications using natural extracts as sage and savory.Materials and methods: Antioxidant-CS based nanoparticles were prepared by ionic gelation with sodium tripolyphosphate (TPP), at pH 5.8 with a mass ratio of 7:1 (CS:TPP), with a theoretical antioxidant-CS loading of 40–50%. The nanoparticles were then characterized by different methods such as photon correlation spectroscopy, laser Doppler anemometry, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR), high-performance liquid chromatographic (HPLC), association efficiency, and antioxidant activity.Results and discussion: Individual and small sizing nanoparticles, around 300 nm, were obtained. SEM confirmed smooth and spherical nanoparticles after freeze-drying. No chemical interactions were found between antioxidants and CS, after encapsulation, by DSC and FTIR. The association efficiency was 51.2% for RA (with 40% loading) and 96.1 and 98.2% for sage and savory nanoparticles, respectively (both with 50% loading). Antioxidant activity values were higher than 0.0348 eq [Asc. Ac.] g/L/g extract and 0.4251 µmol/eq Trolox/g extract.Conclusion: The extracts under study are promising vehicles for RA drug delivery in CS nanocarriers.

Highlights

  • The nanoparticles were characterized by different methods such as photon correlation spectroscopy, laser Doppler anemometry, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR), high-performance liquid chromatographic (HPLC), association efficiency, and antioxidant activity

  • There are no reports in the literature that have demonstrated the good performance of CS nanoparticles to incorporate these extracts in order to bring the huge benefits of rosmarinic acid (RA) antioxidant, as well as, other compounds that may act synergistically

  • Zeta potential values of ±30 mV indicate that the colloidal system is stable in time and that amino groups of CS are on the surface, which is documented in some similar studies of antioxidants encapsulation in CS nanoparticles (Harris et al, 2011)

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Summary

Introduction

Salvia officinalis and Satureja montana (sage and savory, respectively) are plants often used in the traditional medicine to improve digestion (Giao et al, 2009), as an disinfectant (Djenane et al, 2011), to decrease blood pressure (Petersen & Simmonds, 2003), to prevent premature ejaculation (Zavatti et al, 2011), to treat neuropathy (Abada et al, 2011), urinary and pulmonary infections (Cardilea et al, 2009), and other diseases such as Alzheimer’s disease (Zhoua et al, 2011) and cancer (Cardilea et al, 2009) Some of these biological activities have been associated with its high contents in RA (Giao et al, 2009; Shahidi et al, 1992; Skoula et al, 2000). Among the different approaches explored so far, colloidal carriers of particular interest, especially those made of mucoadhesive polymers, assure drug time retention at the absorption site (Campos et al, 2004) For this application, chitosan (CS) has become of interesting for the association and delivery of labile macromolecular compounds (Silva et al, 2011). There are no reports in the literature that have demonstrated the good performance of CS nanoparticles to incorporate these extracts in order to bring the huge benefits of RA antioxidant, as well as, other compounds that may act synergistically

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