Abstract

Nanosystems used in pharmaceutical formulations have shown promising results in enhancing the administration of drugs of difficult formulations. In particular, porous silica nanoparticles have demonstrated excellent properties for application in biological systems; however, there are still several challenges related to the development of more effective and biocompatible materials. An interesting approach to enhance these nanomaterials has been the development of nanoantioxidant carriers. In this work, a hybrid nanoantioxidant carrier based on porous silica nanoplatform with rosmarinic acid antioxidant immobilized on its surface were developed and characterized. Techniques such as dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), N2 adsorption–desorption measurements, differential scanning calorimetry (DSC), Fourier transform–infrared spectroscopy (FT-IR), and 2,2-diphenyl-1-picrylhydrazyl (DPPH●) assay were used to characterize and evaluate the antioxidant activity of nanocarriers. In addition, drug release profile was evaluated using two biorelevant media. The antioxidant activity of rosmarinic acid was maintained, suggesting the correct disposition of the moiety. Kinetic studies reveal that more morin is released in the simulated intestinal fluid than in the gastric one, while an anomalous non–Fickian release mechanism was observed. These results suggest a promising antioxidant nanocarrier suitable for future application in drug delivery.

Highlights

  • Great advancements in the area of nanomaterials have brought about opportunities to improve various processes in fields related to engineering, food industry, biomedicine, and the pharmaceutical industry, among others [1,2,3]

  • Employing similar protocols to those previously reported, the rosmarinic acid (RA), an ester derived from a hydroxycinnamic acid, was successfully attached onto amino-functionalized mesoporous silica nanoparticles through an amide bond between the carboxylic acid of RA and APTES amino group on the surface of the nanoparticles (Figure 1a)

  • A hybrid nanoantioxidant carrier based on porous silica nanoplatform with rosmarinic acid antioxidant immobilized on its surface was successfully development and characterized

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Summary

Introduction

Great advancements in the area of nanomaterials have brought about opportunities to improve various processes in fields related to engineering, food industry, biomedicine, and the pharmaceutical industry, among others [1,2,3]. The metal-phenolic networks approach [18] or covalent immobilization could overcome these drawbacks, generating a better pharmaceutical excipient (for non-porous particles) or, in the case of carrier particles, a better pharmaceutical vehicle The latter ones, in general, are hybrid materials inspired by the carrier properties of inorganic nanoplatforms with functionalized antioxidants on the surface. Arriagada and colleagues developed core-shell mesoporous silica nanospheres functionalized with caffeic acid, showing the ability of the antioxidant nanomaterial to protect oxidation-sensitive molecules [21] These types of nanoantioxidant attempt to generate more effective and biocompatible materials, by using natural polyphenols to coat nanoparticles and by releasing biomolecules with potential pharmacological activity, such as flavonoids

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