Rutin-Loaded Solid Lipid Nanoparticles: Characterization and In Vitro Evaluation.

Alessia Irrera,Vincenza Crupi,Domenico Majolino,Valentina Venuti,Cinzia Anna Ventura,Federica De Gaetano,Barbara Testagrossa,Giuseppe Acri,Silvana Tommasini,Donatella Paolino,Maria Chiara Cristiano,Giuseppe Paladini,Rosanna Stancanelli

doi:10.3390/molecules26041039

Abstract

This study was aimed at preparing and characterizing solid lipid nanoparticles loading rutin (RT-SLNs) for the treatment of oxidative stress-induced diseases. Phospholipon 80H® as a solid lipid and Polysorbate 80 as surfactant were used for the SLNs preparation, using the solvent emulsification/diffusion method. We obtained spherical RT-SLNs with low sizes, ranging from 40 to 60 nm (hydrodynamic radius) for the SLNs prepared starting from 2% and 5% (w/w) theoretical amount. All prepared formulations showed negative zeta-potential values. RT was efficiently encapsulated within SLNs, obtaining high encapsulation efficiency and drug content percentages, particularly for SLNs prepared with a 5% theoretical amount of RT. In vitro release profiles and analysis of the obtained data applying different kinetic models revealed Fickian diffusion as the main mechanism of RT release from the SLNs. The morphology of RT-SLNs was characterized by scanning electron microscopy (SEM), whereas the interactions between RT and the lipid matrix were investigated by Raman spectroscopy, evidencing spectral modifications of characteristic bands of RT due to the establishment of new interactions. Finally, antioxidant activity assay on human glioblastoma astrocytoma (U373) culture cells showed a dose-dependent activity for RT-SLNs, particularly at the highest assayed dose (50 μM), whereas the free drug showed the lesser activity.

Highlights

In recent years, various drug delivery systems have been developed with the aim of overcoming the limitations that represent the failure of conventional pharmaceutical dosage forms, such as the poor solubility of the drug in biological fluids or the insufficient plasmatic concentration of drug due to poor absorption, rapid metabolism, and elimination
The morphology of RT-solid lipid nanoparticles (SLNs) was characterized by scanning electron microscopy (SEM), whereas the interactions between RT and the lipid matrix were investigated by Raman spectroscopy, evidencing spectral modifications of characteristic bands of RT due to the establishment of new interactions
As a matter of fact, since only a fixed amount of drug can be incorporated in a given amount of lipid, the increase of initial drug concentration requires an increase in the quantity of lipid in the nanodroplets, which will give rise to larger SLNs

Summary

Introduction

Various drug delivery systems have been developed with the aim of overcoming the limitations that represent the failure of conventional pharmaceutical dosage forms, such as the poor solubility of the drug in biological fluids or the insufficient plasmatic concentration of drug due to poor absorption, rapid metabolism, and elimination. Colloidal systems formed by polymeric or lipidic substances, such as nanoparticles, nanoemulsions, and liposomes, have aroused most of the interest in pharmaceutical technology [1,2]. If compared to traditional colloidal carriers, SLNs exhibit great potential as suitable drug delivery systems [6,7,8,9] thanks to their low toxicity, large surface area, prolonged drug release, superior cellular uptake, as well as capability to improve solubility and the bioavailability of drugs [10,11]. Compared to polymeric nanoparticles, SLNs have the advantage of being biocompatible and biodegradable [12,13,14,15,16,17]

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