Abstract

The intranasal administration of nanostructured lipid carriers (NLCs) has been suggested as a promising strategy to improve the fast treatment of epilepsy. This route allows for drug passage directly from the nose to the brain, avoiding the need of bypassing the blood–brain barrier. In addition, the quality-by-design (QbD) approach is a useful tool for the optimization of manufacturing variables, resulting in effective and safe pharmaceutical formulations. The aim of this work was to use the QbD approach to optimize a NLCs formulation for the nose-to-brain delivery of diazepam. The studies began with the screening of excipients and the assessment of the lipid-drug compatibility. The central composite design was used to evaluate the effects of critical material attributes (CMAs) (ratio of solid and liquid lipids and the amount of drug and emulsifiers) on the CQAs of the diazepam-loaded NLCs formulation (particle size, polydispersity index (PDI), zeta potential (ZP) and encapsulation efficiency (EE)). The results showed that the most adequate ratios of lipids and emulsifiers were 6.65:2.85 and 4.2:0.3 (%, w/w), with values of 84.92 nm, 0.18, −18.20 mV and 95.48% for particle size, PDI, ZP and EE, respectively. This formulation was selected for further studies related to the optimization of critical process parameters (CPPs).

Highlights

  • Precirol® 5 ATO and Cetiol® V were selected as the solid lipid (SL) and the liquid lipid (LL), respectively

  • Tween 80® and sodium deoxycholate were selected as emulsifiers and a drug concentration of 0.50% was selected to prepare the diazepam-loaded nanostructured lipid carriers (NLCs) formulation (Table 1)

  • Optimizing NLCs formulations is critical to achieve a reproducible quality of the final pharmaceutical products, in terms of both efficacy and safety

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Summary

Introduction

Neurological disorders, including epilepsy, require a rapid and effective treatment targeting the brain. In this area, the intranasal administration of lipid nanosystems, such as nanostructured lipid carriers (NLCs) has been suggested as a promising strategy. The quality-by-design (QbD) approach has been applied to optimize NLCs formulations, improving the manufacturing processes and ensuring the quality and safety of the final products. The aim of this work was to use the QbD approach to optimize a NLCs formulation for the nose-to-brain delivery of diazepam, improving epilepsy emergency treatment. The QbD approach was applied to evaluate the effects of CMAs on CQAs in the diazepam-loaded NLCs formulation

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