Abstract
The nasal route has been used for many years for the local treatment of nasal diseases. More recently, this route has been gaining momentum, due to the possibility of targeting the central nervous system (CNS) from the nasal cavity, avoiding the blood−brain barrier (BBB). In this area, the use of lipid nanoparticles, such as nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN), in nasal formulations has shown promising outcomes on a wide array of indications such as brain diseases, including epilepsy, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and gliomas. Herein, the state of the art of the most recent literature available on in vitro studies with nasal formulations of lipid nanoparticles is discussed. Specific in vitro cell culture models are needed to assess the cytotoxicity of nasal formulations and to explore the underlying mechanism(s) of drug transport and absorption across the nasal mucosa. In addition, different studies with 3D nasal casts are reported, showing their ability to predict the drug deposition in the nasal cavity and evaluating the factors that interfere in this process, such as nasal cavity area, type of administration device and angle of application, inspiratory flow, presence of mucoadhesive agents, among others. Notwithstanding, they do not preclude the use of confirmatory in vivo studies, a significant impact on the 3R (replacement, reduction and refinement) principle within the scope of animal experiments is expected. The use of 3D nasal casts to test nasal formulations of lipid nanoparticles is still totally unexplored, to the authors best knowledge, thus constituting a wide open field of research.
Highlights
IntroductionDifferent strategies have been investigated to increase the drug passage through the blood−brain barrier (BBB), such as electromagnetic force-field techniques and mini-pump-assisted intracranial delivery
The results showed that the fungal growth inhibition was significant at concentrations above 0.5 μg/mL, for the yeast-extract peptone dextrose medium, with a growth inhibition of 92% for ketoconazole-loaded nanostructured lipid carriers (NLC) and 50% for ketoconazole solution
The results showed that there was no significant change between the NLC formulation and the pure drug, indicating that pioglitazone-loaded NLC is safe for neuronal cells
Summary
Different strategies have been investigated to increase the drug passage through the BBB, such as electromagnetic force-field techniques and mini-pump-assisted intracranial delivery. These methods are invasive and can lead to the passage of toxins to the brain, being nonselective and neurotoxic [9,10,11]. It is essential to find new ways to avoid the need to bypass the BBB to target drugs to the brain In this area, intranasal administration has emerged as the only direct drug delivery route to the brain via the olfactory and trigeminal nerves, without the need to pass into the systemic circulation and cross the BBB. The use of in vitro nasal cavity and computational models to predict the in vivo performance of nasal formulations is reported
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