Development of nanoemulsions for the delivery of clofazimine to macrophages and immunomodulation evaluation
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Date
2022-06-27
Authors
Mata Casimiro, Luis Daniel
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Abstract
The lung is the organ in charge of the gas exchange process in our bodies. This means that it is exposed to external stimuli the whole time. These interactions with foreign matter can shift the internal equilibrium of this organ towards pathogenesis, which can result in the inflammations of the lungs, which in turn limits the airflow. Unfortunately, the administration of corticosteroids for the treatment of inflammation has been associated with the development of diseases like osteoporosis, diabetes, etc. Therefore, we propose the development of O/W Nanoemulsions for the delivery of Clofazimine, a BCS class II drug with anti-inflammatory and anti-bacterial properties, to a macrophage model and evaluate its immunomodulation effect. The solubility of CFZ was investigated in different oils prior to the development of the formulations by applying design of experiments and microfluidics technology. The Nanoemulsions were characterized in terms of size, Pdi, zeta potential, filterability, and endotoxin content before investigating their safety profile and anti-inflammatory properties in vitro. The results demonstrated that the mixture of Sesame oil with MCT can solubilize ~13 mg/mL of CFZ and the application of DoE allow us to obtain NE of different sizes which show great repeatability in terms of size and Pdi. Furthermore, they preserve ≥70% of cell viability at concentrations ≤1 mg/mL and diminish the amount of cytokine secretion in a macrophage-like cell model.
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Keywords
Lung-inflammation, Nanoemulsions, Drug delivery, Nanomedicine