Abstract
Thymoquinone (TQ), the main active constituent of Nigella sativa, has demonstrated broad-spectrum antimicrobial, antioxidant, and anti-inflammatory effects, which suggest its potential use in secondary infections caused by COVID-19. However, clinical deployment has been hindered due to its limited aqueous solubility and poor bioavailability. Therefore, a targeted delivery system to the lungs using nanotechnology is needed to overcome limitations encountered with TQ. In this project, a novel TQ-loaded poly(ester amide) based on L-arginine nanoparticles was prepared using the interfacial polycondensation method for a dry powder inhaler targeting delivery of TQ to the lungs. The nanoparticles were characterized by FTIR and NMR to confirm the structure. Transmission electron microscopy and Zetasizer results confirmed the particle diameter of 52 nm. The high-dose formulation showed the entrapment efficiency and loading capacity values of TQ to be 99.77% and 35.56%, respectively. An XRD study proved that TQ did not change its crystallinity, which was further confirmed by the DSC study. Optimized nanoparticles were evaluated for their in vitro aerodynamic performance, which demonstrated an effective delivery of 22.7–23.7% of the nominal dose into the lower parts of the lungs. The high drug-targeting potential and efficiency demonstrates the significant role of the TQ nanoparticles for potential application in COVID-19 and other respiratory conditions.
Highlights
COVID-19 has caused an emergent pandemic that has resulted in an extraordinary worldwide health crisis [1,2]
An X-ray Diffraction (XRD) study proved that TQ did not change its crystallinity, which was further confirmed by the Differential Scanning Calorimetry (DSC) study
It is characterized by inflammation, oxidation, and an exaggerated immune response, which in some cases can progress into a cytokine storm, which may develop into acute respiratory distress syndrome (ARDs) [3]
Summary
COVID-19 has caused an emergent pandemic that has resulted in an extraordinary worldwide health crisis [1,2]. The lungs are an attractive drug delivery route owing to their additional advantages, including the large surface area, thin epithelial layer, and high vascularization, which allows significant absorption of the inhaled dosage forms Such properties allow for lower doses to be delivered, and reduced side effects [20,21]. Polymeric nanoparticles have attracted great attention as a potential drug delivery system to the lungs because they can efficiently deliver a wide range of therapeutic molecules to the targeted area within the respiratory system [22–24]. These fine particles can augment the rate and extent of dissolution of sparingly soluble drugs. This may lead to a decrease in peripheral side effects
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