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A remodeled ivermectin polycaprolactone-based nanoparticles for inhalation as a promising treatment of pulmonary inflammatory diseases

Mohammed et al., European Journal of Pharmaceutical Sciences, doi:10.1016/j.ejps.2024.106714
Jan 2024  
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Ivermectin for COVID-19
4th treatment shown to reduce risk in August 2020
*, now known with p < 0.00000000001 from 100 studies, recognized in 22 countries.
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In Vitro and rat study showing that an optimized polycaprolactone-based nanoparticle formulation of ivermectin for inhalation had improved lung deposition, bioavailability, and anti-inflammatory effects compared to oral ivermectin. Authors prepared and optimized ivermectin-loaded nanoparticles using solvent evaporation and Box-Behnken design. In rats, inhaled nanoparticles achieved 5-fold higher lung and 3-fold higher plasma AUC versus oral ivermectin. Nanoparticles reduced proinflammatory cytokines IL-6, IL-10, IL-13, TNF-α and markers indicating lung injury. High dose inhaled ivermectin was safe and effective in reducing inflammation, suggesting potential for treating lung diseases like COVID-19.
7 studies investigate novel formulations of ivermectin for improved efficacy Albariqi, Albariqi (B), Chaccour, Errecalde, Mansour, Mohammed, Saha
Mohammed et al., 30 Jan 2024, USA, peer-reviewed, 4 authors. Contact:
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A remodeled ivermectin polycaprolactone-based nanoparticles for inhalation as a promising treatment of pulmonary inflammatory diseases
Nagia Sabaa Wafiq Mohammed, Nagia Ahmed El-Megrab, Azza A Hasan, Eman Gomaa
European Journal of Pharmaceutical Sciences, doi:10.1016/j.ejps.2024.106714
In recent years, ivermectin (IVM), an antiparasitic drug of low water solubility and poor oral bioavailability, has shown a profound effect on inflammatory mediators involved in diseases, such as acute lung injury, lung fibrosis, and COVID-19. In order to maximize drug bioavailability, polymeric nanoparticles can be delivered through nebulizers for pulmonary administration. The aim of this study was to prepare IVMloaded polycaprolactone (PCL) nanoparticles (NPs) by solvent evaporation method. Box-Benkhen design (BBD) was used to optimize entrapment efficiency (Y 1 ), percent drug release after 6 h (Y 2 ), particle size (Y 3 ), and zeta potential (Y 4 ). A study was conducted examining the effects of three independent variables: PCL-IVM ratio (A), polyvinyl alcohol (PVA) concentration (B), and sonication time (C). The optimized formula was also compared to the oral IVM dispersion for lung deposition, in-vivo behavior, and pharmacokinetic parameters. The optimized IVM-PCL-NPs formulation was spherical in shape with entrapment efficiency (% EE) of 93.99 ± 0.96 %, about 62.71 ± 0.53 % released after 6 hours, particle size of 100.07 ± 0.73 nm and zeta potential of -3.30 ± 0.23 mV. Comparing the optimized formulation to IVM-dispersion, the optimized formulation demonstrated greater bioavailability with greater area under the curve AUC 0-t of 710.91 ± 15.22 μg .ml -1 .h for lung and 637.97 ± 15.43 μg .ml -1 .h for plasma. Based on the results, the optimized NPs accumulated better in lung tissues, exhibiting a twofold longer residence time (MRT 4.78 ± 0.55 h) than the IVM-dispersion (MRT 2.64 ± 0.64 h). The optimized nanoparticle formulation also achieved higher c max (194.90 ± 5.01 μg/ml), and lower k el (0.21 ± 0.04 h -1 ) in lungs. Additionally, the level of inflammatory mediators was markedly reduced. To conclude, inhalable IVM-PCL-NPs formulation was suitable for the pulmonary delivery and may be one of the most promising approaches to increase IVM bioavailability for the successful treatment of a variety of lung diseases.
Conflict of interest The authors report no conflicts of interest. Author contribution Sabaa
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