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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.
No treatment is 100% effective. Protocols combine complementary and synergistic treatments. * >10% efficacy in meta analysis with ≥3 clinical studies.
3,800+ studies for 60+ treatments. c19ivm.org
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: sabaawafiq@gmail.com.
This PaperIvermectinAll
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
References
Abbas, Labbez, Nordholm, Ahlberg, Size-Dependent Surface Charging of Nanoparticles, The Journal of Physical Chemistry C, doi:10.1021/jp709667u
Ahmed, Ibrahim, Samy, Kaseem, Nutan et al., Biodegradable injectable in situ implants and microparticles for sustained release of montelukast: in vitro release, pharmacokinetics, and stability, AAPS PharmSciTech, doi:10.1208/s12249-014-0101-3
Al-Mazidi, Alotaibi, Nedjadi, Chaudhary, Alzoghaibi et al., Blocking of cytokines signalling attenuates evoked and spontaneous neuropathic pain behaviours in the paclitaxel rat model of chemotherapy-induced neuropathy, European Journal of Pain, doi:10.1002/ejp.1169
Allam, Hamdallah, Abdallah, Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation, International journal of nanomedicine, doi:10.2147/IJN.S139706
Alshehri, Imam, Formulation and evaluation of butenafine loaded PLGA-nanoparticulate laden chitosan nano gel, Drug Delivery, doi:10.1080/10717544.2021.1995078
Alshehri, Imam, Rizwanullah, Fakhri, Rizvi et al., Effect of chitosan coating on PLGA nanoparticles for oral delivery of thymoquinone: In vitro, ex vivo, and cancer cell line assessments, Coatings, doi:10.3390/coatings11010006
Aminu, Audu, Polycaprolactone-based nanoparticles for advanced therapeutic applications, Polymeric Nanosystems, doi:10.1016/B978-0-323-85656-0.00003-6
Ayoub, Elantouny, El-Nahas, Ghazy, Injectable PLGA Adefovir microspheres; the way for long term therapy of chronic hepatitis-B, European journal of pharmaceutical sciences, doi:10.1016/j.ejps.2018.03.016
Ayoub, Jasti, Elantouny, Elnahas, Ghazy, Comparative study of PLGA in-situ implant and nanoparticle formulations of entecavir; in-vitro and in-vivo evaluation, Journal of Drug Delivery Science and Technology, doi:10.1016/j.jddst.2020.101585
Badran, Alanazi, Ibrahim, Alshora, Taha et al., Optimization of Bromocriptine-Mesylate-Loaded Polycaprolactone Nanoparticles Coated with Chitosan for Nose-to-Brain Delivery: In Vitro and In Vivo Studies, Polymers, doi:10.3390/polym15193890
Behera, Barik, Joshi, Shah, Formulation and evaluation of Rifampicin loaded poly-ε-caprolactone nano-particles using 3 2 factorial design, International Journal of Pharmaceutial Sciences And Research
Bhattacharya, Genotoxicity and in vitro investigation of Gefitinib-loaded polycaprolactone fabricated nanoparticles for anticancer activity against NCI-H460 cell lines, Journal of Experimental Nanoscience, doi:10.1080/17458080.2022.2060501
Bilati, Allémann, Doelker, Sonication Parameters for the Preparation of Biodegradable Nanocapsulesof Controlled Size by the Double Emulsion Method, Pharmaceutical Development and Technology, doi:10.1081/PDT-120017517
Blum, Saltzman, High loading efficiency and tunable release of plasmid DNA encapsulated in submicron particles fabricated from PLGA conjugated with poly-L-lysine, Journal of controlled release, doi:10.1016/j.jconrel.2008.04.002
Caly, Druce, Catton, Jans, Wagstaff, The FDA-approved drug ivermectin inhibits the replication of SARS-CoV-2 in vitro, Antiviral Research, doi:10.1016/j.antiviral.2020.104787
Chaccour, Abizanda, Irigoyen-Barrio, Casellas, Aldaz et al., Nebulized ivermectin for COVID-19 and other respiratory diseases, a proof of concept, doseranging study in rats, Scientific reports, doi:10.1038/s41598-020-74084-y
Chen, Wang, Preparation and characterization of atrazineloaded biodegradable PLGA nanospheres, Journal of Integrative Agriculture, doi:10.1016/S2095-3119(19)62613-4
Cui, Cun, Tao, Yang, Shi et al., Preparation and characterization of melittin-loaded poly (DL-lactic acid) or poly (DL-lactic-co-glycolic acid) microspheres made by the double emulsion method, Journal of Controlled Release, doi:10.1016/j.jconrel.2005.07.001
De Castro Jr, Gregianin, Burger, Continuous high-dose ivermectin appears to be safe in patients with acute myelogenous leukemia and could inform clinical repurposing for COVID-19 infection, Leukemia & Lymphoma, doi:10.1080/10428194.2020.1786559
Dua, Rapalli, Shukla, Singhvi, Shastri et al., Multi-drug resistant Mycobacterium tuberculosis & oxidative stress complexity: Emerging need for novel drug delivery approaches, Biomedicine & Pharmacotherapy, doi:10.1016/j.biopha.2018.08.101
Elmowafy, Alhakamy, Shalaby, Alshehri, Ali et al., Hybrid polylactic acid/Eudragit L100 nanoparticles: A promising system for enhancement of bioavailability and pharmacodynamic efficacy of luteolin, Journal of Drug Delivery Science and Technology, doi:10.1016/j.jddst.2021.102727
Esmaeili, Atyabi, Dinarvand, Preparation and characterization of estradiol-loaded PLGA nanoparticles using homogenization-solvent diffusion method, DARU Journal of Pharmaceutical Sciences
Fude, Dongmei, Anjin, Mingshi, Kai et al., Preparation and characterization of melittin-loaded poly (dl-lactic acid) or poly (dl-lactic-co-glycolic acid) microspheres made by the double emulsion method, Journal of Controlled Release, doi:10.1016/j.jconrel.2005.07.001
Fulzele, Chatterjee, Shaik, Jackson, Singh, Inhalation delivery and anti-tumor activity of celecoxib in human orthotopic non-small cell lung cancer xenograft model, Pharmaceutical research, doi:10.1007/s11095-006-9074-6
Garg, Singh, Bhatia, Raza, Singh et al., Systematic development of transethosomal gel system of piroxicam: formulation optimization, in vitro evaluation, and ex vivo assessment, AAPS pharmscitech, doi:10.1208/s12249-016-0489-z
Gilbert, Slechta, A Case of Ivermectin-Induced Warfarin Toxicity: First Published Report, Hospital Pharmacy, doi:10.1177/0018578718758972
Goel, Baboota, Sahni, Ali, Exploring targeted pulmonary delivery for treatment of lung cancer, International journal of pharmaceutical investigation
Guo, Dou, Li, Zhang, Bhutto et al., Ivermectionloaded solid lipid nanoparticles: preparation, characterisation, stability and transdermal behaviour, Artificial Cells, Nanomedicine, and Biotechnology, doi:10.1080/21691401.2017.1307207
Guzzo, Furtek, Porras, Chen, Tipping et al., Safety, tolerability, and pharmacokinetics of escalating high doses of ivermectin in healthy adult subjects, The Journal of Clinical Pharmacology, doi:10.1177/009127002237994
Habib, Sayed, Elsayed, Enhanced transdermal delivery of ondansetron using nanovesicular systems: fabrication, characterization, optimization and ex-vivo permeation study-Box-Cox transformation practical example, European journal of pharmaceutical sciences, doi:10.1016/j.ejps.2018.01.044
Haggag, Matchett, Dakir, Buchanan, Osman et al., Nanoencapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells, International journal of pharmaceutics, doi:10.1016/j.ijpharm.2017.02.006
Hernández-Giottonini, Rodríguez-Córdova, Gutiérrez-Valenzuela, Peñuñuri-Miranda, Zavala-Rivera et al., PLGA nanoparticle preparations by emulsification and nanoprecipitation techniques: Effects of formulation parameters, Rsc Advances, doi:10.1039/C9RA10857B
Hitzman, Elmquist, Wattenberg, Wiedmann, Development of a respirable, sustained release microcarrier for 5fluorouracil I: In vitro assessment of liposomes, microspheres, and lipid coated nanoparticles, Journal of pharmaceutical sciences, doi:10.1002/jps.20591
Ibraheem, Iqbal, Agusti, Fessi, Elaissari, Effects of process parameters on the colloidal properties of polycaprolactone microparticles prepared by double emulsion like process, Colloids and Surfaces A: Physicochemical and Engineering Aspects, doi:10.1016/j.colsurfa.2014.01.012
Ibrahim, Ayoub, El-Bassossy, El-Nahas, Gomaa, Investigation of Alogliptin-Loaded In Situ Gel Implants by 23 Factorial Design with Glycemic Assessment in Rats, Pharmaceutics, doi:10.3390/pharmaceutics14091867
Ichite, Chougule, Jackson, Fulzele, Safe et al., Enhancement of docetaxel anticancer activity by a novel diindolylmethane compound in human non-small cell lung cancer, Clinical Cancer Research, doi:10.1158/1078-0432.CCR-08-1558
Jahromi, Ghazali, Ashrafi, Azadi, A comparison of models for the analysis of the kinetics of drug release from PLGA-based nanoparticles, Heliyon, doi:10.1016/j.heliyon.2020.e03451
Jaques, Kim, Measurement of total lung deposition of inhaled ultrafine particles in healthy men and women, Inhalation toxicology, doi:10.1080/08958370050085156
Ji, Cen, Lin, Hu, Fang et al., Study on the subacute inhalation toxicity of ivermectin TC in rats, Chinese Journal of Comparative Medicine
Jiang, Klein, Niederacher, Du, Marx et al., C/T polymorphism of the intercellular adhesion molecule-1 gene (exon 6, codon 469). A risk factor for coronary heart disease and myocardial infarction, International journal of cardiology, doi:10.1016/S0167-5273(02)00138-9
Keum, Noh, Baek, Lim, Hwang et al., Practical preparation procedures for docetaxelloaded nanoparticles using polylactic acid-co-glycolic acid, International journal of nanomedicine, doi:10.2147/IJN.S24547
Laing, Gillan, Devaney, Ivermectin-old drug, new tricks?, Trends in parasitology, doi:10.1016/j.pt.2017.02.004
Lalan, Tandel, Lalani, Patel, Misra, Inhalation drug therapy: Emerging trends in nasal and pulmonary drug delivery, Novel Drug Delivery Technologies: Innovative Strategies for Drug Repositioning, doi:10.1007/978-981-13-3642-3
Laskin, Malaviya, Laskin, Role of Macrophages in Acute Lung Injury and Chronic Fibrosis Induced by Pulmonary Toxicants, Toxicological Sciences, doi:10.1093/toxsci/kfy309
Lauweryns, Baert, Alveolar clearance and the role of the pulmonary lymphatics, American Review of Respiratory Disease
Li, Zhan, Anti-parasite drug ivermectin can suppress ovarian cancer by regulating lncRNA-EIF4A3-mRNA axes, EPMA Journal, doi:10.1007/s13167-020-00209-y
Lu, Xiong, Sun, Yu, Hu et al., Sustained release ivermectin-loaded solid lipid dispersion for subcutaneous delivery: in vitro and in vivo evaluation, Drug delivery, doi:10.1080/10717544.2017.1284945
Ma, Xu, Wu, Li, Zhong et al., Ivermectin contributes to attenuating the severity of acute lung injury in mice, Biomedicine & Pharmacotherapy, doi:10.1016/j.biopha.2022.113706
Madelung, Østergaard, Bertelsen, Jørgensen, Jacobsen et al., Impact of sodium dodecyl sulphate on the dissolution of poorly soluble drug into biorelevant medium from drug-surfactant discs, International Journal of Pharmaceutics, doi:10.1016/j.ijpharm.2014.02.043
Mansour, Rhee, Wu, Nanomedicine in pulmonary delivery, International journal of nanomedicine, doi:10.2147/ijn.s4937
Mansour, Shamma, Ahmed, Sabry, Esmat et al., Safety of inhaled ivermectin as a repurposed direct drug for treatment of COVID-19: A preclinical tolerance study, International Immunopharmacology, doi:10.1016/j.intimp.2021.108004
Martin, Jans, Antivirals that target the host IMPα/β1-virus interface, Biochemical Society Transactions, doi:10.1042/BST20200568
Mehta, Bothiraja, Kadam, Pawar, Potential of dry powder inhalers for tuberculosis therapy: facts, fidelity and future, Artificial cells, nanomedicine, and biotechnology, doi:10.1080/21691401.2018.1513938
Nnamani, Hansen, Windbergs, Lehr, Development of artemether-loaded nanostructured lipid carrier (NLC) formulation for topical application, International Journal of Pharmaceutics, doi:10.1016/j.ijpharm.2014.10.004
Padhi, Mirza, Verma, Khuroo, Panda et al., Revisiting the nanoformulation design approach for effective delivery of topotecan in its stable form: an appraisal of its in vitro Behavior and tumor amelioration potential, Drug Delivery, doi:10.3109/10717544.2015.1105323
Patel, Raval, Manvar, Airao, Bhatt et al., Lung cancer targeting efficiency of Silibinin loaded Poly Caprolactone/Pluronic F68 Inhalable nanoparticles: In vitro and In vivo study, Plos one, doi:10.1371/journal.pone.0267257
Patlolla, Chougule, Patel, Jackson, Tata et al., Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers, Journal of Controlled Release, doi:10.1016/j.jconrel.2010.02.006
Rch, Alveolar surface forces and lung architecture, Comparative Biochemistry and Physiology--Part B: Biochemistry and Molecular Biology, doi:10.1016/S1095-6433(01)00315-4
Ruiz, Orozco, Hoyos, Giraldo, Study of sonication parameters on PLA nanoparticles preparation by simple emulsionevaporation solvent technique, European Polymer Journal, doi:10.1016/j.eurpolymj.2022.111307
Rőszer, Understanding the Mysterious M2 Macrophage through Activation Markers and Effector Mechanisms, Mediators of Inflammation, doi:10.1155/2015/816460
Sahoo, Panyam, Prabha, Labhasetwar, Residual polyvinyl alcohol associated with poly (D, L-lactide-co-glycolide) nanoparticles affects their physical properties and cellular uptake, Journal of controlled release, doi:10.1016/S0168-3659(02)00127-X
Saptarshi, Duschl, Lopata, Interaction of nanoparticles with proteins: relation to bio-reactivity of the nanoparticle, Journal of nanobiotechnology
Sarkar, Bhattacharya, Application of statistical design to evaluate critical process parameters and optimize formulation technique of polymeric nanoparticles, Royal Society open science, doi:10.1098/rsos.190896
Schürch, Gehr, Im, Hof, Geiser et al., Etoposide-loaded PLGA and PCL nanoparticles I: preparation and effect of formulation variables, Respiration Physiology, doi:10.1016/0034-5687
Tavares, De Araújo, Fraceto, Ivermectin-loaded polymeric nanoparticles: Screening the effects of polymers, methods, and the usefulness of mathematical models, Journal of Nanoscience and Nanotechnology, doi:10.1166/jnn.2017.13111
Thakur, Chellappan, Dua, Mehta, Satija et al., Patented therapeutic drug delivery strategies for targeting pulmonary diseases, Expert opinion on therapeutic patents, doi:10.1080/13543776.2020.1741547
Triplett, Rathman, Optimization of β-carotene loaded solid lipid nanoparticles preparation using a high shear homogenization technique, Journal of nanoparticle research, doi:10.1007/s11051-008-9402-3
Venkateswarlu, Manjunath, Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles, Journal of Controlled Release, doi:10.1016/j.jconrel.2004.01.005
Vishwa, Moin, Gowda, Rizvi, Hegazy et al., Pulmonary targeting of inhalable moxifloxacin microspheres for effective management of tuberculosis, Pharmaceutics, doi:10.3390/pharmaceutics13010079
Xu, Khan, Burgess, A quality by design (QbD) case study on liposomes containing hydrophilic API: I. Formulation, processing design and risk assessment, International Journal of Pharmaceutics, doi:10.1016/j.ijpharm.2011.07.012
Yadav, Saini, Arora, MCP-1: chemoattractant with a role beyond immunity: a review, Clinica chimica acta, doi:10.1016/j.cca.2010.07.006
Yang, Chung, Bai, Chan, Effect of preparation conditions on morphology and release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion method, Chemical Engineering Science, doi:10.1016/S0009-2509(99)00503-5
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