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Inhaled Edoxaban dry powder inhaler formulations: Development, characterization and their effects on the coagulopathy associated with COVID-19 infection.
Rashid, Md Abdur; Muneer, Saiqa; Mendhi, Jayanti; Sabuj, Mohammad Zaidur Rahman; Alhamhoom, Yahya; Xiao, Yin; Wang, Tony; Izake, Emad L; Islam, Nazrul.
  • Rashid MA; Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Aseer 62529, Saudi Arabia.
  • Muneer S; School of Chemistry and Physics, Faculty of Science, Queensland University of Technology, Brisbane, Queensland, Australia.
  • Mendhi J; Queensland University of Technology, Centre for Biomedical Technology, Brisbane, Queensland, Australia.
  • Sabuj MZR; Pharmacy Discipline, School of Clinical Sciences, Faculty of Health, Queensland University of Technology, Brisbane, Queensland, Australia.
  • Alhamhoom Y; Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Aseer 62529, Saudi Arabia.
  • Xiao Y; Queensland University of Technology, Centre for Biomedical Technology, Brisbane, Queensland, Australia; Australia-China Centre for Tissue Engineering and Regenerative Medicine, Queensland University of Technology, Brisbane, Queensland, Australia.
  • Wang T; Central Analytical Research Facility, Institution for Future Environment, Queensland University of Technology, Brisbane, Queensland, Australia.
  • Izake EL; School of Chemistry and Physics, Faculty of Science, Queensland University of Technology, Brisbane, Queensland, Australia.
  • Islam N; Pharmacy Discipline, School of Clinical Sciences, Faculty of Health, Queensland University of Technology, Brisbane, Queensland, Australia; Centre for Immunology and Infection Control (CIIC), Queensland University of Technology (QUT), Brisbane, Queensland, Australia. Electronic address: nazrul.islam@
Int J Pharm ; 608: 121122, 2021 Oct 25.
Article in English | MEDLINE | ID: covidwho-1433361
ABSTRACT
Herein, we demonstrated the development and characterization of a dry powder inhaler (DPI) formulation of edoxaban (EDX); and investigated the in-vitro anticoagulation effect for the management of pulmonary or cerebral coagulopathy associated with COVID-19 infection. The formulations were prepared by mixing the inhalable micronized drug with a large carrier lactose and dispersibility enhancers, leucine, and magnesium stearate. The drug-excipient interaction was studied using X-Ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) methods. The drug and excipients showed no physical inter particulate interaction. The in-vitro drug aerosolization from the developed formulation was determined by a Twin Stage Impinger (TSI) at a flow rate of 60 ± 5 L /min. The amount of drug deposition was quantified by an established HPLC-UV method. The fine particle fraction (FPF) of EDX API from drug alone formulation was 7%, whereas the formulations with excipients increased dramatically to almost 7-folds up to 47%. The developed DPI formulation of EDX showed a promising in-vitro anticoagulation effect at a very low concentration. This novel DPI formulation of EDX could be a potential and effective inhalation therapy for managing pulmonary venous thromboembolism (VTE) associated with COVID-19 infection. Further studies are warranted to investigate the toxicity and clinical application of the inhaled EDX DPI formulation.
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Full text: Available Collection: International databases Database: MEDLINE Document Type: Article Main subject: Pyridines / Thiazoles / Blood Coagulation Disorders / Dry Powder Inhalers / COVID-19 Subject: Pyridines / Thiazoles / Blood Coagulation Disorders / Dry Powder Inhalers / COVID-19 Type of study: Risk factors Language: English Journal: Int J Pharm Year: 2021

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Full text: Available Collection: International databases Database: MEDLINE Document Type: Article Main subject: Pyridines / Thiazoles / Blood Coagulation Disorders / Dry Powder Inhalers / COVID-19 Subject: Pyridines / Thiazoles / Blood Coagulation Disorders / Dry Powder Inhalers / COVID-19 Type of study: Risk factors Language: English Journal: Int J Pharm Year: 2021
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