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Pharmaceutics. 2021 Aug 27;13(9). doi: 10.3390/pharmaceutics13091347.

Lung Targeted Lipopolymeric Microspheres of Dexamethasone for the Treatment of ARDS.

Pharmaceutics

Sabna Kotta, Hibah Mubarak Aldawsari, Shaimaa M Badr-Eldin, Lenah S Binmahfouz, Rana Bakur Bakhaidar, Nagaraja Sreeharsha, Anroop B Nair, Chandramouli Ramnarayanan

Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  2. Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  3. Department of Pharmacology and Toxicology, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  4. Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
  5. Department of Pharmaceutics, Vidya Siri College of Pharmacy, Off Sarjapura Road, Bangalore 560035, India.
  6. Department of Pharmaceutical Chemistry, Vidya Siri College of Pharmacy, Off Sarjapura Road, Bangalore 560035, India.

PMID: 34575422 PMCID: PMC8471313 DOI: 10.3390/pharmaceutics13091347

Abstract

Acute respiratory distress syndrome (ARDS), a catastrophic illness of multifactorial etiology, involves a rapid upsurge in inflammatory cytokines that leads to hypoxemic respiratory failure. Dexamethasone, a synthetic corticosteroid, mitigates the glucocorticoid-receptor-mediated inflammation and accelerates tissue homeostasis towards disease resolution. To minimize non-target organ side effects arising from frequent and chronic use of dexamethasone, we designed biodegradable, lung-targeted microspheres with sustained release profiles. Dexamethasone-loaded lipopolymeric microspheres of PLGA (Poly Lactic-co-Glycolic Acid) and DPPC (Dipalmitoylphosphatidylcholine) stabilized with vitamin E TPGS (D-α-tocopheryl polyethylene glycol succinate) were prepared by a single emulsion technique that had a mean diameter of 8.83 ± 0.32 μm and were spherical in shape as revealed from electron microscopy imaging. Pharmacokinetic and biodistribution patterns studied in the lungs, liver, and spleen of Wistar rats showed high selectivity and targeting efficiency for the lung tissue (

Keywords: ARDS; dexamethasone; lung inflammation; lung targeting; microspheres

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