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Research Article Open access CC BY 4.0

Spray-dried, Biodegradable, Linezolid-loaded Microspheres for Use in the Treatment of Lung Diseases

Mazen Gharsan Al-Gharsan, Sree Harsha

Journal of Advances in Medical and Pharmaceutical Sciences · pp. 38–58 · Published 9 Oct 2023

10.9734/jamps/2023/v25i9642

Abstract

Introduction: Researchers worldwide are currently seeking innovative treatment options to combat the alarming increase in bacterial resistance to antimicrobial drugs. Staphylococcus aureus, a frequently encountered and potentially life-threatening bacterium, has become particularly problematic. Linezolid is one of the few medicines on the market that can treat bacteria resistant to other antibiotics. This is the first antibacterial oxazolidinone that has shown to be therapeutically efficacious. Linezolid is a new Oxazolidinone medicine. It kills a broad spectrum of bacteria, including Staphylococcus aureus. Objectives: To reduce non-target organ adverse effects associated with frequent and chronic Linezolid usage, we developed biodegradable, lung-targeted microspheres with sustained release profile. Methods: In this work, a Buchi B-90 nanospray drier was used to prepare a Linezolid-loaded carbopol microsphere (CLSMO)-based formulation. The spray-drying process was optimized using a face-centered central composite design (CCD). Results: The average particle size was 7.516 µm, and the surface of the microspheres was shriveled, according to scanning electron microscope imaging. Drug content and yield were determined to be 73% 3.1% and 72% ± 2.4%., respectively, and drug release (99.1%) peaked for up to 12 hours in vitro. FTIR spectral analysis results suggest that there are no significant physical and chemical interactions between the functional groups of Linezolid and carbopol 934P polymer which ultimately form a stable blend. Linezolid, Carbopol, and CLSMO all had XRD patterns that showed the linezolid would be molecularly dispersed in the polymer. The DSC findings revealed the drug's amorphous nature, which explains the absence of characteristic peaks, indicating a lack of well-defined crystalline structure. Conclusion: The optimized formulation shows significant potential for use as a drug-delivery system in in-vivo applications, particularly in targeted drug delivery to the lungs.

Drug delivery lung diseases therapeutic utility

References (21)

  1. 1 The Effectiveness of Self-Management Mobile Phone and Tablet Apps in Long-term Condition Management: A Systematic Review [DOI]
  2. 2 The Global Burden of Respiratory Disease [DOI]
  3. 3 Polymeric micelles and cancer therapy: an ingenious multimodal tumor-targeted drug delivery system [DOI]
  4. 4 Current Status of Radiopharmaceutical Therapy [DOI]
  5. 5 Application of PLGA as a Biodegradable and Biocompatible Polymer for Pulmonary Delivery of Drugs [DOI]
  6. 6 Systematic review of association between critical errors in inhalation and health outcomes in asthma and COPD [DOI]
  7. 7 Size, concentration, and origin of human exhaled particles and their dependence on human factors with implications on infection transmission [DOI]
  8. 8 Microsphere Polymers in Molecular Imprinting: Current and Future Perspectives [DOI]
  9. 9 Injectable systems of chitosan in situ forming composite gel incorporating linezolid-loaded biodegradable nanoparticles for long-term treatment of bone infections [DOI]
  10. 10 DESIGN, FORMULATION AND IN VITRO DRUG RELEASE FROM TRANSDERMAL PATCHES CONTAINING IMIPRAMINE HYDROCHLORIDE AS MODEL DRUG [DOI]
  11. 11 The recent insight in the release of anticancer drug loaded into PLGA microspheres [DOI]
  12. 12 In Vitro and In Vivo Evaluation of Nanoparticles Prepared by Nano Spray Drying for Stomach Mucoadhesive Drug Delivery [DOI]
  13. 13 Preparation of cassava starch-gelatin yolk-shell microspheres by water-in-water emulsion method [DOI]
  14. 14 Effects of Surface Morphology and Type of Cross-Linking of Chitosan-Pectin Microspheres on Their Degree of Swelling and Favipiravir Release Behavior [DOI]
  15. 15 An overview on microspheres
  16. 16 Study of stability, kinetic parameters and release of lysozyme immobilized on chitosan microspheres by crosslinking and covalent attachment for cotton fabric functionalization [DOI]
  17. 17 High azithromycin concentration in lungs by way of bovine serum albumin microspheres as targeted drug delivery: lung targeting efficiency in albino mice [DOI]
  18. 18 Recent Advances in Microspheres Technology for Drug Delivery [DOI]
  19. 19 Novel, Blended Polymeric Microspheres for the Controlled Release of Methotrexate: Characterization and In Vivo Antifibrotic Studies [DOI]
  20. 20 An Efficient, Lung-Targeted, Drug-Delivery System To Treat Asthma Via Microparticles
  21. 21 Drug Delivery and Translational Research [DOI]

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