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Related Concept Videos

Inhaled Medications01:23

Inhaled Medications

507
Inhaled medications are crucial for managing chronic obstructive pulmonary disease (COPD) and asthma. They are essential for effective treatment and control, ensuring optimal respiratory health and well-being. Inhaled medication delivers drugs directly to the lungs, providing a rapid onset of action and reducing systemic side effects compared to oral or injectable medications. Three primary types of inhalation devices are used to administer these medications: nebulizers, metered-dose inhalers...
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Repurposing Bedaquiline for Effective Non-Small Cell Lung Cancer (NSCLC) Therapy as Inhalable Cyclodextrin-Based

Vineela Parvathaneni1, Rasha S Elbatanony1,2, Mimansa Goyal1

  • 1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA.

International Journal of Molecular Sciences
|May 5, 2021
PubMed
Summary

Repurposed anti-tuberculosis drug bedaquiline (BDQ) was formulated into an inhalable cyclodextrin complex for non-small cell lung cancer (NSCLC). This formulation enhances BDQ solubility and shows promising anti-cancer efficacy via inhalation.

Keywords:
bedaquilineinhalationmolecular dockingnon-small cell lung cancersulfobutylether-β-cyclodextrin

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Area of Science:

  • Pharmaceutical Sciences
  • Oncology
  • Drug Delivery

Background:

  • Drug repurposing accelerates development for challenging diseases like non-small cell lung cancer (NSCLC).
  • Bedaquiline (BDQ), an anti-tuberculosis drug, shows potential for anti-cancer applications.
  • Developing effective delivery systems is crucial for inhaled therapies.

Purpose of the Study:

  • To develop an inhalable cyclodextrin complex of bedaquiline (BDQ-CD).
  • To evaluate the anti-cancer activity and lung deposition of the BDQ-CD complex in NSCLC models.

Main Methods:

  • Phase solubility and molecular modeling identified SBE-β-CD for complexation.
  • Aqueous solubility, solid-state characterization, and in vitro lung deposition were assessed.
  • Cytotoxicity studies were performed on NSCLC cell lines (H1299, A549).

Main Results:

  • BDQ solubility increased 2.8 × 10³-fold upon complexation with SBE-β-CD.
  • The BDQ-CD complex exhibited excellent inhalable properties (MMAD 2.9 µm, FPF 83.3%).
  • The BDQ-CD complex showed slightly enhanced cytotoxicity compared to BDQ alone in H1299 cells.

Conclusions:

  • BDQ-CD complex formation significantly enhances BDQ solubility and stability.
  • The developed formulation is suitable for inhalation with efficient lung deposition.
  • BDQ-CD complex represents a promising inhaled therapeutic strategy for NSCLC.