Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small

Salman M Ghazwani1, Sami Alhazmi2, Salhah M Ghazwani3

  • 1Department of Surgery, Faculty of Medicine, Jazan University, Saudi Arabia.

Insights

Nebulized nintedanib ufasomes (NLU) offer improved lung cancer treatment. This novel formulation enhances nintedanib

Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Oncology

Background:

  • Nintedanib is used for non-small cell lung cancer (NSCLC).
  • Nintedanib has poor oral bioavailability due to low solubility and first-pass metabolism.
  • There is a need for improved drug delivery methods for nintedanib in NSCLC treatment.

Purpose of the Study:

  • To develop and evaluate nebulized nintedanib ufasomes (NLU) for enhanced NSCLC therapy.
  • To improve nintedanib's sustainability, targeting, bioavailability, and effectiveness.

Main Methods:

  • Formulation optimization using Design Expert software.
  • Evaluation of NLU aerodynamics, cytotoxicity, bioavailability, and targeting.
  • In vivo efficacy and safety study in a Lewis lung carcinoma (LLC) mouse model.

Main Results:

  • NLU significantly increased nintedanib's sustainability (49.5%), bioavailability (6.63-fold), and targeting (8.99-fold).
  • NLU reduced the IC50 value by 4.7-fold.
  • Nebulized NLU demonstrated superior anti-tumor, anti-inflammatory, and anti-oxidative effects compared to oral nintedanib.

Conclusions:

  • Nebulized nintedanib ufasomes (NLU) represent a promising targeted therapy for NSCLC.
  • The optimal NLU formulation at 100 mg/kg is safe and effective.
  • NLU overcomes the limitations of oral nintedanib, offering enhanced therapeutic potential.

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