Sorafenib Loaded Inhalable Polymeric Nanocarriers against Non-Small Cell Lung Cancer

Pharm Res. 2020 Mar 12;37(3):67. doi: 10.1007/s11095-020-02790-3.


Purpose: This exploration is aimed at developing sorafenib (SF)-loaded cationically-modified polymeric nanoparticles (NPs) as inhalable carriers for improving the therapeutic efficacy of SF against non-small cell lung cancer (NSCLC).

Methods: The NPs were prepared using a solvent evaporation technique while incorporating cationic agents. The optimized NPs were characterized by various physicochemical parameters and evaluated for their aerosolization properties. Several in-vitro evaluation studies were performed to determine the efficacy of our delivery carriers against NSCLC cells.

Results: Optimized nanoparticles exhibited an entrapment efficiency of ~40%, <200 nm particle size and a narrow poly-dispersity index. Cationically-modified nanoparticles exhibited enhanced cellular internalization and cytotoxicity (~5-fold IC50 reduction vs SF) in various lung cancer cell types. The inhalable nanoparticles displayed efficient aerodynamic properties (MMAD ~ 4 μM and FPF >80%). In-vitro evaluation also resulted in a superior ability to inhibit cancer metastasis. 3D-tumor simulation studies further established the anti-cancer efficacy of NPs as compared to just SF.

Conclusion: The localized delivery of SF-loaded nanoparticles resulted in improved anti-tumor activity as compared to SF alone. Therefore, this strategy displays great potential as a novel treatment approach against certain lung cancers.

Keywords: 3D spheroids; Sorafenib; cationically modified particles; inhalable nanoparticle; non-small cell lung cancer.

MeSH terms

  • Administration, Inhalation
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacology
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Cations / chemistry
  • Cell Line, Tumor
  • Drug Carriers / chemistry
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Polymers / chemistry
  • Sorafenib / administration & dosage*
  • Sorafenib / pharmacology


  • Antineoplastic Agents
  • Cations
  • Drug Carriers
  • Polymers
  • Sorafenib