Abstract
Poor water solubility and low oral bioavailability limit the clinical application
of Erlotinib as an anticancer. For this purpose, we encapsulated erlotinib in the
solid lipid nanoparticles (SLN) and designed a spray-dried dry powder inhalable (DPI)
formulation. Erlotinib-loaded SLNs were prepared using self-nanoemulsifying and characterized
for physicochemical properties. Pulmonary deposition of spray-dried DPI formulation
was performed using Next Generation Impactor. The particle size and zeta potential
of Erlotinib-loaded SLNs were 300 to 800 nm and −18 to −32 mV, respectively. High
drug entrapment efficiency in the narrow range of 80–85% was achieved. Cytotoxicity
results indicated that cell growth inhibition of free drug and drug loaded nanoparticles
is dose- and time-dependent. Inhalable dry powders prepared from drug-loaded SLNs
were found to have a fine particle fraction in the range of 6.92±0.99 –11.24±2.4%,
mean mass aerodynamic diameter in the range of 4.52±0.1 to 6.67±0.5 µm. The findings
revealed that the proposed inhalable dry powder formulation loaded with erlotinib
SLN has potential in lung cancer therapy through pulmonary route.
Key word
drug delivery - bioavailability - anticancer drugs