Formulation of osimertinib nano lipid carriers: Optimization, characterization and cytotoxicity assessment

In the present study, orally administered Osimertinib nanostructured lipid carriers (OSM-NLCs) was prepared by the hot-melt emulsification and sonication method. The formulations were optimized by Box-Behnken design to get the optimum composition. The optimized formulation (OSM-NLCop) was further evaluated for in-vitro, ex-vivo parameters as well as in-vitro cytotoxicity evaluation against lung cancer cell line. The selected OSM-NLCop has shown a particle size of 162.6 ± 3.5 nm, PDI 0.25, entrapment efficiency 80.2 ± 3.9% with the negative zeta potential (− 24.7 mV). OSM-NLCop showed significant (p < 0.05) high drug release (82.52 ± 5.4%) as compared to pure OSM (24.7 ± 3.6%). Drug release profile from OSM-NLCop displayed Fickian release kinetic with Korsmeyer-Peppas release model. It also exhibited significantly high permeation with 4.8-fold enhancement in the permeation flux than pure OSM dispersion. OSM-NLCs also depicted (p < 0.05) lesser cytotoxicity against the tested lung cancer cell and reduced IC50 value as compared to pure OSM. From the findings, it can be concluded that NLCs are promising carriers for the delivery of OSM and may improve the therapeutic efficacy against lung cancer cell lines.