Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs): A strategy for improved oral delivery

Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) of docetaxel were prepared using varying ratios of Capmul PG 8 NF (oil), Cremophor EL (surfactant) and Transcutol-P (co-surfactant). The optimized L-SNEDDS (L-11) was transformed into self-nanoemulsifying powder (SNEP) by physical adsorption on to Neusilin US2 and evaluated for dissolution behavior, in vitro cytotoxicity and in vivo oral bioavailability. Optimized L-SNEDDS (L-11) composed of 50% of oil, 41.7% of surfactant and 8.3% co-surfactant produced stable emulsion with smaller globules (43 +/- 3 nm). In vitro dissolution studies showed the rapid drug release within 5min (95.42 +/- 1%) from SNEP (N) . In vitro cytotoxicity assessed by the MTT assay using MCF-7 human breast cancer cell lines revealed that L-SNEDDS significantly reduced the IC50 value and was 2.3 times lower than the pure docetaxel. Further, the oral bioavailability studies in male Wistar rats showed higher C (max) values following treatment with SNEP (N) (0.98 +/- 0.13 mu g/mL) and L-SNEDDS (1.09 +/- 0.06 mu g/mL) compared to pure docetaxel (0.37 +/- 0.04 mu g/mL).