Carvone Schiff base of isoniazid as a novel antitumor agent: Nanoemulsion development and pharmacokinetic evaluation
, Mashooq A. Bhat, Muzaffar Iqbal, Abdullah Al-Dhfyan, Faiyaz Shakeel . 2015
In the present study, various nanoemulsion formulations of carvone Schiff base of isoniazid (CSB-INH) were
developed by aqueous phase titration method in order to evaluate its anticancer potential. Developed
nanoemulsions of CSB-INH were characterized in terms of thermodynamic stability, self-nanoemulsification
efficiency, droplet size, polydispersity index (PI), zeta potential (ZP), viscosity, refractive index (RI), % transmittance
(% T), surface morphology and in vitro drug release studies. Based on lowest droplet size (19.4 nm), least
PI (0.189), lowest viscosity (29.6 cP), optimal values of ZP (−30.8 mV) & RI (1.341), highest % T (98.9%), highest
drug release profile (94.5% after 24 h) and the presence of lowest concentration of Triacetin (12% w/w), formulation
N1 was selected for in vitro cytotoxicity and in vivo pharmacokinetic studies. Cytotoxicity studies on
human colon cancer cells indicated that CSB-INH in optimized nanoemulsion is around nine times more efficacious
than free CSB-INH. Pharmacokinetic studies in Albino rats showed rapid absorption (rate and extent) of
CSB-INH from optimized nanoemulsion as compared to its suspension formulation. These results indicated the
potential of developed nanoemulsion for oral delivery of CSB-INH for chemoprevention of colon cancer.
