Enhancing Bioavailability of Abiraterone Acetate by Nanostructured Lipid Carriers: In Vivo, In Vitro Characterization and Cytotoxicity Assessment

Abiraterone is an antiandrogen medication used for the treatment of prostate cancer. Abiraterone acetate (ABA) was found to be resistant to esterase and gets rapidly deacetylated to abiraterone in vivo that results in potent CYP450 C17 inhibition. The present work deals with the preparation of ABA-loaded nano-structured lipid carrier (NLC) by high sheer homogenization method and the evaluation by particle size, poly dispersity index (PDI) and zeta potential measurement, in-vitro drug release study, in vivo pharmacokinetic study and in vitro cytotoxicity study characterized by dynamic light scattering (DLS) method. The optimal size, PDI and zeta potential obtained using DLS were 37.92 nm, 0.209 - 0.499 and -18.3 mV respectively. In vitro drug release study demonstrated improved traversion of NLC through the dialysis membrane with potential sustained release for 12 hr. In vivo pharmacokinetics was performed to observe the bioavailability of ABA NLC. The studies in oral route demonstrated no significant improvement in oral bioavailability. The in vitro cytotoxicity study in Du-145 prostate carcinoma cell lines, expressed higher cytotoxicity for NLC formulation which was concentration dependent with p value <0.001 at all concentrations starting at 0.002 ug to 0.1 ug.