Solid supersaturated self-nanoemulsifying drug delivery system for abiraterone acetate: improved drug loading,...

Abiraterone acetate (ABT) is an androgen biosynthesis inhibitor approved for the treatment of prostate cancer. However, the treatment course of ABT is constrained by its high dose, poor solubility and permeability issues. A solid supersaturated self-nanoemulsifying drug delivery system (ssSNEDDS) is an excellent approach for improving drug loading. The aim was to increase the solubility and drug loading of ABT in SNEDDS via supersaturation by using a polymeric precipitation inhibitor (HPMC E5). Liquid SNEDDS were thoroughly optimized with a mixture design followed by solidification with Aerosil^® 200 by the adsorption method. The developed ABT-ssSNEDDS showed a nano-ranged particle size of 106.23 ± 4.15 nm and PDI of 0.234 ± 0.0069. Furthermore, the powder showed an angle of repose of 34.86 ± 0.30° indicating good flow properties with smooth morphology under SEM analysis. DSC and PXRD studies revealed amorphization of ABT in the ABT-ssSNEDDS group. Furthermore, the dissolution study demonstrated significantly higher ABT release from ABT-ssSNEDDS in comparison to free ABT after 2 h in pH 1.2 and 6.8 pH buffer. In-vitro cell culture studies in the PC-3 cell line denoted significantly enhanced anticancer activity and cellular uptake. Thus, ABT-ssSNEDDS could be an encouraging approach for improved oral therapy and enhanced drug loading of ABT.