FABRICATION AND CHARACTERIZATION OF Β-CYCLODEXTRIN-BASED NANO SPONGES FOR DELIVERY OF ABIRATERONE ACETATE

Abstract

Abiraterone acetate is a steroidal progesterone derivative that inhibits the enzymes CYP17A1, CYP11B1, and the androgen receptor antagonist. It is clinically used in adrenal, testicular, and prostatic cancer. Abiraterone has limited use, due to poor water solubility and low oral bioavailability (<10%). The current study focused on the enhancement of water solubility of abiraterone using β-cyclodextrin nano sponges, which are a hyper cross-linked novel nano-drug delivery system. Design and optimization of β-cyclodextrin nano sponges were carried out, using the modified solvent method. Polymer to cross-linker ratio, solvent volume, and reaction time were defined as critical parameters for optimization. Fourier-transform Infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, Zeta sizer, and powdered X-ray diffraction technique were used for characterization. Drug entrapment and In-vitro dissolution studies were performed and samples were analyzed using reverse phase high performance liquid chromatography. Optimized β-cyclodextrin nano sponges were porous para-crystalline particles (25.3%) with an average particle size of 463.4 nm. High drug entrapment leads to enhancement of solubility by 17.33 folds and a 3-fold increase in drug dissolution profile. The present approach offers the best way to increase the solubility of abiraterone by formulating a nano-size hyper cross-linked βcyclodextrin nano sponges which can tend to the improvement of abiraterone oral bioavailability.