Preparation and Characterization of Anastrozole Nanocrystal Fast Dissolving Tablets Using Super Disintegrants and Co-Processed Excipients for Enhanced Drug Release

A potent aromatase inhibitor, anastrozole (ANS), in the clinical management of breast cancer in postmenopausal women suffers from many limitations, such as severe adverse effects, poor solubility, and short plasma half-life. In this study, we aimed to develop the anastrozole nanocrystal (ANS-NC) loaded fast dissolving tablets to lower these problems by following the nanotechnology-based drug delivery system. ANS nanoparticles (NPs) were prepared by an optimized nanoprecipitation method with different carrier ratios (1:0.5, 1:0.75, and 1:1) of Poloxamer F68, Gelucire 44/14, PVP K-30, and PVA. Using the direct compression method, NPs were incorporated into fast dissolving tablets formulated with super disintegrants including crospovidone, sodium starch glycolate (SSG), and croscarmellose sodium (CS). Among the various formulations, F18 (Croscarmellose sodium with co-processed Crospovidone) showed the best performance. Various evaluations were conducted, including solubility analysis, particle size measurement, zeta potential, and in vitro dissolution. Particle size optimization, crucial for biocompatibility and stability, resulted in sizes ranging from 334 to 411 nm, with the optimized formulation F3 having a size of 387.2 nm, which improved solubility and stability. F3 exhibited a high drug release rate of 95.18% within 1 h. F15, prepared with Crospovidone, released 98.98% within 40 min. Notably, F18 showed the highest drug release of 99% in just 20 min, with excellent flow properties, outperforming all other formulations in terms of drug release. The present study successfully demonstrated the formulation of fast-dissolving (FD) tablets (FDTs) containing anastrozole nanocrystals (ANS-NCs) to address the limitations of conventional Anastrozole therapy, including poor solubility, short plasma half-life, and adverse effects.