Formulation, optimization, and in vitro evaluation of anastrozole-loaded nanostructured lipid carriers for improved anticancer activity
The present study aims to develop and optimize anastrozole (ANZ)-nanostructured lipid carriers (ANZ-NLCs) for improved anticancer efficacy. In a nutshell, ANZ-NLCs were prepared by a 32 factorial design approach through the solvent evaporation method. In this study, key formulation factors impacting particle size, % drug encapsulation, and zeta potential were optimized in ANZ-NLCs. The physicochemical characterization and in vitro cytotoxicity, cell apoptosis, cell cycle analysis, cell uptake, and investigation of apoptotic nuclei by DAPI study was performed on MCF 7 to assess the potential of ANZ-NLCs. The optimized batch exhibited the spherical and smooth surface morphology that was confirmed by AFM and HR-TEM. In addition, the optimized batch showed 164.4 nm particle size, 62.95% entrapment efficiency, and −26.3 mV zeta potential. Elucidation of FTIR and H NMR studies revealed compatibility of ANZ with the carrier lipids and DSC and XRD confirmed amorphous ANZ-NLCs (which was the type of NLC formed). The in vitro ANZ release study revealed the significance of compritol in release modulation from ANZ-NLCs. Herein, the optimized batch demonstrated extended-release in different release media (upto 48 h), following the fickian type. In vitro anticancer efficacy was assessed by cytotoxicity, cell apoptosis, cell cycle analysis, cell uptake, and apoptotic nuclei, which confirmed the significant anticancer efficacy of ANZ-NLCs compared to free ANZ. Consequently, ANZ-NLCs made from compritol 888 ATO and capryol could be a prospective formulation exhibiting significant anticancer potential in the oral delivery of ANZ for the effective dealing of breast cancer (BC).
Dhiarysheel Ghadge, Sopan Nangare, Namdeo Jadhav,
Formulation, optimization, and in vitro evaluation of anastrozole-loaded nanostructured lipid carriers for improved anticancer activity,
Journal of Drug Delivery Science and Technology, 2022, 103354, ISSN 1773-2247,
https://doi.org/10.1016/j.jddst.2022.103354.