Archu Singh, Y. Neupane, Bharti Mangla
Jun 13, 2019
Citations
5
Influential Citations
77
Citations
Quality indicators
Journal
Journal of pharmaceutical sciences
Abstract
Exemestane (EXE), a novel oral steroidal aromatase inhibitor, approved for the treatment of breast cancer. However, its oral clinical application is limited because of low aqueous solubility and low oral bioavailability. Here, we aim to design and fabricate Nanostructured Lipid Carriers (NLCs) using Precirol® ATO5 and Flaxseed oil as the solid lipid and liquid lipid, respectively. EXE loaded NLCs were spherical in shape and with the hydrodynamic diameter of 131.3±2.43 nm, polydispersity index (PDI) 0.205 ± 0.06 and % Entrapment efficiency (% EE) 85.6 ± 1.20%. In vitro release study demonstrated a sustained release pattern for 24 h with relative burst release at the initial time point. Differential scanning calorimetry (DSC) and Powder X-ray diffraction (PXRD) studies showed reduced crystallinity and complete encapsulation of drug within lipid matrix. Ex vivo gut permeation study and Confocal Laser Scanning Microscopy (CLSM) revealed that NLCs comprising of lipid blend and surfactant enhanced intestinal permeability of EXE. Moreover, in vivo pharmacokinetic study on female Wistar rats found to 3.9-fold augment in oral bioavailability of EXE through NLCs compared with EXE suspension. Herein, we depict that loading of EXE into NLCs hold promising approach for the oral delivery of EXE in cancer therapy.