Formulation and evaluation of self-nanoemulsifying drug delivery system for improved oral delivery of exemestane hydrochloride

Abstract

Exemestane HCl (EXM) is a new irreversible steroidal aromatase inhibitor for adjuvant therapy of hormonally sensitive breast cancer in post-menopausal women. EXM's low water solubility hinders solid oral dosage form development. The current work aims to increase EXM solubility by formulating the self nanoemulsifying drug delivery (SNEDDs) system. The water titration approach was employed in the development of SNEDDs. Based on solubility tests, SNEDDs components Caprol Microexpress and Labrafac were selected as oil phase, Tween 80 as surfactant, and Triacetin as co-surfactant. Phase investigations were carried out with various surfactant:co-surfactant ratios (1:1, 1:2, 1:3, 2:1, 3:1). Tween 80: triacetin (1:2) and (1:3) with Caprol Microexpress and Labrafac alone had the greatest nanoemulsion area. Visual evaluation, optical clarity, particle size, medication concentration, and viscosity were used to optimise 10 formulations. F3, F7, and F8 batches had the lowest size at 7.313 ± 1.44 nm, 6.379 ± 0.45 nm, and 14.67 ± 0.37 nm, respectively, with self-emulsification times under 1 min.But optical clarity data was suggested that F7 was not showing any precipitation up to 24 H. Overall, the developed SNEDDS formulation could be a promising approach for the improved oral delivery of EXE with enhanced dissolution and bioavailability.