Publications

first_pagesettingsOrder Article Reprints Open AccessArticle Application of Box-Behnken Design in the Preparation, Optimization, and In-Vivo Pharmacokinetic Evaluation of Oral Tadalafil-Loaded Niosomal Film by Kawthar K. Abla 1,Amina T. Mneimneh 1,Ahmed N. Allam 2,*ORCID andMohammed M. Mehanna 3,*ORCID 1 Pharmaceutical Nanotechnology Research Lab, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon 2 Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt 3 Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt * Authors to whom correspondence should be addressed. Pharmaceutics 2023, 15(1), 173; https://doi.org/10.3390/pharmaceutics15010173 Received: 18 November 2022 / Revised: 28 December 2022 / Accepted: 28 December 2022 / Published: 3 January 2023 (This article belongs to the Special Issue Recent Advances in Polymeric Delivery Vehicles for Controlled and Sustained Drug Release) Download Browse Figures Review Reports Versions Notes Abstract Benign prostatic hyperplasia (BPH) affects about 90% of men whose ages are over 65. Tadalafil, a selective PDE-5 inhibitor, was approved by FDA for BPH, however, its poor aqueous solubility and bioavailability are considered major drawbacks. This work intended to develop and evaluate oral fast dissolving film containing tadalafil-loaded niosomes for those who cannot receive the oral dosage form. Niosomes were statistically optimized by Box-Behnken experimental design and loaded into a polymeric oral film. Niosomes were assessed for their vesicular size, uniformity, and zeta potential. The thickness, content uniformity, folding endurance, tensile strength, disintegration time, and surface morphology were evaluated for the prepared polymeric film. The optimized niosomes revealed high entrapment efficiency (99.78 ± 2.132%) and the film was smooth with good flexibility and convenient thickness (110 ± 10 µm). A fast release of tadalafil was achieved within 5 min significantly faster than the niosomes-free drug film. The in-vivo bioavailability in rats established that the optimized niosomal film enhanced tadalafil systemic absorption, with higher peak concentration (Cmax = 0.63 ± 0.03 µg/mL), shorter Tmax value (0.66-fold), and relative bioavailability of 118.4% compared to the marketed tablet. These results propose that the oral film of tadalafil-loaded niosomes is a suitable therapeutic application that can be passed with ease to geriatric patients who suffer from BPH.