Gurunanak College of Pharmacy, Nagpur-440026, Maharashtra, India
*Email: shobhayadav1402@gmail.com
Received: 18th Sep, 2025; Revised: 26th Oct, 2025; Accepted: 26th Nov, 2025; Available Online: 1st December, 2025
Tadalafil (TDF), acting as a phosphodiesterase-5 inhibitor and clinically used for benign prostatic hyperplasia, pulmonary arterial hypertension, and erectile dysfunction suffers from poor aqueous solubility and low oral bioavailability. In this research investigation, a stable nanosuspension (NS) of Tadalafil (TDF) was developed and optimized using high-shear homogenization (HSH) within a Quality by Design (QbD) framework. Box–Behnken design assessed the effects of drug-to-stabilizer ratio, homogenization speed, and time on particle size, PDI, and drug loading. The optimized NS showed a particle size of 515.9 ± 42 nm, PDI 0.539 ± 0.034, and drug loading around 70%. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) confirmed partial amorphization of TDF. FE-SEM analysis revealed spherical nanosized particles. Dissolution studies demonstrated >90% release within 60 min compared with 20% for pure TDF suspension. Stability testing under accelerated conditions confirmed physical stability for 3 months. Pharmacokinetic evaluation in Wistar rats revealed significantly higher Cmax and AUC for NS, corresponding to ~2.5-fold improvement in relative oral bioavailability versus drug suspension. This work demonstrates that HSH is a robust, scalable approach for improving solubility, dissolution, and bioavailability of tadalafil.
Keywords: Tadalafil; nanosuspension; high shear homogenization; solubility enhancement; Box–Behnken design; pharmacokinetics.
How to cite this article: Ubgade S, Kilor V, Sapkal N, Lohiya G, Ubgade A, Ittadwar A. Formulation and Optimization of Tadalafil Nanosuspension Using High Shear Homogenization and Design of Experiments Approach for Solubility and Bioavailability Enhancement. Int J Drug Deliv Technol. 2026;16(1): 659-671; DOI: 10.25258/ijddt.16.1.68
Source of support: Nil.
Conflict of interest: None