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ACTA Pharmaceutica Sciencia
2026 , Vol 64 , Num 3
Overcoming solubility challenges of eplerenone via nanomicelles-driven strategy
1 Uruk University, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq2 Ministry of Health, Directorate of Technical Affairs, Department of Pharmacy, Baghdad, Iraq
3 Mustansiriyah University, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq
4 University of AL-Esraa, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq
DOI : 10.23893/1307-2080.APS64022 Viewed : 1106 - Downloaded : 474 Eplerenone (EPR) is a selective mineralocorticoid receptor antagonist used to treat hypertension and heart failure with low water solubility and substantial first-pass metabolism, which limits its oral bioavailability. Nanomicelles (NMs) are nano-sized, self-assembling structures with a hydrophobic core (HC) and hydrophilic shell, utilized as a medication delivery system for poorly water-soluble pharmaceuticals. The present study aimed to formulate EPR exhibiting poor water solubility into NMs to enhance its aqueous solubility, dissolution, and oral bioavailability. Eleven EPR nano-dispersions were prepared employing a thin film hydration method with different surfactants (Soluplus, TPGS, and Solutol) at different ratios, either as a single surfactant or in combination of two surfactants. Various characterization techniques were employed for the optimized nanomicelles, including Fourier transform infrared (FTIR) spectroscopy and field emission-scanning electron microscopy. The results revealed that the particle size (PS) of the majority of developed EPR formulations fell within the nanoscale range. The optimal formulation (F2) has a Particle size of 66.42 nm and a polydispersity index (PDI) of 0.086. The in vitro cumulative release percentage from the NMs was 99.9% within 5 minutes, compared with only 2.42% for the pure drug. The FTIR shows that there was no change in the position of the EPR NM functional group. The findings demonstrated that Soluplus NMs enhanced the solubility and in vitro release profile of EPR, making them an excellent carrier for poorly soluble medications, particularly when rapid release is desired. Keywords : eplerenone, nanomicelles, Soluplus, Solutol, TPGS