Eplerenone

This Cochrane review of five randomized placebo‑controlled trials (1437 patients) assessed eplerenone for primary hypertension. Meta‑analysis showed a mean systolic blood pressure reduction of 9.21 mmHg (95% CI ‑11.08 to ‑7.34) and diastolic reduction of 4.18 mmHg (95% CI ‑5.03 to ‑3.33) with eplerenone 50‑200 mg/day, compared to placebo. No clear dose‑response effect was observed across the 50‑200 mg range, while 25 mg was ineffective and evidence for >200 mg insufficient. Withdrawal due to adverse events did not differ from placebo, but adverse event reporting was incomplete. No data on mortality or cardiovascular morbidity were available. The authors conclude that eplerenone lowers blood pressure but evidence on clinical outcomes and long‑term harm is lacking.

Fig. 1 Study flow diagram. (Tam TS, et al., 2017)

Eplerenone nanocrystals (mean size 46.8 nm) were prepared using a bottom‑up controlled crystallization technique during freeze‑drying, optimized via D‑optimal mixture design. The nanocrystals showed a 17‑fold increase in saturation solubility (155.9 vs. 8.96 µg/mL) and ∼95% dissolution in 10 minutes versus 29% for bulk drug. In vivo, they improved oral bioavailability (higher AUC and Cmax, lower Tmax) with no acute toxicity. This formulation strategy is promising for poorly water‑soluble drugs.

Fig. 2 Particle size distribution curve (A) and scanning electron microscopic image (B) of the optimized EPL-NCs.(Khan MA, et al., 2021)