sildenafil-citrate and precirol

With the non-selective vasodilating action, short half-life and first-pass metabolism of sildenafil (SC), local application in the lung for pulmonary arterial hypertension is of high demand. Although several nanosystems have been lately investigated, nanostructured lipid carriers (NLCs) give promises of potential safety, biodegradability and controlled drug release. In the current study, NLCs comprising either precirol, stearic acid or beeswax as solid lipid in presence of oleic acid as liquid lipid and PVA or poloxamer as emulsifier were prepared. Optimized NLCs (200-268 nm in size) were appraised versus SLNs both in vitro and in vivo. Precirol/PVA-based SLNs and NLCs ensued high entrapment efficiencies (EE > 95%) and controlled release behaviour over 6 h even though NLCs showed higher release profile. Stability studies at 4 °C indicated potential colloidal and entrapment stability over 3 months. Interestingly, NLCs demonstrated efficient nebulization, low interaction with mucin and higher viability of A549 cells (3-fold increase in IC

Topics: A549 Cells; Administration, Inhalation; Animals; Cell Survival; Delayed-Action Preparations; Diglycerides; Drug Carriers; Humans; Hypertension, Pulmonary; Lipids; Male; Nanostructures; Phosphodiesterase 5 Inhibitors; Polyvinyl Alcohol; Rats, Sprague-Dawley; Sildenafil Citrate