Design of self-nanoemulsifying system to enhance absorption and bioavailability of poorly permeable Aliskiren hemi-fumarate
The aim of this study was to develop self-nanoemulsifying system (SNES) to improve the oral bioavailability of Aliskiren hemi-fumarate (AF). The solubility of AF in various oils, surfactants and, co-surfactants was studied to select the proper components of the system. The composition of SNES was further optimized with the aid of pseudo-ternary phase diagram study where efficient self-emulsifying region was identified.
The formulations characterized for droplet size, poly dispersity index, zeta potential, emulsification time, % transmittance, refractive index, cloud point, electroconductivity, drug content, viscosity, in vitro drug release study, and ex-vivo drug permeation. Pharmacokinetic study for the optimized formulation compared to AF solution were carried out. Stability study was performed for the optimized formulation after storage at room temperature for 3 months. TEM analysis demonstrated spherical shape of droplets which had sizes in the range of (10.2–12.9 n. m). PDI values were (0.29–0.38) and zeta potential values were (−8.26 to −23.5 mv).
Drug permeation from SNES formulae was significantly higher than that of drug solution. Cmax and AUC0-24 of SNES formulation were 3.05 and 2.5 fold increases than drug solution. These results suggested that SNES could be a promising carrier to improve oral bioavailability of AF.
Article Information: Author links open overlay panelAbeer Khattab, MahaMohamed, Emad B.Basalious; Journal of Drug Delivery Science and Technology, 2020.