Nanoformulation, Characterization, and In Vivo Pharmacokinetic Studies of Diosgenin- and Emodin-Loaded Polymeric Nanoparticles.

Obstruct pharmacokinetics and low bioavailability of diosgenin (DG) and emodin (ED) are major limitations for their therapeutic success in several inflammatory diseases. Nanoencapsulation of both drugs will promisingly overcome these limitations. Herein, polylactic-co-glycolic acid (PLGA) was used for nanoformulation of diosgenin- and emodin-loaded PLGA nanoparticle (DGn and EDn) via modified solvent-emulsion-diffusion-evaporation method. Functional stability of prepared nanoparticles and in vitro physiological characterization including mean particle sizes distribution, polydispersity index, surface zeta potential, and morphological examinations were performed. Moreover, drug loading and encapsulation efficiency were also evaluated by measuring drug concentration through spectroscopy and HPLC method. Both drug nanoformulations demonstrated functional drug stability, 200–270 nm sizes with homogeneous particle distribution, negative surface zeta potential stability, and uniform spherical morphology. Moreover, nanoparticles showed in vitro controlled drug release pattern over 24 h with 40–70% of drug depletion. Pharmacokinetics analysis was performed on sixteen rats equally distributed in four groups (DG, ED, DGn, and EDn). Pure drugs and nanoformulations were orally (10 mg/kg) administrated to animal model, and pharmacokinetic profiles of both drugs were evaluated. PLGA nanoparticles were significantly able to alter the pharmacokinetics of DG, while little improvement was observed for ED. Consequently, changes in pharmacokinetics of both drugs are attributed to size and surface characteristics of nanoparticles. DGn and EDn subsidize increased mean plasma residence time and maximize area under curve with decreased drug clearance rate. Resulting in vitro characteristics and in vivo pharmacokinetics data reveal the efficacy of DGn and EDn to be suitable nano-drug delivery modalities with improved bioavailability and pharmacological strength. [ABSTRACT FROM AUTHOR]