Formulation and Development of CoQ10-Loaded s-SNEDDS for Enhancement of Oral Bioavailability

Coenzyme (CoQ10) is a poorly soluble drug strategically selected to enrich oral bioavailability by incorporating in solid self-nanoemulsifying drug delivery system (s-SNEDDS) comprised of oil, surfactant, and cosurfactant. The conventional self-emulsifying drug delivery system (SEDDS) and liquid SNEDDS (l-SNEDDS) usually have the problem of drug instability and precipitation. The selected oils, surfactant, and cosurfactant with maximum drug solubility were Lauroglycol FCC, Labrasol, and Transcutol P. The ternary phase diagrams were constructed, and selected formulations from ternary phase diagrams were subjected to thermodynamic stability and self-dispersibility test and characterized for emulsion droplet size and droplet size distribution. The optimized formulation was comprised of Lauroglycol FCC 20 % (w/w), Labrasol 10 % (w/w), and Transcutol P 20 % (w/w) as oil, surfactant, and cosurfactant. The transmission electron microscopy (TEM) study of optimized l-SNEDDS reported mean globule size of 34 nm was transformed into s-SNEDDS by spray-drying technique using solid carrier. The s-SNEDDS was characterized for differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), and X-ray diffraction (X RD). The in vitro release profile of s-SNEDDS showed drug release (97.5 +/- 4.5 %), marketed formulation (57.96 +/- 0.54 %), and CoQ10 powder (0.36 +/- 0.06 %) in 1 hour. The pharmacokinetic study of optimized s-SNEDDS in male Wistar rats revealed the improved maximum concentration (C (max)) (3.4-fold vs CoQ10 powder; 1.4-fold vs marketed formulation) and area under the curve (AUC) (5-fold vs CoQ10 powder; 2-fold vs marketed formulation). With this result, s-SNEDDS could be of potential to enhance the oral bioavailability of CoQ10. Thus, s-SNEDDS in addition to enhancing the dissolution and oral bioavailability often results in low production cost, easy processing, and better patient compliance.