Coenzyme Q10 (
CoQ10) is an
antioxidant with well-established pharmacological activities against several
chronic diseases; however, it is marketed only as a nutritional supplement without any claims of its therapeutic activity and one of the reasons for this could be the poor oral bioavailability rendering difficulties in administering this molecule to achieve therapeutic concentrations. Therefore, the present investigation was aimed at improving the oral bioavailability of
CoQ10 by delivering it as nanoparticulate formulation. Biodegradable nanoparticulate formulations based on
poly(lactide-co-gylcolide) (PLGA) were prepared by
emulsion technique using quaternary
ammonium salt didodecyldimethylammonium bromide (DMAB) as a stabilizer. The effect of initial
CoQ10 loading on entrapment efficiency and the particle size was studied using 5-75% initial load resulting in good entrapment efficiency (61-83%) without any appreciable increase in the particle size for 5-30% loading (107-110 nm). However, 50% and 75% led to increase in particle size with no appreciable changes in entrapment efficiency. The intestinal uptake of
CoQ10 as a
suspension in
carboxymethylcellulose (CMC), a commercial formulation and the developed nanoparticulate formulation was studied in male Sprague-Dawley (SD) rats and found to be 45%, 75% and 79%, respectively, suggesting that solubility and permeability related problems of
CoQ10 were overcome by nanoparticulate formulation. Furthermore, the developed nanoparticulate formulation was evaluated for its therapeutic potential in renal hypertensive animals (Goldblatt 2K1C model), demonstrating improved efficacy at a 60% lowered dose as compared to
CoQ10 suspension and superior efficacy than the commercial formulation at an equal dose. Together, these results indicate the potential of nanotechnology in improving the therapeutic value of molecules like
CoQ10, facilitating its usage as first line therapeutic agent thus revolutionizing its role in current medical
therapy.