Purpose: The objective of this study was to formulate and optimize Candesartan Cilexetil
(CC) loaded nanostructured lipid carriers (NLCs) for enhanced oral bioavailability.
Method: Glycerol monostearate (GMS), Oleic acid, Tween 80 and Span 40 were selected as a solid
lipid, liquid lipid, surfactant and co- surfactant, respectively. The CC-NLCs were prepared by hot
emulsion probe sonication technique and optimized using experimental design approach. The formulated
CC-NLCs were evaluated for various physicochemical parameters and further optimized formulation
(CC-NLC-Opt) was assessed for in vivo pharmacokinetic and pharmacodynamic activity.
Results: The optimized formulation (CC-NLC-Opt) showed particle size (183.5±5.89nm), PDI
(0.228±0.13), zeta potential (-28.2±0.99mV), and entrapment efficiency (88.9±3.69%). The comparative
in vitro release study revealed that CC-NLC-Opt showed significantly better (p<0.05) release and
enhanced permeation as compared to CC-suspension. The in vivo pharmacokinetic study gave many
folds increase in oral bioavailability than CC suspension, which was further confirmed by antihypertensive
activity in a murine model.
Conclusion: Thus, the results of ex vivo permeation, pharmacokinetic study and pharmacodynamics
study suggest the potential of CC-NLCs for improved oral delivery.