Design and optimization of candesartan loaded self-nanoemulsifying drugdelivery system for improving its dissolution rate and pharmacodynamicpotential

摘要

During the last decades, much attention has been focused on SNEDDS approach to resolveconcerns of BCS II class drugs with accentuation on upgrading the solubility andbioavailability. The present hypothesis confirms the theory that SNEDDS can reduce theimpact of food on Candesartan solubilization, thereby offering the potential for improvedoral delivery without co-administration with meals. The present studies describequality-by-design-based development and characterization of Candesartan loaded SNEDDS forimproving its pharmacodynamic potential. D-optimal mixture design was used for systematicoptimization of SNEDDS, which showed globule size of 13.91 nm, more rapid drug releaserate of >90% in 30 min and 16 s for self-emulsification. The optimized formulationswere extensively evaluated, where an drug release studyindicated up to 1.99- and 1.10-fold enhancement in dissolution rate from SNEDDS over puredrug and marketed tablet. pharmacodynamic investigation alsoshowed superior antihypertensive potential of SNEDDS in normalizing serum lipid levels ascompared to pure drug and marketed tablet that was executed on male Wistar rats. Overall,this paper reports successful systematic development of candesartan-loaded SNEDDS withdistinctly improved biopharmaceutical performance. This research work interpreted a majorrole of SNEDDS for enhancing the rate of dissolution and bioavailability of poorly watersoluble drugs.