Abstract
The present work was designed to formulate and statistically optimize transdermal amlodipine nanostructured lipid carriers (AMNLCs) using lipid blends. The formulation was optimized by using the independent variables Peceol (liquid lipid as X1), GMS (solid lipid as X2) and Tween-80 concentration (surfactant as X3). Their effects were assessed on dependent variables particle size (Y1), transdermal flux (Y2), and entrapment efficiency (Y3). The optimized formulation was further evaluated for in vitro drug release, confocal laser scanning microscopy, physicochemical evaluation, and in-vivo absorption study. The optimized amlodipine nanostructured lipid carriers (AMNLCopt) showed low particle size (123.8 nm), enhanced transdermal flux (58.33 μg/cm2/h), and higher entrapment efficiency (88.11%). Further, it showed prolonged drug release and followed higuchi release kinetics with R2 closer to unity. The rhodamine red (RR) loaded RR-AMNLCopt revealed an enhanced permeation to the deeper layer of the skin after assessing through confocal laser scanning microscopy (CLSM). The in-vivo absorption study presented enhanced improvement in bioavailability of amlodipine in the wistar rats. From the study, it was concluded that the experimental design based AMNLCs showed the quadratic relationship between independent and dependent variables and also found to be a proficient carrier for transdermal delivery of amlodipine.
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•Amlodipine loaded nanostructured lipid carriers using Peceol, GMS and Tween-80.•AM-NLCopt showed lower particle size, higher transdermal flux and entrapment efficiency.•Rhodamine loaded AMNLCopt showed an enhanced permeation to the deeper layers of the skin.•The transdermal absorption study presented enhanced improvement in bioavailability.•The formulation was also assessed for skin interaction study and found to be safe.