Design, formulation, in-vitro and in-vivo pharmacokinetic evaluation of Nicardipine- nanostructured lipid carrier for transdermal drug delivery system

Nicardipine hydrochloride (NCP), a calcium channel blocker, may be useful for treating chronic stable angina and hypertension through a therapeutic transdermal system because it has a low dose, short half-life, and high first-pass metabolism. This study used a hydrogel incorporating nanostructured lipid carriers (NLCs) to enhance NCP retention and skin permeability. The NLCs formula was fine-tuned using a Central composite design with three factors and three levels. The effects of sonication time, lipid concentration, and surfactant concentration on particle size, Entrapment Efficiency (EE), and polydispersity index (PDI) were also studied. There were two main components to the strategy that allowed it to succeed. Mean particle size in the optimized formulation was 107.78 nm, and the entrapment efficiency was 70.52%. Drug loading was 6.59%. A pharmaceutical release research discovered that NCP has a half-life of 10 h in vitro. The selected formulation was then placed into a Carbopol gel, and ex-vivo permeation studies showed that the gel with NLCs provided more penetration (66.45%) and longer sustained release (up to 11 h) than the free drug-based gel. The gel used in NLCs is especially notable for limiting systemic access and minimizing the risk of side effects from free drug. The in-vivo absorption study shown that NCP bioavailability was greatly improved in wistar rats. Using an experimental methodology, we found that NCP-NLCs could efficiently transport NCP across the skin by transdermal injection, and that there was a quadratic relationship between the variables of interest.