Volume 11,Issue 6
Construction and Transdermal Absorption Characteristics of Kongmian Shuibao Melatonin Transdermal Nano-Delivery System for Overcoming the First-Pass Effect
Oral administration of melatonin is severely limited by significant hepatic first-pass metabolism, low bioavailability, and high pharmacokinetic variability. To overcome these limitations, the Yixintang Kongmian Shuibao team developed a novel melatonin nano-composite formulation with an ultra-small particle size (10–15 nm). In vitro transdermal permeability across excised male Sprague-Dawley rat skin was evaluated using Franz diffusion cells, with melatonin concentrations quantified via high-performance liquid chromatography (HPLC). The nano-composite demonstrated significantly higher transdermal absorption profiles compared to conventional oral and benchmark formulations, achieving therapeutically effective doses required for human sleep regulation. Furthermore, a 7-day repeated dermal application study in rabbits confirmed zero incidence of erythema or edema, establishing superior skin compatibility. This nano-delivery system represents a highly promising non-invasive transdermal candidate for sleep improvement.
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