Nanostructured lipid carrier loaded with Zingiber officinale oil to enhance transdermal bioactive delivery for topical formulation

Abstract

This study reported on the enhancement of Zingiber officinale (Z. officinale) oil delivery, a bioactive with poor water solubility, by incorporating it into nanostructured lipid carriers (NLC) for transdermal bioactive delivery in topical formulations using the ultrasonication technique with a D–optimal mixture design approach. The independent factors in the process included the percentage of Z. officinale oil, solid lipid (glyceryl monostearate (GMS)), and liquid lipid (virgin coconut oil (VCO)). The study characterized the NLC– Z. officinale oil formulation based on particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) as the dependent variables. Besides, Transmission Electron Microscopy (TEM), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflection (FTIR–ATR), and Differential Scanning Calorimetry (DSC) were also employed. The optimized NLC–Z. officinale oil formulation, comprising 0.36 % Z. officinale oil, 0.14 % solid lipid (GMS), and 0.50 % liquid lipid (VCO). The study's results demonstrated that the finely tuned NLC– Z. officinale oil formulation, with an average diameter of 90.71 ± 9.48 nm, a PDI of 0.147 ± 0.01, a ZP of –45.7 ± 0.67 mV, and an EE of 88.80 ± 11.18 %, exhibited a controlled and sustained release profile following the Korsmeyer–Peppas model. The in vitro penetration studies on excised Sprague–Dawley rat skin and Strat–M® showcased the heightened penetration flux of NLC–Z. officinale oil compared to Z. officinale oil. Furthermore, in vivo distribution studies in female Sprague–Dawley rats underscored the deep penetration of NLCs into the dermal layer after 12 h of application. Notably, a 3–hour treatment with NLC–Z. officinale oil triggered the release of free fatty acids (FFA). The 90 days storage stability study revealed no significant changes in NLC– Z. officinale oil concerning PS and PDI, affirming its stability over time. These findings illuminated the potential applications of NLC– Z. officinale oil as a robust transdermal bioactive delivery system for Z. officinale oil. This underscored its significance in pharmaceutical formulations, providing a novel avenue for therapeutic purposes.