<p>Formulation And Evaluation Of Nanostructured Lipid Carriers (NLCs) Of 20(S)-Protopanaxadiol (PPD) By Box-Behnken Design</p>

Abstract

Background20(S)-Protopanaxadiol (PPD) has a higher anti-wrinkle effect than the other glycone forms of ginsenosides. However, as PPD has low solubility in water and a high molecular weight, it cannot easily penetrate the stratum corneum layer, which is the rate-limiting step of topical skin delivery. Thus, the objective was to enhance the topical skin deposition of PPD using an optimized nanostructured lipid carriers (NLC) formulation. NLC formulations were optimized using a Box-Behnken design.Materials and methodsNLC formulations were optimized using a Box-Behnken design, where the amount of PDD (X1), volume of the liquid lipid (X2), and amount of surfactant (X3) were set as the independent variables, while the particle size (Y1), polydispersity index (PDI) (Y2), and entrapment efficiency (EE) (Y3) were dependent factors. An in vitro deposition study was performed using Strat-M® and human cadaver skin, while in vivo skin irritation effect of the NLC formulation was evaluated in humans.ResultsAn NLC was successfully prepared based on the optimized formulation determined using the Box-Behnken design. The particle size, PDI, and EE of the NLC showed less than 5% difference from the predicted values. The in vitro deposition of PPD after the application of the NLC formulation on a Strat-M® artificial membrane and human cadaver skin was significantly higher than that of the controls. Moreover, NLC formulations with and without PDD were not skin irritants in a human study.ConclusionAn NLC formulation for the topical delivery of PPD was successfully optimized using the Box-Behnken design, and could be further developed to enhance the topical skin deposition of PPD.

Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol

“…Notably, the mean particle size of the NLCs formulations (F2, 498 nm; F4, 246 nm) containing Capmul MCM EP as an oil was larger than that of the SLNs formulations (F1, 165 nm; F3, 133 nm). This increase in particle size is consistent with other previous studies that have reported larger sizes in NLCs formulations when oil is added into the solid lipid phase of SLNs [ 30 , 31 , 32 ]. However, the high EE (>95%) and orobol content (≈1.0%) in the F1–F4 formulations were not significantly affected by the existence of oil and an increase of particle size.…”

Orobol from enzyme biotransformation attenuatesDermatophagoides farinae-induced atopic dermatitis-like symptoms in NC/Nga mice

“…For these reasons, many researchers are searching for new phytochemicals with use as topical formulations to increase their stability and delivery efficiency. [30][31][32][33][34] In this study, for the first time, we found a metabolite of genistein, orobol, which has anti-atopic effects in animals and cell models.…”

Finasteride-loaded nano-lipidic carriers for follicular drug delivery: preformulation screening and Box-Behnken experimental design for optimization of variables

“…The dependent variables selected were mean particles size (Y 1 ), zeta potential (Y 2 ) and encapsulation efficiency (Y 3 ). The lower (−1), medium (0) and higher (+1) values for each factor were selected on the basis of literature survey [ 12 , 24 , 25 ]. The data analysis was performed by ANOVA.…”