Abstract

Resveratrol (RSV) is a potent lipophilic antioxidant with a low aqueous solubility. Novel nanoformulations have been successfully developed and evaluated to increase the potential of resveratrol as a skin targeting antioxidant. Nanoformulations were prepared using a spontaneous emulsification method, and characterized and evaluated for their capabilities to penetrate/permeate the skin. In nanoformulations, the thermodynamic activity of the RSV penetration into/permeation through the skin was correlated with the thermodynamic activity of the RSV in the formulations. When terpenes were incorporated into the nanoformulations, the permeation of RSV through the skin increased and correlated with an increasing lipophilicity of the terpene. The nanoemulsion containing eugenol showed the highest RSV penetration into the stratum corneum (SC) and the epidermis-dermis-follicle region, whereas the limonene containing nanoemulsion had the highest RSV permeation through the skin (the enhancement ratios, compared to a saturated solution of RSV, were (i) 9.55 and (ii) 12.61, respectively, based on the average RSV amount (i) in each skin region and (ii) permeation through skin).

Highlights

  • Resveratrol (E-5-(4-hydroxystyryl) benzene-1,3-diol; RSV) is a potent natural polyphenolic antioxidant [1] that can be extracted abundantly from grape skin and seeds, berries, peanuts, and red wine

  • The nanoformulations all significantly increased the penetration of RSV in the stratum corneum (SC) and deeper skin tissues compared to the RSV-saturated solution, regardless of the terpene content (Figure 5a)

  • Surfactant-containing nanoformulations were chosen as they offer the advantages of a simplicity of fabrication, excellent solubilizing capacity, and attractive appearance

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Summary

Introduction

Resveratrol (E-5-(4-hydroxystyryl) benzene-1,3-diol; RSV) is a potent natural polyphenolic antioxidant [1] that can be extracted abundantly from grape skin and seeds, berries, peanuts, and red wine. Of particular relevance to this article, RSV has demonstrated a potential for antiaging effects and for protecting against UV damage in the skin due to its antioxidant and collagen stimulating activity [8,9]. AA rraannggee ooff aapppprrooaacchheess hhaavvee bbeeeenn iinnvveessttigigaateteddtotoiimmpprroovveetthhee ttooppiiccaallddeelilviveeryryooff RRSSVV,, iinncclluuddiinngg mmicircoro/n/annaoneomemulsuiolsnios n[s14[]1,4n],ionsioomsoems e[1s5][,15e]t,hoetshomoseosm[e1s6][,1n6]a,nonsapnoonsgpeosn[g1e7s], [1m7i]c,rompiacrrtoicpleasrt[i1c8le],s a[1n8d], naanndopnaarnticolpesar[t1i9c]l.eNs [a1n9o]/.mNicaroneom/mulisciroonesmpurolsviiodnespparrotivcuidlaer padarvtaicnutalgaersafdovraanttoapgiecsalfoprroadtuocptifcoarlmpurloadtiuonct bfeocramusuelathtieoynabreectraaunssepathreenyt aorpetitcraallnysipsoatrreonpticoapntidcaklilnyetiiscoatlrlyopstiacbalencdoklloinidesti[c2a0l]l.y stable colloids [20]. Transcutol® (Ethoxydiglycol - CAS# 111-90-0) were gifts from Gattefossé (Saint-Priest, France). Orthophosphoric acid, hematoxylin, eosin and ethanol were purchased from Thermo Fisher Scientific. (Ethoxydiglycol - CAS# 111-90-0) were gifts from Gattefossé (Saint-Priest, France). Orthophosphoric acid, hematoxylin, eosin and ethanol were purchased from Thermo Fisher Scientific (Scoresby, Australia). Deionised water was passed through a Milli Q apparatus (Millipore Corporation, Bedford, MA, USA)

Nanocarrier Development Strategy
Formulation of Nanoemulsions
Physical Characterization and Stability Evaluation
Experimental Set Up
Skin Distribution Study
HPLC Assay of Resveratrol
Data Analysis
Statistical Analysis
Physical Characteristics of RSV Nanoformulations
Effect of Modifying the Oil Phase and Surfactant Composition
Incorporation of Eugenol
Incorporation of Limonene and Eucalyptol
Stability of Nanoformulations
Discussion
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