TY - JOUR
T1 - Skin penetration behavior of lipid-core nanocapsules for simultaneous delivery of resveratrol and curcumin
AU - Friedrich, Rossana B.
AU - Kann, Birthe
AU - Coradini, Karine
AU - Offerhaus, Herman L.
AU - Beck, Ruy C.R.
AU - Windbergs, Maike
N1 - Funding Information:
The authors thank Dr. Chiara de Rossi for TEM image acquisition, Petra König for support with MTT tests and Peter Meiers for help with skin preparation. The German Academic Exchange Service (DAAD) and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) are acknowledged for financial support.
Publisher Copyright:
© 2015 Elsevier B.V.
PY - 2015/8/5
Y1 - 2015/8/5
N2 - Polyphenols, which are secondary plant metabolites, gain increasing research interest due to their therapeutic potential. Among them, resveratrol and curcumin are two agents showing antioxidant, anti-inflammatory, antimicrobial as well as anticarcinogenic effects. In addition to their individual therapeutic effect, increased activity was reported upon co-delivery of the two compounds. However, due to the poor water solubility of resveratrol and curcumin, their clinical application is currently limited. In this context, lipid-core nanocapsules (LNC) composed of an oily core surrounded by a polymeric shell were introduced as drug carrier systems with the potential to overcome this obstacle. Furthermore, the encapsulation of polyphenols into LNC can increase their photostability. As the attributes of the polyphenols make them excellent candidates for skin treatment, the aim of this study was to investigate the effect of co-delivery of resveratrol and curcumin by LNC upon topical application on excised human skin. In contrast to the formulation with one polyphenol, resveratrol penetrated into deeper skin layers when the co-formulation was applied. Based on vibrational spectroscopy analysis, these effects are most likely due to interactions of curcumin and the stratum corneum, facilitating the skin absorption of the co-administered resveratrol. Furthermore, the interaction of LNC with primary human skin cells was analyzed encountering a cellular uptake within 24 h potentially leading to intracellular effects of the polyphenols. Thus, the simultaneous delivery of resveratrol and curcumin by LNC provides an intelligent way for immediate and sustained polyphenol delivery for skin disease treatment.
AB - Polyphenols, which are secondary plant metabolites, gain increasing research interest due to their therapeutic potential. Among them, resveratrol and curcumin are two agents showing antioxidant, anti-inflammatory, antimicrobial as well as anticarcinogenic effects. In addition to their individual therapeutic effect, increased activity was reported upon co-delivery of the two compounds. However, due to the poor water solubility of resveratrol and curcumin, their clinical application is currently limited. In this context, lipid-core nanocapsules (LNC) composed of an oily core surrounded by a polymeric shell were introduced as drug carrier systems with the potential to overcome this obstacle. Furthermore, the encapsulation of polyphenols into LNC can increase their photostability. As the attributes of the polyphenols make them excellent candidates for skin treatment, the aim of this study was to investigate the effect of co-delivery of resveratrol and curcumin by LNC upon topical application on excised human skin. In contrast to the formulation with one polyphenol, resveratrol penetrated into deeper skin layers when the co-formulation was applied. Based on vibrational spectroscopy analysis, these effects are most likely due to interactions of curcumin and the stratum corneum, facilitating the skin absorption of the co-administered resveratrol. Furthermore, the interaction of LNC with primary human skin cells was analyzed encountering a cellular uptake within 24 h potentially leading to intracellular effects of the polyphenols. Thus, the simultaneous delivery of resveratrol and curcumin by LNC provides an intelligent way for immediate and sustained polyphenol delivery for skin disease treatment.
KW - Cellular uptake
KW - Co-encapsulation
KW - Curcumin
KW - Lipid-core nanocapsules
KW - Resveratrol
KW - Skin penetration
KW - 2023 OA procedure
UR - https://www.scopus.com/pages/publications/84938524223
U2 - 10.1016/j.ejps.2015.07.018
DO - 10.1016/j.ejps.2015.07.018
M3 - Article
C2 - 26215463
SN - 0928-0987
VL - 78
SP - 204
EP - 213
JO - European journal of pharmaceutical sciences
JF - European journal of pharmaceutical sciences
M1 - 3328
ER -