TY - JOUR
T1 - Enhanced cutaneous bioavailability of dehydroepiandrosterone mediated by nano-encapsulation
AU - Badihi, Amit
AU - Debotton, Nir
AU - Frušić-Zlotkin, Marina
AU - Soroka, Yoram
AU - Neuman, Rami
AU - Benita, Simon
PY - 2014/9/10
Y1 - 2014/9/10
N2 - Polymeric nanocarriers, especially nanospheres (NSs) and nanocapsules (NCs), can promote the penetration of their cargo through the skin barrier, towards improved cutaneous bioavailability. Dehydroepiandrosterone (DHEA), an endogenous hormone exhibiting poor aqueous solubility, was shown to be effective in modulating skin-aging processes following topical application. In this study, we designed adequate DHEA preparations, in an attempt to enable local delivery of the active ingredient to the viable skin layers. In addition, the potential efficiency of DHEA NCs on dermal collagen synthesis was evaluated. Cryo-TEM observations and thermal analysis indicated that DHEA was successfully incorporated within a stable NC-based delivery system. Moreover, higher [ 3H]-DHEA levels were recorded in the viable skin layers following different incubation periods of NCs on excised pig skin specimens as compared to DHEA oil solution (free molecule). Furthermore, significantly higher (4-fold) skin flux values were observed for the DHEA NCs as compared to the values elicited by the oil control solution. Finally, collagen synthesis in human skin organ culture, assessed by the incorporation of [3H]-proline, was up to 42% higher for DHEA NCs 48 h post-topical application than for the untreated specimens. Overall, these results suggest that poly lactic-co-glycolic acid (PLGA)-based NCs have promising potential to be used topically for various skin disorders.
AB - Polymeric nanocarriers, especially nanospheres (NSs) and nanocapsules (NCs), can promote the penetration of their cargo through the skin barrier, towards improved cutaneous bioavailability. Dehydroepiandrosterone (DHEA), an endogenous hormone exhibiting poor aqueous solubility, was shown to be effective in modulating skin-aging processes following topical application. In this study, we designed adequate DHEA preparations, in an attempt to enable local delivery of the active ingredient to the viable skin layers. In addition, the potential efficiency of DHEA NCs on dermal collagen synthesis was evaluated. Cryo-TEM observations and thermal analysis indicated that DHEA was successfully incorporated within a stable NC-based delivery system. Moreover, higher [ 3H]-DHEA levels were recorded in the viable skin layers following different incubation periods of NCs on excised pig skin specimens as compared to DHEA oil solution (free molecule). Furthermore, significantly higher (4-fold) skin flux values were observed for the DHEA NCs as compared to the values elicited by the oil control solution. Finally, collagen synthesis in human skin organ culture, assessed by the incorporation of [3H]-proline, was up to 42% higher for DHEA NCs 48 h post-topical application than for the untreated specimens. Overall, these results suggest that poly lactic-co-glycolic acid (PLGA)-based NCs have promising potential to be used topically for various skin disorders.
KW - Collagen
KW - DHEA
KW - Nanocapsules
KW - Permeation
KW - PLGA
KW - Skin
UR - http://www.scopus.com/inward/record.url?scp=84903984909&partnerID=8YFLogxK
U2 - 10.1016/j.jconrel.2014.06.019
DO - 10.1016/j.jconrel.2014.06.019
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C2 - 24956487
AN - SCOPUS:84903984909
SN - 0168-3659
VL - 189
SP - 65
EP - 71
JO - Journal of Controlled Release
JF - Journal of Controlled Release
ER -