TY - JOUR
T1 - Nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) for retinyl palmitate
T2 - effect on skin permeation
AU - Clares, Beatriz
AU - Calpena, Ana C.
AU - Parra, Alexander
AU - Abrego, Guadalupe
AU - Alvarado, Helen
AU - Fangueiro, Joana F.
AU - Souto, Eliana B.
N1 - Funding Information:
The authors would like to thank to Gattefossé for kindly supplying the nanoemulsion ingredients used in this study and Hospital Barcelona-SCIAS (Barcelona, Spain) for providing skin samples. Spanish Ministry of Education, Culture and Sport is also acknowledged. Ms. Joana Fangueiro wishes to acknowledge Fundação para a Ciência e Tecnologia do Ministério da Ciência e Tecnologia (FCT, Portugal) under the reference SFRH/BD/80335/2011. FCT and European Funds ( FEDER and COMPETE ) are also acknowledged under the research project PTDC/SAU-FAR/113100/2009.
Publisher Copyright:
Copyright © 2014 Elsevier B.V. All rights reserved.
PY - 2014/10/1
Y1 - 2014/10/1
N2 - The aim of this study was to develop biocompatible lipid-based nanocarriers for retinyl palmitate (RP) to improve its skin delivery, photostability and biocompatibility, and to avoid undesirable topical side effects. RP loaded nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) were characterized in terms of size, surface electrical charge, pH, drug encapsulation efficiency and morphology. Spherical-shaped nanocarriers with a negatively charged surface (>|40|mV) and mean size lower than 275 nm were produced with adequate skin compatibility. The rheological properties showed that aqueous dispersions of SLNs followed a non-Newtonian behavior, pseudoplastic fluid adjusted to Herschel-Bulkley equation, whereas LPs and NEs exhibited a Newtonian behavior. SLNs offered significantly better photoprotection than LPs and NEs for RP. The cumulative amount of drug permeated through human skin at the end of 38 h was 6.67 ± 1.58 μg, 4.36 ± 0.21 μg and 3.64 ± 0.28 μg for NEs, LPs and SLNs, respectively. NEs flux was significantly higher than SLNs and LPs: NEs (0.37 ± 0.12 μg/h) > LPs (0.15 ± 0.09 μg/h) > SLNs (0.10 ± 0.05 μg/h). LPs offered significant higher skin retention than NEs and SLNs. Finally, even though all developed nanocarriers were found to be biocompatible, according to histological studies, NE was the system that most disrupted the skin. These encouraging findings can guide in proper selection of topical carriers among the diversity of available lipid-based nanocarriers, especially when a dermatologic or cosmetic purpose is desired.
AB - The aim of this study was to develop biocompatible lipid-based nanocarriers for retinyl palmitate (RP) to improve its skin delivery, photostability and biocompatibility, and to avoid undesirable topical side effects. RP loaded nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) were characterized in terms of size, surface electrical charge, pH, drug encapsulation efficiency and morphology. Spherical-shaped nanocarriers with a negatively charged surface (>|40|mV) and mean size lower than 275 nm were produced with adequate skin compatibility. The rheological properties showed that aqueous dispersions of SLNs followed a non-Newtonian behavior, pseudoplastic fluid adjusted to Herschel-Bulkley equation, whereas LPs and NEs exhibited a Newtonian behavior. SLNs offered significantly better photoprotection than LPs and NEs for RP. The cumulative amount of drug permeated through human skin at the end of 38 h was 6.67 ± 1.58 μg, 4.36 ± 0.21 μg and 3.64 ± 0.28 μg for NEs, LPs and SLNs, respectively. NEs flux was significantly higher than SLNs and LPs: NEs (0.37 ± 0.12 μg/h) > LPs (0.15 ± 0.09 μg/h) > SLNs (0.10 ± 0.05 μg/h). LPs offered significant higher skin retention than NEs and SLNs. Finally, even though all developed nanocarriers were found to be biocompatible, according to histological studies, NE was the system that most disrupted the skin. These encouraging findings can guide in proper selection of topical carriers among the diversity of available lipid-based nanocarriers, especially when a dermatologic or cosmetic purpose is desired.
KW - Liposomes
KW - Nanoemulsions
KW - Nanotechnology
KW - Percutaneous penetration
KW - Retinyl palmitate
KW - Solid lipid nanoparticles
UR - http://www.scopus.com/inward/record.url?scp=85027920363&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2014.08.001
DO - 10.1016/j.ijpharm.2014.08.001
M3 - Article
C2 - 25102113
AN - SCOPUS:85027920363
SN - 0378-5173
VL - 473
SP - 591
EP - 598
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -