title: Nanoemulsions (NEs), liposomes (LPs) and solid lipid nanoparticles (SLNs) for retinyl palmitate: effect on skin permeation.
abstract: 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.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Campus of Cartuja street s/n, 18071 Granada, Spain.
authors.forename: Beatriz
authors.initials: B
authors.lastname: Clares
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Barcelona, Joan XXIII Av. s/n, 08028 Barcelona, Spain.
authors.forename: Ana C
authors.initials: AC
authors.lastname: Calpena
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Barcelona, Joan XXIII Av. s/n, 08028 Barcelona, Spain.
authors.forename: Alexander
authors.initials: A
authors.lastname: Parra
authors.affiliation: Department of Physical Chemistry, School of Pharmacy, University of Barcelona, Joan XXIII Av. s/n, 08028 Barcelona, Spain.
authors.forename: Guadalupe
authors.initials: G
authors.lastname: Abrego
authors.affiliation: Department of Physical Chemistry, School of Pharmacy, University of Barcelona, Joan XXIII Av. s/n, 08028 Barcelona, Spain.
authors.forename: Helen
authors.initials: H
authors.lastname: Alvarado
authors.affiliation: CEBIMED, Research Centre for Biomedicine, Fernando Pessoa University, UFP-FCS, Praça 9 de Abril, 349, P-4249-004 Porto, Portugal; Faculty of Health Sciences, Fernando Pessoa University, UFP-FCS, Rua Carlos da Maia, 296, 4200-150 Porto, Portugal.
authors.forename: Joana F
authors.initials: JF
authors.lastname: Fangueiro
authors.affiliation: CEBIMED, Research Centre for Biomedicine, Fernando Pessoa University, UFP-FCS, Praça 9 de Abril, 349, P-4249-004 Porto, Portugal; Faculty of Health Sciences, Fernando Pessoa University, UFP-FCS, Rua Carlos da Maia, 296, 4200-150 Porto, Portugal; Institute of Biotechnology and Bioengineering, Centre of Genomics and Biotechnology, University of Trás-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal. Electronic address: eliana@ufp.edu.pt.
authors.forename: Eliana B
authors.initials: EB
authors.lastname: Souto
mesh_terms: D000975:Antioxidants / Q000008:administration & dosage* / Q000737:chemistry; D004224:Diterpenes; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D004655:Emulsions; D006801:Humans; D066298:In Vitro Techniques; D008055:Lipids / Q000008:administration & dosage* / Q000737:chemistry; D008081:Liposomes; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D000084562:Retinyl Esters; D012212:Rheology; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D014801:Vitamin A / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry
chemical_list: D000975:Antioxidants; D004224:Diterpenes; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D008081:Liposomes; D000084562:Retinyl Esters; D014801:Vitamin A; C014794:retinol palmitate
keywords: Liposomes; Nanoemulsions; Nanotechnology; Percutaneous penetration; Retinyl palmitate; Solid lipid nanoparticles