Evaluation of percutaneous absorption of naproxen from different liposomal formulations.
The present study concerns the percutaneous absorption of naproxen (NPX), as model anti-inflammatory drug, included in liposome formulations constituted of different lipids: stratum corneum lipids (SCL) and phosphatidylcholine/cholesterol (PC/CHOL). Liposome dispersions were produced using two different methods: reverse-phase evaporation (REV) and thin layer evaporation (TLE). Morphology and dimensions of the disperse phase were characterized by cryo-transmission electron microscopy (cryo-TEM) and photon correlation spectroscopy, respectively. X-ray diffraction was employed to determine the structural organization of the vesicles. In vitro diffusion was studied by Franz cell on liposome dispersions viscosized by carbomer. Tape stripping was performed to investigate in vivo the performance of differently composed liposomes as NPX delivery system. Cryo-TEM showed spherical vesicles and bigger irregular elongated nanoparticles for TLE SCL liposomes. REV resulted in spherical and elongated multilamellar vesicles. Also X-ray diffraction evidenced L alpha or L beta multilamellar vesicles for PC/CHOL and SCL liposome respectively. The in vitro study showed a lower NPX flux for SCL with respect to PC/CHOL liposome. Tape stripping corroborate the in vitro findings regarding SCL, suggesting that liposomes create a drug reservoir mixing with SC lipids, whilst PC/CHOL liposome promoted NPX permeation through the skin. Liposome lipid composition seems to affect NPX permeation through the skin.
Puglia
Carmelo
C
Department of Pharmaceutical Sciences, University of Catania, Catania, Italy. capuglia@unict.it
Bonina
Francesco
F
Rizza
Luisa
L
Cortesi
Rita
R
Merlotti
Elena
E
Drechsler
Markus
M
Mariani
Paolo
P
Contado
Catia
C
Ravani
Laura
L
Esposito
Elisabetta
E
D000279:Administration, Cutaneous; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000378:metabolism; D020285:Cryoelectron Microscopy; D004304:Dosage Forms; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry*; D009288:Naproxen / Q000378:metabolism; D010713:Phosphatidylcholines / Q000378:metabolism; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects*; D014961:X-Ray Diffraction; D014965:X-Rays
D004304:Dosage Forms; D008055:Lipids; D008081:Liposomes; D010713:Phosphatidylcholines; D009288:Naproxen; D002784:Cholesterol