title: Menthosomes, novel ultradeformable vesicles for transdermal drug delivery: optimization and characterization.
abstract: Menthosomes, novel deformable carriers for the enhancement of transdermal delivery are introduced in this study. Meloxicam (MX)-loaded menthosomes were formulated, and their physicochemical characteristics and skin permeability were evaluated. A two-factor spherical and second-order composite experimental design was used to prepare the formulation of the menthosomes. Ten formulations of menthosomes composed of a phospholipid as the lipid bilayer carrier, cholesterol (Chol) as a stabilizer and cetylpyridinium chloride (CPC) and L-menthol as penetration enhancers were prepared. The amounts of Chol and CPC were selected as causal factors. Physicochemical characteristics (particle size, size distribution, zeta potential, elasticity and drug content) and an in vitro skin-permeation study of meloxicam-loaded menthosomes were evaluated. The concentrations of MX that permeated the skin at 2-12 h and the flux were selected as response variables. The optimal formulation was estimated using a nonlinear response-surface method incorporating thin-plate spline interpolation. The experimental values were very close to the values predicted by the computer programs in this study. A Bayesian network analysis was applied to gain a mechanistic understanding of the relationships between causal factors and response variables.
authors.affiliation: Department of Pharmaceutics, Hoshi University, Ebara 2–4–41, Shinagawa-ku, Tokyo 142–8501, Japan.
authors.forename: Sureewan
authors.initials: S
authors.lastname: Duangjit
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Obata
authors.forename: Hiromu
authors.initials: H
authors.lastname: Sano
authors.forename: Shingo
authors.initials: S
authors.lastname: Kikuchi
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Onuki
authors.forename: Praneet
authors.initials: P
authors.lastname: Opanasopit
authors.forename: Tanasait
authors.initials: T
authors.lastname: Ngawhirunpat
authors.forename: Yoshie
authors.initials: Y
authors.lastname: Maitani
authors.forename: Kozo
authors.initials: K
authors.lastname: Takayama
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002594:Cetylpyridinium / Q000737:chemistry; D002784:Cholesterol / Q000737:chemistry; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D066298:In Vitro Techniques; D008297:Male; D000077239:Meloxicam; D008610:Menthol / Q000737:chemistry; D051379:Mice; D008812:Mice, Hairless; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013843:Thiazines / Q000008:administration & dosage / Q000737:chemistry*; D013844:Thiazoles / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D004337:Drug Carriers; D013843:Thiazines; D013844:Thiazoles; D008610:Menthol; D002784:Cholesterol; D002594:Cetylpyridinium; D000077239:Meloxicam