title: Skin penetration and deposition of carboxyfluorescein and temoporfin from different lipid vesicular systems: In vitro study with finite and infinite dosage application.
abstract: The aim of the present research is to evaluate the influence of different lipid vesicular systems as well as the effect of application mode on skin penetration and deposition behaviors of carboxyfluorescein (hydrophilic model drug) and temoporfin (lipophilic model drug). All of the lipid vesicular systems, including conventional liposomes, invasomes and ethosomes, were prepared by film hydration method and characterized for particle size distribution, ζ-potential, vesicular shape and surface morphology, in vitro human skin penetration and skin deposition. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) defined that all of lipid vesicles had almost spherical structures with low polydispersity (PDI < 0.2) and nanometric size range (z-average no more than 150 nm). In addition, all lipid vesicular systems exhibited a negative zeta potential. In vitro skin penetration and deposition experiments demonstrated that, in the case of CF with finite dose application (10 μl/cm²) and infinite dose application (160 μl/cm²), lipid vesicular systems, especially ethosomes and invasomes, compared with non-vesicular systems, can significantly improve the delivery of hydrophilic drug such as carboxyfluorescein into skin deep layers or across the skin. While in the case of mTHPC with finite and infinite dose application, most of drug accumulation was observed in the skin superficial layer for both lipid vesicular systems and non-vesicular systems. The results also revealed that the factors influencing the drug skin distribution concern the physicochemical characteristics of the drug, the choice of the vehicle formulation and the application mode applied.
authors.affiliation: Department of Pharmaceutical Technology, Friedrich-Schiller-University Jena, Lessing-str. 8, D-07743 Jena, Germany.
authors.forename: Ming
authors.initials: M
authors.lastname: Chen
authors.forename: Xiangli
authors.initials: X
authors.lastname: Liu
authors.forename: Alfred
authors.initials: A
authors.lastname: Fahr
mesh_terms: D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D005452:Fluoresceins / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D006860:Hydrogen Bonding; D057927:Hydrophobic and Hydrophilic Interactions; D066298:In Vitro Techniques; D008027:Light; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes; D008652:Mesoporphyrins / Q000737:chemistry / Q000493:pharmacokinetics*; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D010316:Particle Size; D010539:Permeability; D012542:Scattering, Radiation; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption / Q000187:drug effects*; D013050:Spectrometry, Fluorescence; D013499:Surface Properties; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D005452:Fluoresceins; D008055:Lipids; D008081:Liposomes; D008652:Mesoporphyrins; C024098:6-carboxyfluorescein; C072269:temoporfin