title: Temoporfin-loaded invasomes: development, characterization and in vitro skin penetration studies.
abstract: Temoporfin (mTHPC) is a highly hydrophobic second generation photosensitizer with low percutaneous penetration. In order to enhance its percutaneous penetration it was necessary to develop a mTHPC-loaded drug carrier system for enhanced skin delivery. mTHPC-loaded invasomes were developed, characterized and investigated for the in vitro percutaneous penetration of mTHPC into abdominal human skin using Franz diffusion cells. mTHPC-loaded invasomes were prepared using non-hydrogenated soybean lecithin (10% w/v), ethanol (3.3% w/v) and a mixture of terpenes (0.5 and 1% w/v). The invasomes obtained were of a sufficiently small particle size (<150 nm) and polydispersity index (<0.3). The particle size of invasomes increased following an increase in the amount of terpenes in the invasomes. All invasomes possessed a negative surface charge. The vesicles appeared to be unilamellar and oligolamellar, spherical and oval in shape. An interesting phenomenon was the finding that with increasing the amount of terpenes, the number of deformed vesicles in the dispersion increased. In vitro skin penetration data revealed that the invasome dispersion with 1% of the mixture of terpenes showed a significantly enhanced deposition (p<0.05) of the drug in the SC compared to liposomes without terpenes and the ethanolic solution.
authors.affiliation: Department of Pharmaceutical Technology, Friedrich Schiller University Jena, Lessingstrasse 8, 07743 Jena, Germany. ninadragicevic@hotmail.com
authors.forename: Nina
authors.initials: N
authors.lastname: Dragicevic-Curic
authors.forename: Dietrich
authors.initials: D
authors.lastname: Scheglmann
authors.forename: Volker
authors.initials: V
authors.lastname: Albrecht
authors.forename: Alfred
authors.initials: A
authors.lastname: Fahr
mesh_terms: D000279:Administration, Cutaneous; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D066298:In Vitro Techniques; D008652:Mesoporphyrins / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D010316:Particle Size; D010539:Permeability; D017319:Photosensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D012867:Skin / Q000187:drug effects / Q000378:metabolism*
chemical_list: D004337:Drug Carriers; D008652:Mesoporphyrins; D017319:Photosensitizing Agents; C072269:temoporfin