title: Lipidic spherulites: formulation optimisation by paired optical and cryoelectron microscopy.
abstract: Objective of this study was to assess the various steps leading to spherulite obtention by means of optical and cryoelectron microscopy. The formulation, resting and hydration steps were optimised. Green-based process and organic-based process were compared. It was found that spherulites could be obtained only when two key steps were followed: a prior resting phase of excipients and the shearing stress of the hydrated excipients. Moreover, the new formulation under study formed spherulites in the 100-200 nm range, which is smaller than previously reported spherulites. Such laboratory scale optimised process led the integration of spherulites in a larger number of prospective studies. Indeed, we finally showed that the encapsulated payload of a hydrophobic compound, such as the anti-angiogenic agent fisetin, was increased to a much higher degree than with a liposomal encapsulation.
authors.affiliation: Université Paris-Descartes - Paris Cité Sorbonne, Faculté des sciences pharmaceutiques et biologiques, Unité de Pharmacologie Chimique et Génétique et d'Imagerie, Paris, France. Electronic address: sylvie.crauste-manciet@parisdescartes.fr.
authors.forename: Sylvie
authors.initials: S
authors.lastname: Crauste-Manciet
authors.forename: Eric
authors.initials: E
authors.lastname: Larquet
authors.forename: Karel
authors.initials: K
authors.lastname: Khawand
authors.forename: Michel
authors.initials: M
authors.lastname: Bessodes
authors.forename: Guy G
authors.initials: GG
authors.lastname: Chabot
authors.forename: Denis
authors.initials: D
authors.lastname: Brossard
authors.forename: Nathalie
authors.initials: N
authors.lastname: Mignet
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry*; D020285:Cryoelectron Microscopy; D004337:Drug Carriers / Q000737:chemistry; D005079:Excipients; D005419:Flavonoids / Q000737:chemistry*; D044948:Flavonols; D057927:Hydrophobic and Hydrophilic Interactions; D008051:Lipid Bilayers / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D055095:Optics and Photonics; D010316:Particle Size; D033081:Shear Strength; D012997:Solvents / Q000737:chemistry
chemical_list: D020533:Angiogenesis Inhibitors; D004337:Drug Carriers; D005079:Excipients; D005419:Flavonoids; D044948:Flavonols; D008051:Lipid Bilayers; D008055:Lipids; D008081:Liposomes; D012997:Solvents; C017875:fisetin
keywords: Fisetin; Lipidic assemblies; Multilamellar vesicles; Onion phase; Spherulite; cryoTEM