title: Evaluation of the versatile character of a nanoemulsion formulation.
abstract: The formulate-ability of six model active pharmaceutical ingredients (API), with different physico-chemical profiles, in a nanoemulsion designed to be intraveinously administrable was explored. Nanoemulsions were spontaneously generated at room temperature by pouring a phosphate buffer in an anhydrous mixture containing pharmaceutically acceptable triglycerides and non-ionic surfactants. After determination of the apparent solubility of each API in excipients and characterization of mixtures by DSC, API-loaded nanoemulsions were formulated and characterized in terms of granulometric properties, surface potential, drug recovery efficiency, pH, osmolarity, in vitro drug release, and stability. Except ciprofloxacin, a BCS class IV drug, all studied APIs were soluble in at least one excipient used, i.e. Labrasol. At 2 wt% API, all drug-loaded nanoemulsions present properties compatible with i.v. administration. The formulation should permit to increase apparent solubility of poorly water-soluble APIs, and also to prolong delivery of hydrophobic as well of more hydrophilic compounds. Herein, the relative affinity of the API for nanodroplets and the release medium would directly influence drug release profiles. Nanoemulsions were stable for 7 days. They could also been extemporaneously reconstituted before use. Such a versatile nanoemulsion would provide a valuable option as formulation strategy for improvement of drug properties.
authors.affiliation: Université Caen Normandie, France; UNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie - FR CNRS INC3M - SF 4206 ICORE, UFR des Sciences Pharmaceutiques, Bd Becquerel), F-14032 Caen, France.
authors.forename: E
authors.initials: E
authors.lastname: Gué
authors.affiliation: Université Caen Normandie, France; UNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie - FR CNRS INC3M - SF 4206 ICORE, UFR des Sciences Pharmaceutiques, Bd Becquerel), F-14032 Caen, France.
authors.forename: M
authors.initials: M
authors.lastname: Since
authors.affiliation: Université Caen Normandie, France; UNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie - FR CNRS INC3M - SF 4206 ICORE, UFR des Sciences Pharmaceutiques, Bd Becquerel), F-14032 Caen, France.
authors.forename: S
authors.initials: S
authors.lastname: Ropars
authors.affiliation: Laboratoire de Chimie Moléculaire et Thioorganique, UMR CNRS 6507, INC3 M FR 3038, ENSICAEN & Université de Caen, 14050 Caen, France.
authors.forename: R
authors.initials: R
authors.lastname: Herbinet
authors.affiliation: Laboratoire de Chimie Moléculaire et Thioorganique, UMR CNRS 6507, INC3 M FR 3038, ENSICAEN & Université de Caen, 14050 Caen, France.
authors.forename: L
authors.initials: L
authors.lastname: Le Pluart
authors.affiliation: Université Caen Normandie, France; UNICAEN, CERMN (Centre d'Etudes et de Recherche sur le Médicament de Normandie - FR CNRS INC3M - SF 4206 ICORE, UFR des Sciences Pharmaceutiques, Bd Becquerel), F-14032 Caen, France. Electronic address: aurelie.malzert-freon@unicaen.fr.
authors.forename: A
authors.initials: A
authors.lastname: Malzert-Fréon
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry / Q000493:pharmacokinetics; D053758:Nanoparticles / Q000737:chemistry* / Q000378:metabolism; D013501:Surface-Active Agents / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D004655:Emulsions; D005989:Glycerides; D013501:Surface-Active Agents; C440220:Labrasol
keywords: Apparent solubility; Labrasol(®); Nanoemulsion; Parenteral administration; Self-emulsification