title: Calorimetry and Langmuir-Blodgett studies on the interaction of a lipophilic prodrug of LHRH with biomembrane models.
abstract: The interaction between an amphiphilic luteinizing hormone-releasing hormone (LHRH) prodrug that incorporated a lipoamino acid moiety (C12-LAA) with biological membrane models that consisted of multilamellar liposomes (MLVs) and phospholipid monolayers, was studied using Differential Scanning Calorimetry (DSC) and Langmuir-Blodgett film techniques. The effect of the prodrug C12[Q1]LHRH on the lipid layers was compared with the results obtained with the pure precursors, LHRH and C12-LAA. Conjugation of LHRH with a LAA promoiety showed to improve the peptide interaction with biomembrane models. Basing on the calorimetric findings, the LAA moiety aided the transfer of the prodrug from an aqueous solution to the biomembrane model.
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, Viale A. Doria, 6, 95125 Catania, Italy. Electronic address: mg.sarpietro@unict.it.
authors.forename: Maria G
authors.initials: MG
authors.lastname: Sarpietro
authors.affiliation: Department of Health Sciences, University "Magna Graecia" of Catanzaro, Campus "S. Venuta", Building of BioSciences, Viale S. Venuta, Germaneto, 88100 Catanzaro, Italy.
authors.forename: Maria L
authors.initials: ML
authors.lastname: Accolla
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, Viale A. Doria, 6, 95125 Catania, Italy.
authors.forename: Nancy
authors.initials: N
authors.lastname: Santoro
authors.affiliation: The University of Queensland, School of Chemistry and Molecular Biosciences (SCMB), Brisbane, Queensland 4072, Australia.
authors.forename: Friederike M
authors.initials: FM
authors.lastname: Mansfeld
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, Viale A. Doria, 6, 95125 Catania, Italy.
authors.forename: Rosario
authors.initials: R
authors.lastname: Pignatello
authors.affiliation: The University of Queensland, School of Chemistry and Molecular Biosciences (SCMB), Brisbane, Queensland 4072, Australia; The University of Queensland, School of Pharmacy, Brisbane, Queensland 4102, Australia.
authors.forename: Istvan
authors.initials: I
authors.lastname: Toth
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, Viale A. Doria, 6, 95125 Catania, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Castelli
mesh_terms: D001682:Biological Availability; D002151:Calorimetry / Q000379:methods*; D002152:Calorimetry, Differential Scanning; D002462:Cell Membrane; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000737:chemistry* / Q000493:pharmacokinetics; D008081:Liposomes; D008954:Models, Biological; D011355:Prodrugs / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D008081:Liposomes; D011355:Prodrugs; D007987:Gonadotropin-Releasing Hormone
keywords: Calorimetry; DMPC; DSC; Drug–membrane interaction; Langmuir–Blodgett film; Lipoamino acids; Liposomes; Prodrug