title: A study on liposomal encapsulation of a lipophilic prodrug of LHRH.
abstract: This study aimed at evaluating whether derivatization of luteinizing hormone-releasing hormone (LHRH) peptide with an amphiphilic lipoamino acid moiety could allow, along with other technological and/or pharmacokinetic advantages, to improve its encapsulation in liposomes, potentially driving its further body distribution and cellular uptake. Experimental data confirmed that a lipophilic derivative of LHRH was efficiently incorporated in various liposomal systems, differing in lipid composition and surface charge, and obtained using different methods of production. Incubation of liposomes, loaded with a fluorescent derivative of the LHRH prodrug, with NCTC keratinocytes or Caco-2 cell cultures showed that the carriers can be rapidly internalized. Conversely, the internalization of the free prodrug occurred only at very high concentrations.
authors.affiliation: a Section of Pharmaceutical Technology, Department of Drug Sciences and.
authors.forename: Rosario
authors.initials: R
authors.lastname: Pignatello
authors.affiliation: a Section of Pharmaceutical Technology, Department of Drug Sciences and.
authors.forename: Teresa
authors.initials: T
authors.lastname: Musumeci
authors.affiliation: b Section of Physiology, Department of Bio-medical Sciences , University of Catania , Catania , Italy .
authors.forename: Adriana C E
authors.initials: AC
authors.lastname: Graziano
authors.affiliation: b Section of Physiology, Department of Bio-medical Sciences , University of Catania , Catania , Italy .
authors.forename: Debora
authors.initials: D
authors.lastname: Lo Furno
authors.affiliation: c School of Chemistry and Molecular Biosciences (SCMB) , and.
authors.forename: Pegah
authors.initials: P
authors.lastname: Varamini
authors.affiliation: c School of Chemistry and Molecular Biosciences (SCMB) , and.
authors.forename: Friederike M
authors.initials: FM
authors.lastname: Mansfeld
authors.affiliation: b Section of Physiology, Department of Bio-medical Sciences , University of Catania , Catania , Italy .
authors.forename: Venera
authors.initials: V
authors.lastname: Cardile
authors.affiliation: c School of Chemistry and Molecular Biosciences (SCMB) , and.|d School of Pharmacy, The University of Queensland, Brisbane , Queensland , Australia.
authors.forename: Istvan
authors.initials: I
authors.lastname: Toth
mesh_terms: D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding; D007987:Gonadotropin-Releasing Hormone / Q000008:administration & dosage* / Q000378:metabolism*; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects / Q000378:metabolism; D008081:Liposomes; D011355:Prodrugs / Q000008:administration & dosage* / Q000378:metabolism*
chemical_list: D008081:Liposomes; D011355:Prodrugs; D007987:Gonadotropin-Releasing Hormone
keywords: Amphiphilicity; LUVET liposomes; MLV liposomes; REV liposomes; cell uptake; fluorescence microscopy; lipoamino acids