A study on liposomal encapsulation of a lipophilic prodrug of LHRH.
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.
['Pignatello|Rosario|R|', 'Musumeci|Teresa|T|', 'Graziano|Adriana C E|AC|', 'Lo Furno|Debora|D|', 'Varamini|Pegah|P|', 'Mansfeld|Friederike M|FM|', 'Cardile|Venera|V|', 'Toth|Istvan|I|']
D018938:Caco-2 Cells D002470:Cell Survival D004305:Dose-Response Relationship, Drug D004339:Drug Compounding D007987:Gonadotropin-Releasing Hormone D006801:Humans D015603:Keratinocytes D008081:Liposomes D011355:Prodrugs
Amphiphilicity lipoamino acids LUVET liposomes MLV liposomes REV liposomes cell uptake fluorescence microscopy