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.

• Amphiphilicity
• cell uptake
• fluorescence microscopy
• lipoamino acids
• LUVET liposomes
• MLV liposomes
• REV liposomes

Declaration of interest

This study was partly supported by the University of Catania (Ricerca di Ateneo). We would like to acknowledge the Australian Research Council for their support of this work with the Discovery Project Grant and Professorial Research Fellowship to I.T. (DP110100212). No conflict of interest must be declared by all the Authors.