A study on liposomal encapsulation of a lipophilic prodrug of LHRH

作者：Pignatello Rosario^*; Musumeci Teresa; Graziano Adriana C E; Lo Furno Debora; Varamini Pegah; Mansfeld Friederike M; Cardile Venera; Toth Istvan

来源：Pharmaceutical Development and Technology, 2016, 21(6): 664-671.

DOI：10.3109/10837450.2015.1041045

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

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.

• 出版日期2016-9