A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Rosario Pignatello, Teresa Musumeci, Adriana C.E. Graziano, Debora Lo Furno, Pegah Varamini, Friederike M. Mansfeld, Venera Cardile, Istvan Toth

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)664-671
Number of pages8
JournalPharmaceutical Development and Technology
Volume21
Issue number6
DOIs
Publication statusPublished - 17 Aug 2016
Externally publishedYes

Keywords

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

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