A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Pignatello, Rosario, Musumeci, Teresa, Graziano, Adriana C. E., Lo Furno, Debora, Varamini, Pegah, Mansfeld, Friederike M., Cardile, Venera and Toth, Istvan (2016) A study on liposomal encapsulation of a lipophilic prodrug of LHRH. Pharmaceutical Development and Technology, 21 6: 664-671. doi:10.3109/10837450.2015.1041045

Author Pignatello, Rosario
Musumeci, Teresa
Graziano, Adriana C. E.
Lo Furno, Debora
Varamini, Pegah
Mansfeld, Friederike M.
Cardile, Venera
Toth, Istvan
Title A study on liposomal encapsulation of a lipophilic prodrug of LHRH
Journal name Pharmaceutical Development and Technology   Check publisher's open access policy
ISSN 1097-9867
Publication date 2016-08-17
Year available 2016
Sub-type Article (original research)
DOI 10.3109/10837450.2015.1041045
Open Access Status Not Open Access
Volume 21
Issue 6
Start page 664
End page 671
Total pages 8
Place of publication Abingdon, Oxfordshire United Kingdom
Publisher Taylor & Francis
Language eng
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.
Keyword Amphiphilicity
Cell uptake
Fluorescence microscopy
Lipoamino acids
LUVET liposomes
MLV liposomes
REV liposomes
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: HERDC Pre-Audit
School of Chemistry and Molecular Biosciences
School of Pharmacy Publications
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