TY - JOUR
T1 - A study on liposomal encapsulation of a lipophilic prodrug of LHRH
AU - Pignatello, Rosario
AU - Musumeci, Teresa
AU - Graziano, Adriana C.E.
AU - Lo Furno, Debora
AU - Varamini, Pegah
AU - Mansfeld, Friederike M.
AU - Cardile, Venera
AU - Toth, Istvan
PY - 2016/8/17
Y1 - 2016/8/17
N2 - 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.
AB - 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.
KW - Amphiphilicity
KW - cell uptake
KW - fluorescence microscopy
KW - lipoamino acids
KW - LUVET liposomes
KW - MLV liposomes
KW - REV liposomes
UR - http://www.scopus.com/inward/record.url?scp=84975258314&partnerID=8YFLogxK
U2 - 10.3109/10837450.2015.1041045
DO - 10.3109/10837450.2015.1041045
M3 - Article
C2 - 25946073
AN - SCOPUS:84975258314
SN - 1083-7450
VL - 21
SP - 664
EP - 671
JO - Pharmaceutical Development and Technology
JF - Pharmaceutical Development and Technology
IS - 6
ER -