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

doi:10.3109/10837450.2015.1041045

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 journal › Article › Research › peer-review

9 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 language	English
Pages (from-to)	664-671
Number of pages	8
Journal	Pharmaceutical Development and Technology
Volume	21
Issue number	6
DOIs	https://doi.org/10.3109/10837450.2015.1041045
Publication status	Published - 17 Aug 2016
Externally published	Yes

Keywords

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

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10.3109/10837450.2015.1041045

Cite this

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title = "A study on liposomal encapsulation of a lipophilic prodrug of LHRH",

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.",

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author = "Rosario Pignatello and Teresa Musumeci and Graziano, \{Adriana C.E.\} and \{Lo Furno\}, Debora and Pegah Varamini and Mansfeld, \{Friederike M.\} and Venera Cardile and Istvan Toth",

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doi = "10.3109/10837450.2015.1041045",

language = "English",

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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

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U2 - 10.3109/10837450.2015.1041045

DO - 10.3109/10837450.2015.1041045

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SN - 1083-7450

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SP - 664

EP - 671

JO - Pharmaceutical Development and Technology

JF - Pharmaceutical Development and Technology

IS - 6

ER -

A study on liposomal encapsulation of a lipophilic prodrug of LHRH

Abstract

Keywords

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