Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome

Eirini A. Fragogeorgi, Irina N. Savina, Theodoros Tsotakos, Elen Efthimiadou, Stavros Xanthopoulos, Lazaros Palamaris, Dimitrios Psimadas, Penelope Bouziotis, George Kordas, Sergey Mikhalovsky, Mohammad Alavijeh, George Loudos

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Liposomes radiolabelling with diagnostic radionuclides is an excellent tool for studying pharmacokinetics with the view of developing liposome-based drug delivery agents. The aim of the present study is to evaluate the in vitro and in vivo behavior of a 99mTc-labeled liposome by applying either a direct labeling strategy via a carboxyl group, LP-COOH, or a surface chelating method via pyridyl ethyl cysteine compound (with the intermediate [ 99mTc(I)(CO)3(H2O)3] +), LP-PEC. 99mTc-LP-COOH was obtained in high radiolabelling yield and radiochemical purity, while 99mTc (I)(CO)3-LP-PEC was initially purified before being in vitro and in vivo evaluated. 99mTc-LP-COOH was less stable in the presence of competitive for 99mTc ligands than 99mTc (I)(CO)3-LP-PEC. According to DLS measurements, the presence of serum as well as the applied radiolabelling conditions did not affect the liposomes' size. The different radiolabelling methods seemed to exert an influence on the biodistribution pattern of the liposomes with the 99mTc(I)(CO)3-LP-PEC showing slow blood clearance, which was also confirmed by in vivo scintigraphic imaging. Nevertheless, passive tumor targeting was attained at a similar extent no matter which radiolabelling technique was followed.

Original languageEnglish
Pages (from-to)333-346
Number of pages14
JournalInternational Journal of Pharmaceutics
Volume465
Issue number1-2
DOIs
Publication statusPublished - Apr 25 2014
Externally publishedYes

Fingerprint

Carbon Monoxide
Liposomes
Neoplasms
Radioisotopes
Pharmacokinetics
In Vitro Techniques
Ligands
Serum
Pharmaceutical Preparations

Keywords

  • Direct labeling
  • Passive targeting
  • Pegylated liposome
  • Scintigraphic imaging
  • Surface chelation labeling

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

Cite this

Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome. / Fragogeorgi, Eirini A.; Savina, Irina N.; Tsotakos, Theodoros; Efthimiadou, Elen; Xanthopoulos, Stavros; Palamaris, Lazaros; Psimadas, Dimitrios; Bouziotis, Penelope; Kordas, George; Mikhalovsky, Sergey; Alavijeh, Mohammad; Loudos, George.

In: International Journal of Pharmaceutics, Vol. 465, No. 1-2, 25.04.2014, p. 333-346.

Research output: Contribution to journalArticle

Fragogeorgi, EA, Savina, IN, Tsotakos, T, Efthimiadou, E, Xanthopoulos, S, Palamaris, L, Psimadas, D, Bouziotis, P, Kordas, G, Mikhalovsky, S, Alavijeh, M & Loudos, G 2014, 'Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome', International Journal of Pharmaceutics, vol. 465, no. 1-2, pp. 333-346. https://doi.org/10.1016/j.ijpharm.2014.01.042
Fragogeorgi, Eirini A. ; Savina, Irina N. ; Tsotakos, Theodoros ; Efthimiadou, Elen ; Xanthopoulos, Stavros ; Palamaris, Lazaros ; Psimadas, Dimitrios ; Bouziotis, Penelope ; Kordas, George ; Mikhalovsky, Sergey ; Alavijeh, Mohammad ; Loudos, George. / Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome. In: International Journal of Pharmaceutics. 2014 ; Vol. 465, No. 1-2. pp. 333-346.
@article{5ea646cba24a4b85ac49e1659fc1b3c3,
title = "Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome",
abstract = "Liposomes radiolabelling with diagnostic radionuclides is an excellent tool for studying pharmacokinetics with the view of developing liposome-based drug delivery agents. The aim of the present study is to evaluate the in vitro and in vivo behavior of a 99mTc-labeled liposome by applying either a direct labeling strategy via a carboxyl group, LP-COOH, or a surface chelating method via pyridyl ethyl cysteine compound (with the intermediate [ 99mTc(I)(CO)3(H2O)3] +), LP-PEC. 99mTc-LP-COOH was obtained in high radiolabelling yield and radiochemical purity, while 99mTc (I)(CO)3-LP-PEC was initially purified before being in vitro and in vivo evaluated. 99mTc-LP-COOH was less stable in the presence of competitive for 99mTc ligands than 99mTc (I)(CO)3-LP-PEC. According to DLS measurements, the presence of serum as well as the applied radiolabelling conditions did not affect the liposomes' size. The different radiolabelling methods seemed to exert an influence on the biodistribution pattern of the liposomes with the 99mTc(I)(CO)3-LP-PEC showing slow blood clearance, which was also confirmed by in vivo scintigraphic imaging. Nevertheless, passive tumor targeting was attained at a similar extent no matter which radiolabelling technique was followed.",
keywords = "Direct labeling, Passive targeting, Pegylated liposome, Scintigraphic imaging, Surface chelation labeling",
author = "Fragogeorgi, {Eirini A.} and Savina, {Irina N.} and Theodoros Tsotakos and Elen Efthimiadou and Stavros Xanthopoulos and Lazaros Palamaris and Dimitrios Psimadas and Penelope Bouziotis and George Kordas and Sergey Mikhalovsky and Mohammad Alavijeh and George Loudos",
year = "2014",
month = "4",
day = "25",
doi = "10.1016/j.ijpharm.2014.01.042",
language = "English",
volume = "465",
pages = "333--346",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-2",

}

TY - JOUR

T1 - Comparative in vitro stability and scintigraphic imaging for trafficking and tumor targeting of a directly and a novel 99mTc (I)(CO)3 labeled liposome

AU - Fragogeorgi, Eirini A.

AU - Savina, Irina N.

AU - Tsotakos, Theodoros

AU - Efthimiadou, Elen

AU - Xanthopoulos, Stavros

AU - Palamaris, Lazaros

AU - Psimadas, Dimitrios

AU - Bouziotis, Penelope

AU - Kordas, George

AU - Mikhalovsky, Sergey

AU - Alavijeh, Mohammad

AU - Loudos, George

PY - 2014/4/25

Y1 - 2014/4/25

N2 - Liposomes radiolabelling with diagnostic radionuclides is an excellent tool for studying pharmacokinetics with the view of developing liposome-based drug delivery agents. The aim of the present study is to evaluate the in vitro and in vivo behavior of a 99mTc-labeled liposome by applying either a direct labeling strategy via a carboxyl group, LP-COOH, or a surface chelating method via pyridyl ethyl cysteine compound (with the intermediate [ 99mTc(I)(CO)3(H2O)3] +), LP-PEC. 99mTc-LP-COOH was obtained in high radiolabelling yield and radiochemical purity, while 99mTc (I)(CO)3-LP-PEC was initially purified before being in vitro and in vivo evaluated. 99mTc-LP-COOH was less stable in the presence of competitive for 99mTc ligands than 99mTc (I)(CO)3-LP-PEC. According to DLS measurements, the presence of serum as well as the applied radiolabelling conditions did not affect the liposomes' size. The different radiolabelling methods seemed to exert an influence on the biodistribution pattern of the liposomes with the 99mTc(I)(CO)3-LP-PEC showing slow blood clearance, which was also confirmed by in vivo scintigraphic imaging. Nevertheless, passive tumor targeting was attained at a similar extent no matter which radiolabelling technique was followed.

AB - Liposomes radiolabelling with diagnostic radionuclides is an excellent tool for studying pharmacokinetics with the view of developing liposome-based drug delivery agents. The aim of the present study is to evaluate the in vitro and in vivo behavior of a 99mTc-labeled liposome by applying either a direct labeling strategy via a carboxyl group, LP-COOH, or a surface chelating method via pyridyl ethyl cysteine compound (with the intermediate [ 99mTc(I)(CO)3(H2O)3] +), LP-PEC. 99mTc-LP-COOH was obtained in high radiolabelling yield and radiochemical purity, while 99mTc (I)(CO)3-LP-PEC was initially purified before being in vitro and in vivo evaluated. 99mTc-LP-COOH was less stable in the presence of competitive for 99mTc ligands than 99mTc (I)(CO)3-LP-PEC. According to DLS measurements, the presence of serum as well as the applied radiolabelling conditions did not affect the liposomes' size. The different radiolabelling methods seemed to exert an influence on the biodistribution pattern of the liposomes with the 99mTc(I)(CO)3-LP-PEC showing slow blood clearance, which was also confirmed by in vivo scintigraphic imaging. Nevertheless, passive tumor targeting was attained at a similar extent no matter which radiolabelling technique was followed.

KW - Direct labeling

KW - Passive targeting

KW - Pegylated liposome

KW - Scintigraphic imaging

KW - Surface chelation labeling

UR - http://www.scopus.com/inward/record.url?scp=84898601984&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84898601984&partnerID=8YFLogxK

U2 - 10.1016/j.ijpharm.2014.01.042

DO - 10.1016/j.ijpharm.2014.01.042

M3 - Article

VL - 465

SP - 333

EP - 346

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -