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 language | English |
|---|---|
| Pages (from-to) | 333-346 |
| Number of pages | 14 |
| Journal | International Journal of Pharmaceutics |
| Volume | 465 |
| Issue number | 1-2 |
| DOIs | |
| Publication status | Published - Apr 25 2014 |
| Externally published | Yes |
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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 journal › Article
}
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 -