In vivo biodistribution of edelfosine-loaded lipid nanoparticles radiolabeled with Technetium-99 m: Comparison of administration routes in mice
Keywords: 
Edelfosine
Lipid nanoparticles
Technetium-99m
Biodistribution
Issue Date: 
2022
Publisher: 
Elsevier
Project: 
info:eu-repo/grantAgreement/MICINN/Investigación fundamental no-orientada/SAF2010-15547/ES/NANOSISTEMAS PARA LA ADMINISTRACION ORAL DE AGENTES ANTITUMORALES ALQUIL-LISOFOSFOLIPIDICOS: DESARROLLO DE LOS NANOTRANSPORTADORES LIPIDICOS Y ESTUDIOS PRECLINICOS
ISSN: 
0939-6411
Note: 
This is an open access article under the CC BY-NC-ND license
Citation: 
Lasa-Saracibar, B. (Beatriz); El-Moukhtari, S.H. (Souhaila H.); Tsotakos, T. (Theodoros); et al. "In vivo biodistribution of edelfosine-loaded lipid nanoparticles radiolabeled with Technetium-99 m: Comparison of administration routes in mice". European Journal of Pharmaceutics and Biopharmaceutics. 175, 2022, 1 - 6
Abstract
Edelfosine (ET) is a potent antitumor agent but causes severe side effects that have limited its use in clinical practice. For this reason, nanoencapsulation in lipid nanoparticles (LNs) is advantageous as it protects from ET side-effects. Interestingly, previous studies showed the efficacy of LNs containing ET in various types of tumor. In this paper, biodistribution studies of nanoencapsulated ET, administered by three routes (oral, intravenous (IV) and intraperitoneal (IP)), were tested in order to select the optimal route of administration. To do this, ET-LNs were labeled with Technetium-99 m (99mTc) and administered by the oral, IV and IP route in mice. IV admin- istration of the radiolabeled LNs led to fast elimination from the blood circulation and increased accumulation in reticulo-endothelial (RES) organs, while their oral administration could not provide any evidence on their bio- distribution since large radiocomplexes were formed in the presence of gastrointestinal fluids. However, when the LNs were administered by the IP route they could access the systemic circulation and provided more constant blood ET-LN levels compared to the IV route. These findings suggest that the IP route can be used to sustain the level of drug in the blood and avoid accumulation in RES organs.

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