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Merck
  • Development of a novel lipophilic, magnetic nanoparticle for in vivo drug delivery.

Development of a novel lipophilic, magnetic nanoparticle for in vivo drug delivery.

Pharmaceutics (2013-12-05)
Thomas Linemann, Louiza B Thomsen, Kristian G du Jardin, Jens C Laursen, Jesper B Jensen, Jacek Lichota, Torben Moos
摘要

The aim of the present study was to evaluate the transfection potential of chitosan-coated, green-fluorescent magnetic nanoparticles (MNPs) (chi-MNPs) after encapsulation inside polyethylglycol (PEG)ylated liposomes that produced lipid-encapsulated chitosan-coated MNPs (lip-MNPs), and also to evaluate how these particles would distribute in vivo after systemic injection. The transfection potential of both chi-MNPs and lip-MNPs was evaluated in vitro in rat brain endothelial 4 (RBE4) cells with and without applying a magnetic field. Subsequently, the MNPs were evaluated in vivo in young rats. The in vitro investigations revealed that the application of a magnetic field resulted in an increased cellular uptake of the particles. The lip-MNPs were able to transfect the RBE4 cells with an incidence of approximately 20% of a commercial transfection agent. The in vivo distribution studies revealed that lip-MNPs had superior pharmacokinetic properties due to evasion of the RES, including hepatic Kuppfer cells and macrophages in the spleen. In conclusion, we were able to design a novel lipid-encapsulated MNP with the ability to carry genetic material, with favorable pharmacokinetic properties, and under the influence of a magnetic field with the capability to mediate transfection in vitro.

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Avanti
DSPE-PEG (2000) 马来酰亚胺, Avanti Research - A Croda Brand 880126P, powder
Avanti
DSPE-PEG (2000) 马来酰亚胺, Avanti Research - A Croda Brand 880126C
Sigma-Aldrich
双十烷基二甲基溴化铵, 98%
Avanti
大豆Lyso PC, Avanti Research - A Croda Brand 840072P, powder