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Development of a Novel Lipophilic, Magnetic Nanoparticle for in Vivo Drug Delivery
Section of Neurobiology, Biomedicine, Department of Health Science and Technology, Aalborg University, Fr. Bajers Vej 3B, 1.216, DK-9220 Aalborg East, Denmark
* Author to whom correspondence should be addressed.
Received: 25 February 2013; in revised form: 2 April 2013 / Accepted: 12 April 2013 / Published: 23 April 2013
Abstract: 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.
Keywords: blood-brain barrier; endothelium; magnetofection; magnetic field; nanoparticle; transfection
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Linemann, T.; Thomsen, L.B.; Jardin, K.G.; Laursen, J.C.; Jensen, J.B.; Lichota, J.; Moos, T. Development of a Novel Lipophilic, Magnetic Nanoparticle for in Vivo Drug Delivery. Pharmaceutics 2013, 5, 246-260.
Linemann T, Thomsen LB, Jardin KG, Laursen JC, Jensen JB, Lichota J, Moos T. Development of a Novel Lipophilic, Magnetic Nanoparticle for in Vivo Drug Delivery. Pharmaceutics. 2013; 5(2):246-260.
Linemann, Thomas; Thomsen, Louiza B.; Jardin, Kristian G.; Laursen, Jens C.; Jensen, Jesper B.; Lichota, Jacek; Moos, Torben. 2013. "Development of a Novel Lipophilic, Magnetic Nanoparticle for in Vivo Drug Delivery." Pharmaceutics 5, no. 2: 246-260.