Development of a Novel Lipophilic, Magnetic Nanoparticle for in Vivo Drug Delivery

Pharmaceutics

Thomas Linemann¹  Louiza B. Thomsen¹  Kristian G. Du Jardin¹  Jens C. Laursen¹  Jesper B. Jensen¹  Jacek Lichota¹ 

[1] Section of Neurobiology, Biomedicine, Department of Health Science and Technology, Aalborg University, Fr. Bajers Vej 3B, 1.216, DK-9220 Aalborg East, Denmark;

关键词: blood-brain barrier;    endothelium;    magnetofection;    magnetic field;    nanoparticle;    transfection;   

DOI  :  10.3390/pharmaceutics5020246

来源: mdpi

【 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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.