Characterization, blood profile and biodistribution properties of surface modified PLGA nanoparticles of SN-38

SN-38, the active metabolite of irinotecan, poses a challenge in terms of drug delivery due to its low solubility and labile lactone ring. The aim of this study was to develop a SN-38 nanoparticulate delivery system to evaluate the in vivo blood profile and biodistribution properties of nanoparticles (NPs). Poly lactide-co-glycolide (PLGA) NPs that were covalently bound to polyethylene glycol-folate (PEG-FOL) were prepared, and their in vivo biodistribution in rats was investigated. Either the SN-38 solution or SN-38 NP suspension was administered intravenously into the tail vein at a dose of 2 mg SN-38 eq./kg. As expected, SN-38 NPs showed a higher plasma concentration in vivo when compared with free SN-38 during a 24h period. Compared with the SN-38 solution, both folate targeted and non-targeted NPs exhibited superior drug concentration in body organs such as the liver, spleen, and lung at 1 and 8 h post-administration. (c) 2010 Elsevier B.V. All rights reserved.