Pharmacokinetics of BMEDA after Intravenous Administration in Beagle Dogs

Abstract

The pharmacokinetics of N,N-bis(2-mercapatoethly)-N',N'-diethylenediamineRe-BMEDA-liposomes, was studied. In this work, beagles received a single injection of BMEDA, at doses of 1, 2, or 5 mg/kg; the concentration of BMEDA in the beagles' plasma was then analyzed and determined by liquid chromatography-mass spectrometry/mass spectrometry. Based on the pharmacokinetic parameters of BMEDA, we found that male and female animals shared similar patterns indicating that the pharmacokinetics of BMEDA is independent of gender differences. In addition, the pharmacokinetics of BMEDA was seen to be non-linear because the increase of mean AUC 0-t and AUC 0-∞ values tend to be greater than dose proportional while the mean Vss and CL values of BMEDA appeared to be dose dependent. The information on the pharmacokinetics of BMEDA generated from this study will serve as a basis to design appropriate pharmacology and toxicology studies for future human use.

Evaluation of 188Re-labeled PEGylated nanoliposome as a radionuclide therapeutic agent in an orthotopic glioma-bearing rat model

“…Most recently, a new drug under investigation, 188 Re-labeled PEGylated nanoliposome ( 188 Re-liposome) has been successfully validated with a series of translational studies for treatment of colon cancer. [15][16][17][18][19][20] Currently, it has also been approved by Department of Health, Taiwan for further human clinical trial for treatment of metastatic colon cancer (Phase I). According to our previous work, 188 Re-liposome had been explored in orthotopic glioma-bearing rat model for diagnostic evaluation where systemic administration was employed for delivering the radiolabeled liposome nanoparticles.…”