1. Investigation of pharmacokinetic properties of a PEGylated bilirubin nanoparticle in male Sprague-Dawley rats using liquid chromatography-quadrupole time-of-flight mass spectrometry.
- Author
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Park, Seo-jin, Lim, Jeong-hyeon, Lee, Jiyu, Lee, Jeongmin, Hwang, Sangsoo, Kim, Hyunjin, Jo, Seunghyun, Shin, Duckhyang, MA, Sang Ho, Kim, Myung L., and Shin, Young G.
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TIME-of-flight mass spectrometry ,SUBCUTANEOUS injections ,POLYETHYLENE glycol ,SPRAGUE Dawley rats ,CARDIOVASCULAR system - Abstract
Polyethylene glycol (PEG) was introduced into synthetic bilirubin 3α and a PEGylated bilirubin 3α nanoparticle (BX-001N, Brixelle®) was developed for the first time. An in vitro microsomal stability study, in vivo PK studies with intravenous bolus (IV) and subcutaneous injection (SC), and a semi-mass balance study of BX-001N were investigated to evaluate its pharmacokinetic (PK) properties in male Sprague-Dawley (SD) rats using developed liquid chromatography-quadrupole time-of-flight mass spectrometry (LC-qTOF/MS). Following IV administration at 10 or 30 mg/kg, BX-001N showed very low clearance (0.33–0.67 mL/min/kg) with predominant distribution in the vascular system (Vd = 51.73–83.02 mL/kg). BX-001N was also very stable in vitro liver microsomal stability study. Following SC administration at 10 or 30 mg/kg, the bioavailability of BX-001N in plasma at 10 mg/kg was around 43% and showed the less dose-proportionality at 30 mg/kg dose. BX-001N was mainly excreted via the urinary pathway (86.59–92.99% of total amount of parent drug in excreta; urine and faeces) not via the biliary one. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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