Jenkem Technology Co., Ltd.

Methoxy-polyethylene glycol amine (mPEG-NH₂), an important pharmaceutical excipient, has been extensively utilized in the field of biomedicine. To advance the development of mPEG-NH₂-related drug delivery systems, it is crucial to understand the safety profile and cellular pharmacokinetic behavior of mPEG-NH₂ polymers. In this study, a straightforward analytical assay based on ultra-high performance liquid chromatography and tandem mass spectrometry (UHPLC-MS/MS) for quantifying mPEG₅-NH₂ in biological matrices was established and validated. Multiple reaction monitoring (MRM) transitions were selected for quantification of mPEG₅-NH₂ (mass-to-charge ratio, m/z 252.1 → 87.7) and octaethylene glycol (OH-PEG₈-OH) (mass-to-charge ratio, m/z 371.2 → 89.2). The UHPLC-MS/MS assay demonstrated excellent linearity within the concentration range of 0.01-10 μg/mL, with an R² value of 0.9996. Both intra-day and inter-day accuracies and precisions of the analytical method were within ± 9.19 %. This analytical assay was successfully applied to study the in vitro cellular toxicity and uptake behavior of mPEG₅-NH₂ in MCF-7 cells. The results indicate that high doses of mPEG₅-NH₂ may have potential toxicity to MCF-7 cells.

As a synthetic polymer, methoxy-polyethylene glycol propionic acid (M-PEG-PA) is widely used in the biomedicine field. Unraveling the pharmacokinetic behavior of M-PEG₆-PA in vivo is crucial for evaluating the safety and efficiency of M-PEG-PA-related polymers or drug delivery systems. A high-throughput and green ultra-performance convergence chromatography-tandem mass spectrometry (UPC²-MS/MS) assay was firstly developed and validated for the determination of M-PEG₆-PA polymers in a biological matrix. The MRM transition (mass to charge ratio, precursor ions→fragment ions) of m/z 367.2→118.9 was used to quantify M-PEG₆-PA in this study. The throughput of the assay is high and the total running time for each sample was only 2 min. The linear range of the developed UPC²-MS/MS assay for quantification of M-PEG₆-PA in a biological matrix is 0.05 to 30 μg/mL (R≥0.995). Intra-day and inter-day precisions for the determination of M-PEG₆-PA by this analytical assay were <6.99%. The absolute recoveries and matrix effects of M-PEG₆-PA ranged from 79.50 to 92.47% and 68.72 to 81.73%, respectively. The UPC²-MS/MS assay was successfully applied to quantify the concentrations of M-PEG₆-PA polymers in rat plasma samples.

As an important chemical reagent, methoxy polyethylene glycol amine (mPEG-NH₂) is widely used in biomedical field. Unraveling the pharmacokinetic behavior of mPEG-NH₂ polymers is essential for revealing the toxicity and efficiency of mPEG-NH₂ related drug delivery systems. In this study, a simple analytical assay based on mass spectrometry (MS) was first established and validated for quantification of mPEG₅-NH₂ in biological matrix. The multiple reaction monitoring (MRM) transitions at m/z 252.2 (precursor ions) → 87.7 (fragment ions) and m/z 371.2 (precursor ions) → 89.2 (fragment ions) were chosen to determine mPEG₅-NH₂ and OH-PEG₈-OH, respectively. The UHPLC-MS/MS assay showed excellent linearity over the range of 0.01-10 μg/mL. Intra-day and inter-day accuracies and precisions of the assay were all within ± 6.44 %. The analytical assay was successfully applied to reveal the in vivo pharmacokinetic behavior of mPEG₅-NH₂ in rats.