Enhancing the Accuracy of Plasma Protein Binding Assays
Enhancing the Accuracy of Plasma Protein Binding (PPB) Assays for Challenging Drug Candidates
An Inotiv Case Study Evaluating Sovicell’s TRANSIL Technology
Authors: Johnson, K. M., Chiodini, E., Denny, L., Fekry, M. I., Pennington, C., Akers, S., & Rumsey, J. (n.d.). Utilizing various plasma protein binding tools for determinating the free fraction of lipophilic and lipopeptide drugs. Inotiv, Maryland Heights, MO; Lipscomb University, Nashville, TN.
This case study, conducted by Inotiv and Lipscomb University, evaluates the effectiveness of Sovicell’s TRANSIL partitioning technology in determining the free fraction of lipophilic and lipopeptide drugs in plasma protein binding (PPB) assays. The study compares Sovicell’s PPB (Plasma Protein Binding) Kit and High Sensitivity Binding (HSB) Kit against traditional methods, such as Rapid Equilibrium Dialysis (RED) and Ultrafiltration (UF), to assess their accuracy, efficiency, and applicability in drug discovery and development.
The TRANSIL PPB Kit utilises immobilized human serum albumin (HSA) and alpha-1-acid glycoprotein (AAG) on beads, while the HSB Kit incorporates lipid membranes to simulate competitive binding between plasma proteins and membranes. Both kits eliminate the need for membrane barriers, which are a common source of error in traditional methods.
Overcoming Accuracy Challenges in Plasma Protein Binding Analysis for Lipophilic and Lipopeptide Drugs
The primary goal of this study was to address the challenges associated with accurately determining the free fraction of drug candidates that are highly protein-bound, lipophilic, or unstable in plasma. Traditional methods like RED and UF often struggle with compounds exhibiting high nonspecific binding, low recovery, or atypical physicochemical properties. Inotiv aimed to evaluate whether Sovicell’s TRANSIL technology could provide a more reliable and efficient alternative for these challenging compounds.
The results of this study support the utility of Sovicell’s TRANSIL technology as a robust and efficient alternative to traditional PPB assays. The TRANSIL technology demonstrated high accuracy in determining the free fraction of drug candidates. The technology addresses many of the limitations of RED and UF, particularly for challenging drug candidates that are highly protein-bound, lipophilic, or unstable in plasma. Inotiv’s findings highlight the capability of TRANSIL kits to improve the accuracy and efficiency of PPB assays in drug discovery and development.
Download the full case study to explore the detailed methodologies, results, and insights from Inotiv’s evaluation. Discover how Sovicell’s innovative TRANSIL technology can enhance your PPB assays and streamline your drug development process.
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