Preclinical Pharmacokinetics and Biodistribution Studies Using HPLC-MS/MS Testing

HPLC-MS/MS is a robust technique that is highly sensitive and does not incorporate the use of radiation or radioactive material to characterize drug pharmacokinetics. Preclinical studies play a vital role in the evaluation of new drug discovery. Therefore, the assessment needs to be accurate to avoid failure in clinical use.

 Pharmacokinetics is the branch of science that describes how does the body react when the living body consumes a drug. It refers to the absorption capability, movement, metabolism, distribution, and excretion process of the targeted drug. The main aim of preclinical pharmacokinetic drug investigation is to recognize the activity of drugs on the targeted components, for example, plasma or blood. An estimated safe dosage form can be justified by using HPLC-MS analysis.

 The in-vivo tests are performed in a few selected species to track the compound of interest (drug). The study of drug movement in the body is called biodistribution studies. Pharmacokinetics and biodistribution studies are two critical elements of the drug discovery system, and their role in the uptake and identification of the target site of action eliminates off-site toxicities. Hence HPLC testing and MS analysis act as quantitative approaches in the development of a new drug candidate.

 HPLC-MS Method in Pharmacokinetics and Biodistribution Studies

 High-Performance Liquid Chromatography is one of the most efficient modes of chromatography and the most used analytical techniques. Mass Spectrometry is the tool that analyzes the molecular mass of the sample extracted from the HPLC assay. Hence, the combination of LC-MS analysis renders a rapid response towards changing clinical methods. The sample for loading in the HPLC column is prepared either by protein participation or by solid-phase extraction.

 In the preclinical analysis of drug development, the sample is loaded on the mobile phase, and a high-pressure pump forces the sample through the column in the stationary phase. The extracted sample is then analyzed using a mass spectrometer.

 In the pharmacokinetic study of drug development, the dosage of the sample compounds starts from a small quantity and slowly escalates to higher doses. It is because if at the highest dose, there are no side effects, the drug can be adapted.

 Current development of HPLC-MS Testing

 LC-MS/MS analysis is a rapid and most often used technique in the drug development process. Improvements and updates in the LC-MS analysis provide high-resolution results and also help with better qualitative and quantitative analysis of the sample under study. These applications support a widespread aspect of the HPLC testing in the LS-MS lab.

 The tools of LC-MS analysis are increasingly used in the various stages of drug development. The steps include- evaluation, metabolism, product structure, in-vivo/in-vitro studies, identification of unwanted material and removal from the sample, and degradation of these samples.

 LC-MS testing is also employed in the identification of chemical degradants that are used during sample preparation and even predict standard models for the analysis of impurities in the sample compound. Overall the combination of both methods provides high-output and aid boost the drug discovery procedure when compared with old traditional techniques.