Analysis of drug/metabolites/biomarkers (qualitative/ quantitative) in biological matrices such as plasma, serum, whole blood, urine, saliva, tissues, etc., is commonly termed‘bioanalysis’. It is an imperative part of overall drug development process starting with in vitro/in situ testing, pre-clinical studies through to clinical studies. In today’s high-throughput drug discovery industry, bioanalytical laboratories usually operate under pressure to meet the demands and reduce development times (Xu et al., 2007). As the results of the bioanalysis directly affect the clinical decision-making process, bioanalytical processes are part of regulatory filings. Thus to improve and regulate these findings, regulatory agencies worldwide have issued guidelines and procedures to ensure the quality of bioanalytical data (Shah et al., 2000). The last decade has witnessed many technological breakthroughs in analytical methodology and instrumentation. Apart from improved selectivity and sensitivity, modern analytical instrumentation has provided an edge to fast and cost-effective bioanalytical method development and validation. Among these modern analytical techniques, liquid chromatography coupled with mass spectrometry is considered to be the benchmark for quantitative/qualitative bioanalysis, imparting specificity, sensitivity and speed (Saunders et al., 2009). However, this most selective and sensitive analytical technique also suffers from limitations such as matrix effect, compromised selectivity and a fall in sensitivity of the analyte of interest in the processed biological matrix (Smeraglia et al., 2002)