Pharmacokinetics and Bioavailability Enhancement of Baicalin: A Review

Abstract

Baicalin is one of the major bioactive components of Scutellaria radix, a Chinese herb that has been used since ancient times. Baicalin has various pharmacological activities, including antitumor, antimicrobial, and antioxidant, and has wide clinical applications. Baicalin displays a distinct pharmacokinetic profile including gastrointestinal hydrolysis, enterohepatic recycling, carrier-mediated transport, and complicated metabolism. The in vivo disposition of baicalin is affected by combinations of other herbs and baicalin can interact with other co-administered drugs due to competition between metabolic enzymes and protein binding. Furthermore, baicalin exhibits altered pharmacokinetic properties under different pathological conditions. Due to its low bioavailability, emerging novel baicalin preparations including nano/micro-scale baicalin delivery systems show better absorption and higher bioavailability in preclinical studies, and show promise for future clinical applications. Thus, this current review offers a comprehensive report on the pharmacokinetic behavior of baicalin and strategies to improve its bioavailability.

Plant-Based Antidiabetic Nanoformulations: The Emerging Paradigm for Effective Therapy

“…Development of nanoscale formulations of baicalin has emerged as a potential approach to enhance the bioavailability of baicalin in achieving better clinical efficacy [125,230]. Baicalin-entrapped nanoliposome has been reported to be an excellent formulation for the oral delivery exhibiting improved stability, biodistribution and oral bioavailability of baicalin [231].…”

Pharmacokinetics of sodium baicalin following intravenous and intramuscular administration to piglets

“…The pharmacokinetic properties of baicalin have been investigated in mouse (Jin et al, ), rat (Huang, Liu, & Zhang, ; Li et al, ; Xing, Chen, & Zhong, ; Yang, Li, Xin, Wang, & Zhang, ) and rabbit (Wei et al, ) models but not in pigs. After oral administration, baicalin displays a distinct pharmacokinetic profile that includes gastrointestinal hydrolysis (Noh et al, ), enterohepatic recycling (Xing et al, ), carrier‐mediated transport (Kalapos‐Kovács et al, ) as well as a complex metabolism (Huang et al, ; Kang et al, ). The poor solubility of baicalin (160 μg/ml) and low oral bioavailability (2.2% after oral administration to rats) severely limit its clinical efficacy and application (Li et al, ; Xing et al, ).…”

“…oral administration, baicalin displays a distinct pharmacokinetic profile that includes gastrointestinal hydrolysis (Noh et al, 2016), enterohepatic recycling (Xing et al, 2005), carrier-mediated transport (Kalapos-Kovács et al, 2015) as well as a complex metabolism (Huang et al, 2019;Kang et al, 2014). The poor solubility of baicalin (160 μg/ml) and low oral bioavailability (2.2% after oral administration to rats) severely limit its clinical efficacy and application (Li et al, 2013;Xing et al, 2005).…”

Retention mechanism of pH‐peak‐focusing in countercurrent chromatographic separation of baicalin and wogonoside from Scutellaria baicalensis Georgi

“…Baicalin and wogonoside are the main bioactive chemical components in the root of S. baicalensis (Figure 1), and their high content in this herb has been regarded as the main chemical marker for its quality control [9]. Apart from the traditional pharmacological actions of baicalin, including anti‐inflammatory, anti‐infection, anti‐diabetic, anti‐hypertensive, and radical scavenging activities [10], baicalin has also been shown to have activities in the prevention of liver and kidney injury [11], immunoregulation [12], amelioration of polycystic ovary syndrome [13], inhibition of some pathogenic bacteria [14], neuroprotection, and cognitive enhancement [15]. Further and above all, baicalin and baicalein were recently identified as novel inhibitors of the 3CL protease of severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) in vitro [16].…”