Pharmacokinetics of pterostilbene in Sprague‐Dawley rats: The impacts of aqueous solubility, fasting, dose escalation, and dosing route on bioavailability

Abstract

Aqueous solubility was identified as a barrier to its oral bioavailability while solubilizing PTS with HP-β-CD substantially increased its bioavailability; dose manipulation was a practical strategy to enhance its bioavailability and systemic exposure; and its delivery through oral mucosa was feasible. As PTS possessed superior pharmacokinetics, it is a favorable candidate for further development.

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

“…Future investigations may address issues of optimization of oral bioavailability by considering alternative formulations (Amri et al, 2012), the use of resveratrol derivatives with higher oral availability, such as pterostilbene (e.g. Yeo et al, 2013), and since only relatively little resveratrol appears to find its way to the brain (Liang et al, 2013;Sale et al, 2004), the role of the parent compound relative to its metabolites, also known to be active (cf. Amri et al, 2012 In addition to the pharmacological normalization of the peripubertal stress-induced social deficit, the present study identified alterations in certain prefrontal cortex subregions following resveratrol treatment.…”

Pterostilbene surpassed resveratrol for anti-inflammatory application: Potency consideration and pharmacokinetics perspective

“…The partial methylation also increases its lipophilicity and may subsequently enhance membrane permeability and biological potency. The aforementioned might explain why PTS is usually found to be more potent than RES in various previous reports (Yeo et al, 2013). Moreover, PTS displayed favourable safety profiles in both pre-clinical and clinical studies (Riche et al, 2013;Ruiz et al, 2009).…”

“…Due to its 3,5-dimethoxy structure, PTS is less susceptible to phase II metabolism. Therefore, the pharmacokinetic profiles of PTS were more favourable than RES as it can achieve greater plasma exposure, longer elimination half-life as well as slower clearance (Yeo, Ho, & Lin, 2013). The partial methylation also increases its lipophilicity and may subsequently enhance membrane permeability and biological potency.…”

Topical treatment with pterostilbene, a natural phytoalexin, effectively protects hairless mice against UVB radiation-induced skin damage and carcinogenesis

“…Pter contains two methoxy groups and one hydroxyl group while Resv has three hydroxyl groups, in consequence Pter is less susceptible to conjugation metabolism and, thus, a longer halflife is expected [18,19]. The dimethoxy structure of Pter enhances its lipophilicity thus increasing membrane permeability and improving its bioavailability [11,16,18,20]. Nevertheless, it is uncertain whether the chemical differences between Resv and Pter may represent a fundamental difference in terms of protection against chronic UVBinduced skin carcinogenesis.…”

“…Pterostilbene, has a more favorable pharmacokinetic profile [15][16][17]. Pter contains two methoxy groups and one hydroxyl group while Resv has three hydroxyl groups, in consequence Pter is less susceptible to conjugation metabolism and, thus, a longer halflife is expected [18,19]. The dimethoxy structure of Pter enhances its lipophilicity thus increasing membrane permeability and improving its bioavailability [11,16,18,20].…”