Kinetic Study of a 2‐Hydroxypropyl‐β‐Cyclodextrin‐Based Formulation of all‐trans‐Retinoic Acid in Sprague‐Dawley Rats After Oral or Intravenous Administration

The Impact of Aqueous Solubility and Dose on the Pharmacokinetic Profiles of Resveratrol

“…The study design and the animal handling protocol of this pharmacokinetic study were modified from several previous studies (21)(22)(23) and approved by the Institutional Animal Care and Use Committee of the National University of Singapore. Adult male Sprague-Dawley rats (250-300 g) were supplied by the Laboratory Animal Center of the National University of Singapore.…”

“…Despite such increase, no statistical differences in pharmacokinetic parameters between sodium resveratrol (Group 4) and HP-β-CD-resveratrol (Group 2) after intravenous administration were found (Table I). These observations are consistent with previous findings with retinoic acids (21,22) and miconazole (26) that HP-β-CD did not exert significant impact on intravenous pharmacokinetic of poorly soluble drugs. After intravenous administration, the major driving force for dissociation of weakly to moderately bound drugs from the cyclodextrin inclusion complex is simple dilution and the drug release is rapid (in fraction of seconds) and quantitative in most cases (27).…”

“…The final clear solution indicated complete dissolution of resveratrol. Such simple preparation method has been used to form intravenous formulations of retinoic acids in pre-clinical studies (21,22). Since RM-β-CD usually has superior solubility and bioavailability enhancing ability, it was used to form a water soluble oral formulation of resveratrol.…”

Pharmacokinetic study of all‐trans‐retinoyl‐β‐d‐glucuronide in Sprague–Dawley rats after single and multiple intravenous administration(s)

“…The standard curves of RAG and ATRA were linear ( r 2 > 0.99) over the calibration ranges (RAG: 0.1–10 μM, ATRA 0.02–0.15 μM). This HPLC assay method was a slight modification of our previously reported methods 19,20…”

Vitamin A enrichment: Caution with encapsulation strategies used for food applications

“…Suspension vs incorporation into 2-hydroxypropyl-β-cyclodextrin Plasma concentration in rats Improved oral bioavailability of ATRA when included into cyclodextrin (33.4% for ATRA-cyclodextrin vs 18.6% for ATRA suspension) (Lin, Chan, Low, Shoon, & Ho, 2000) 13-Cis-retinoic acid (13-cis RA)…”