Kinetic study of a 2-hydroxypropyl-beta-cyclodextrin-based formulation of all-trans-retinoic acid in Sprague-Dawley rats after oral or intravenous administration

all-trans-Retinoic acid (ATRA, vitamin A acid, or tretinoin) is a potent ch emotherapeutic agent far the treatment of acute promyelocytic leukemia (APL ). Its poor aqueous solubility not only affects its oral absorption but als o prevents it from forming an aqueous parenteral formulation. Recently, we developed a water-soluble formulation of ATRA with 2-hydroxypropyl-beta-cyc lodextrin (HP beta CD). In present study, this formulation was tested in Sp rague-Dawley rats. Kinetic study of ATRA was carried out after oral or intr avenous administration. Though there were no statistical differences in any of the estimated pharmacokinetic parameters between ATRA sodium salt and H P beta CD-based ATRA after intravenous administration, inclusion of ATRA in to HP beta CD was found to greatly improve the oral absorption of ATRA. (C) 2000 Wiley-Liss, Inc. and the American Pharmaceutical Association.