✦ LIBER ✦

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

✍ Scribed by Hai-Shu Lin; Sui Yung Chan; Kerwin Siew Yang Low; Mei Leng Shoon; Paul C. Ho

Publisher: John Wiley and Sons
Year: 2000
Tongue: English
Weight: 191 KB
Volume: 89
Category: Article
ISSN: 0022-3549
DOI: 10.1002/(sici)1520-6017(200002)89:2<260::aid-jps13>3.0.co;2-q

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✦ Synopsis

all-trans-Retinoic acid (ATRA, vitamin A acid, or tretinoin) is a potent chemotherapeutic agent for the treatment of acute promyelocytic leukemia (APL). Its poor aqueous solubility not only affects its oral absorption but also prevents it from forming an aqueous parenteral formulation. Recently, we developed a water-soluble formulation of ATRA with 2-hydroxypropyl-␤-cyclodextrin (HP␤CD). In present study, this formulation was tested in Sprague-Dawley rats. Kinetic study of ATRA was carried out after oral or intravenous administration. Though there were no statistical differences in any of the estimated pharmacokinetic parameters between ATRA sodium salt and HP␤CD-based ATRA after intravenous administration, inclusion of ATRA into HP␤CD was found to greatly improve the oral absorption of ATRA.