Volume 89, Issue 2 pp. 260-267
Research Article

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

Hai-Shu Lin

Hai-Shu Lin

Department of Pharmacy, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260

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Sui Yung Chan

Sui Yung Chan

Department of Pharmacy, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260

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Kerwin Siew Yang Low

Kerwin Siew Yang Low

Department of Pharmacology, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260

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Mei Leng Shoon

Mei Leng Shoon

Department of Pharmacology, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260

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Paul C. Ho

Corresponding Author

Paul C. Ho

Department of Pharmacy, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260

Department of Pharmacy, National University of Singapore, 10 Kent Ridge Crescent, Singapore 119260Search for more papers by this author

Abstract

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-β-cyclodextrin (HPβCD). 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 HPβCD-based ATRA after intravenous administration, inclusion of ATRA into HPβCD was found to greatly improve the oral absorption of ATRA. © 2000 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 89: 260–267, 2000

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