Please use this identifier to cite or link to this item:
|Title:||Biopharmaceutics of 13-cis-retinoic acid (isotretinoin) formulated with modified β-cyclodextrins||Authors:||Lin, H.-S.
|Issue Date:||16-Aug-2007||Citation:||Lin, H.-S., Leong, W.W.Y., Yang, J.A., Lee, P., Chan, S.Y., Ho, P.C. (2007-08-16). Biopharmaceutics of 13-cis-retinoic acid (isotretinoin) formulated with modified β-cyclodextrins. International Journal of Pharmaceutics 341 (1-2) : 238-245. ScholarBank@NUS Repository. https://doi.org/10.1016/j.ijpharm.2007.03.050||Abstract:||13-cis-Retinoic acid (13-cis-RA), also known as isotretinoin, is commonly used in the management of severe acne. Its clinical efficacy in oncology has also been documented. As a vitamin A derivative, it is not soluble in water. This solubility barrier not only affects its oral absorption but also makes parenteral delivery difficult. Recently, water-soluble formulations of 13-cis-RA have been attempted with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and randomly methylated-β-cyclodextrin (RM-β-CD). In this study, the pharmacokinetic profiles of these two formulations were assessed in Sprague-Dawley rats after single intravenous or oral administration. We found that 13-cis-RA was eliminated from the body through a dose-independent process after intravenous injection of either sodium salt or the HP-β-CD formulation within the tested dosage range (2.0-7.5 mg/kg). Furthermore, HP-β-CD did not alter the kinetic profile of 13-cis-RA after intravenous administration in comparison with 13-cis-RA sodium salt. We also found that RM-β-CD dramatically enhanced the oral absorption of 13-cis-RA. At 10.0 mg/kg, the bioavailability of 13-cis-RA formulated with RM-β-CD was about three-fold higher than that of the control (13-cis-RA suspended in 0.5% carboxymethylcellulose (CMC)). Similarly, the oral absorption of 13-cis-RA was not saturated within our tested range (2.5-10.0 mg/kg) and the bioavailability remained unchanged. These results demonstrated that HP-β-CD and RM-β-CD were suitable excipients for the delivery of 13-cis-RA. © 2007 Elsevier B.V. All rights reserved.||Source Title:||International Journal of Pharmaceutics||URI:||http://scholarbank.nus.edu.sg/handle/10635/105704||ISSN:||03785173||DOI:||10.1016/j.ijpharm.2007.03.050|
|Appears in Collections:||Staff Publications|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Nov 28, 2019
WEB OF SCIENCETM
checked on Nov 28, 2019
checked on Nov 30, 2019
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.