Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.ijpharm.2007.03.050
DC FieldValue
dc.titleBiopharmaceutics of 13-cis-retinoic acid (isotretinoin) formulated with modified β-cyclodextrins
dc.contributor.authorLin, H.-S.
dc.contributor.authorLeong, W.W.Y.
dc.contributor.authorYang, J.A.
dc.contributor.authorLee, P.
dc.contributor.authorChan, S.Y.
dc.contributor.authorHo, P.C.
dc.date.accessioned2014-10-29T01:49:25Z
dc.date.available2014-10-29T01:49:25Z
dc.date.issued2007-08-16
dc.identifier.citationLin, 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
dc.identifier.issn03785173
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/105704
dc.description.abstract13-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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.ijpharm.2007.03.050
dc.sourceScopus
dc.subject13-cis-Retinoic acid
dc.subjectIsotretinoin
dc.subjectModified β-cyclodextrin
dc.subjectPharmacokinetics
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.description.doi10.1016/j.ijpharm.2007.03.050
dc.description.sourcetitleInternational Journal of Pharmaceutics
dc.description.volume341
dc.description.issue1-2
dc.description.page238-245
dc.description.codenIJPHD
dc.identifier.isiut000249138300028
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