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Oral formulation strategies to improve the bioavailability and mitigate the food effect of abiraterone acetate

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dc.contributor.authorSchultz, H.B.
dc.contributor.authorMeola, T.R.
dc.contributor.authorThomas, N.
dc.contributor.authorPrestidge, C.A.
dc.date.issued2020
dc.description.abstractAbiraterone acetate, marketed as Zytiga®, is an antiandrogen medication used in the treatment of prostate cancer. Abiraterone acetate is a BCS Class IV compound associated with several oral delivery challenges. Its low solubility and high lipophilicity lead to poor oral bioavailability (<10%) and a dramatic positive food effect (5–10-fold). Hence, a large dose of abiraterone acetate (1000 mg per day) is prescribed to patients who must fast for at least 1 h before and 2 h after administration. The recent expiry of Zytiga®s’ patent has led to the emergence of publications describing improved oral formulation strategies for abiraterone acetate. This review aims to discuss the characteristics of abiraterone acetate that lead to its unfavorable oral delivery, examine the oral formulation strategies that have been applied, and to describe potential alternative oral formulation strategies that have been used for other BCS Class IV drugs, to determine the most valuable strategies to develop novel and improved alternatives to the current commercial product. Specific emphasis of this review is placed on enabling oral formulation strategies that can improve solubilization and bioavailability, reduce the clinical dose and remove the pharmaceutical food effect to ultimately provide prostate cancer patients with a more efficient formulation with greater patient compliance.
dc.identifier.citationInternational Journal of Pharmaceutics, 2020; 577(119069):1-12
dc.identifier.doi10.1016/j.ijpharm.2020.119069
dc.identifier.issn0378-5173
dc.identifier.issn1873-3476
dc.identifier.orcidMeola, T.R. [0000-0002-7827-6256]
dc.identifier.urihttps://hdl.handle.net/11541.2/141921
dc.language.isoen
dc.publisherElsevier BV
dc.relation.fundingAustralian Government
dc.rightsCopyright 2020 Elsevier B.V. Access Condition Notes: Accepted manuscript available on open access
dc.source.urihttps://doi.org/10.1016/j.ijpharm.2020.119069
dc.subjectabiraterone acetate
dc.subjectpoorly water-soluble drug
dc.subjectoral delivery
dc.subjectbioavailability
dc.subjectfood effect
dc.subjectprostate cancer
dc.titleOral formulation strategies to improve the bioavailability and mitigate the food effect of abiraterone acetate
dc.typeJournal article
pubs.publication-statusPublished
ror.fileinfo12249118320001831 13249118310001831 Open Access Postprint
ror.mmsid9916370008501831

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