Docetaxel epimerization in silicone films: A case of drug excipient incompatibility

Mohsin, S, Arellano, I, Choudhury, N and Garg, S 2014, 'Docetaxel epimerization in silicone films: A case of drug excipient incompatibility', Drug Testing and Analysis, vol. 6, no. 10, pp. 1076-1084.


Document type: Journal Article
Collection: Journal Articles

Title Docetaxel epimerization in silicone films: A case of drug excipient incompatibility
Author(s) Mohsin, S
Arellano, I
Choudhury, N
Garg, S
Year 2014
Journal name Drug Testing and Analysis
Volume number 6
Issue number 10
Start page 1076
End page 1084
Total pages 9
Publisher John Wiley & Sons
Abstract Docetaxel (DTX) is an anti-cancer compound derived from 10-deacetyl baccatin III which is indicated for treatment of breast, lung, prostate, gastro-esophageal, and head and neck cancers. Epimerization of DTX at the C-7 hydroxyl position has intrigued chemists and has been implicated in loss of potency, as well as in the development of resistance in tumour cells. For localized controlled delivery of this agent, silicone films were prepared from a commercially available silicone kit. High levels of epimeric degradants were unexpectedly found in the in vitro release media. Herein, we discuss this anomalous DTX degradation to epimeric impurities, and discuss the possible reasons for degradation. Systematic stability studies were performed on the release media and the silicone kit components. It was found that release media and tin-based catalyst present in the silicone kit could be responsible for the epimeric conversion. This unusual case of chemical incompatibility can affect product performance and can even lead to development of resistance in tumour cells towards DTX.
Subject Physical Chemistry of Materials
Biomaterials
Composite and Hybrid Materials
Keyword(s) silicone
docetaxel
epimerization
chemical incompatibility
degradation
DOI - identifier 10.1002/dta.1617
Copyright notice Copyright © 2014 John Wiley & Sons, Ltd.
ISSN 1942-7603
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