Skin delivery potency and antitumor activities of temozolomide ester prodrugs


Clinical trials have shown temozolomide to be an effective agent for treatment of malignant melanoma. In order to investigate its suitability for delivery via the skin, a series of temozolomide esters was synthesized as prodrugs. In vitro assays demonstrated temozolomide, temozolomide acid and the hexyl ester equi-effective against selected cancer cell lines. The susceptibility of the esters to enzyme hydrolysis and their effectiveness for application to the skin were investigated. The esters effectively diffuse through rat skin and the hexyl ester demonstrated profound potency for penetrating through skin. Topical application of 5% (w/v) hexyl ester in DMSO solution on a mouse model demonstrated a significant inhibition of tumor growth. These results suggest that temozolomide esters could be an effective alternative to temozolomide in the treatment of skin cancer. © 2005 Elsevier Ireland Ltd. All rights reserved.

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Divisions: College of Health & Life Sciences > School of Biosciences
College of Health & Life Sciences > Aston Pharmacy School
Uncontrolled Keywords: cytotoxicity,prodrugs,skin delivery,temozolomide,temozolomide acid,temozolomide esters,Cancer Research,Molecular Biology,Oncology
Publication ISSN: 1872-7980
Last Modified: 23 Oct 2019 09:54
Date Deposited: 20 Apr 2010 09:18
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Related URLs: http://www.scop ... tnerID=8YFLogxK (Scopus URL)
Published Date: 2006-11-28
Authors: Suppasansatorn, Panassaya
Wang, Guocheng
Conway, Barbara R.
Wang, Weidong
Wang, Yongfeng


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