Skin delivery potency and antitumor activities of temozolomide ester prodrugs

Panassaya Suppasansatorn, Guocheng Wang, Barbara R. Conway, Weidong Wang, Yongfeng Wang

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)42-52
Number of pages11
JournalCancer Letters
Volume244
Issue number1
DOIs
Publication statusPublished - 28 Nov 2006
Externally publishedYes

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temozolomide
Prodrugs
Esters
Skin
Skin Neoplasms
Dimethyl Sulfoxide
Melanoma
Neoplasms
Hydrolysis
Clinical Trials

Cite this

Suppasansatorn, Panassaya ; Wang, Guocheng ; Conway, Barbara R. ; Wang, Weidong ; Wang, Yongfeng. / Skin delivery potency and antitumor activities of temozolomide ester prodrugs. In: Cancer Letters. 2006 ; Vol. 244, No. 1. pp. 42-52.
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Skin delivery potency and antitumor activities of temozolomide ester prodrugs. / Suppasansatorn, Panassaya; Wang, Guocheng; Conway, Barbara R.; Wang, Weidong; Wang, Yongfeng.

In: Cancer Letters, Vol. 244, No. 1, 28.11.2006, p. 42-52.

Research output: Contribution to journalArticle

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T1 - Skin delivery potency and antitumor activities of temozolomide ester prodrugs

AU - Suppasansatorn, Panassaya

AU - Wang, Guocheng

AU - Conway, Barbara R.

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AU - Wang, Yongfeng

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AB - 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.

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