Skin delivery potency and antitumor activities of temozolomide ester prodrugs

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

doi:10.1016/j.canlet.2005.11.029

Skin delivery potency and antitumor activities of temozolomide ester prodrugs

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

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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. © 2005 Elsevier Ireland Ltd. All rights reserved.

Original language	English
Pages (from-to)	42-52
Number of pages	11
Journal	Cancer Letters
Volume	244
Issue number	1
DOIs	https://doi.org/10.1016/j.canlet.2005.11.029
Publication status	Published - 28 Nov 2006

Keywords

cytotoxicity
prodrugs
skin delivery
temozolomide
temozolomide acid
temozolomide esters

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10.1016/j.canlet.2005.11.029

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title = "Skin delivery potency and antitumor activities of temozolomide ester prodrugs",

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. {\textcopyright} 2005 Elsevier Ireland Ltd. All rights reserved.",

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author = "Panassaya Suppasansatorn and Guocheng Wang and Conway, {Barbara R.} and Weidong Wang and Yongfeng Wang",

year = "2006",

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TY - JOUR

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

AU - Suppasansatorn, Panassaya

AU - Wang, Guocheng

AU - Conway, Barbara R.

AU - Wang, Weidong

AU - Wang, Yongfeng

PY - 2006/11/28

Y1 - 2006/11/28

N2 - 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.

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. © 2005 Elsevier Ireland Ltd. All rights reserved.

KW - cytotoxicity

KW - prodrugs

KW - skin delivery

KW - temozolomide

KW - temozolomide acid

KW - temozolomide esters

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UR - https://www.sciencedirect.com/science/article/pii/S030438350501030X?via%3Dihub

U2 - 10.1016/j.canlet.2005.11.029

DO - 10.1016/j.canlet.2005.11.029

M3 - Article

C2 - 16412562

SN - 0304-3835

VL - 244

SP - 42

EP - 52

JO - Cancer Letters

JF - Cancer Letters

IS - 1

ER -

Skin delivery potency and antitumor activities of temozolomide ester prodrugs

Abstract

Keywords

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