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KMID : 0369820070370050311
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Jorunal of Korean Pharmaceutical Sciences
2007 Volume.37 No. 5 p.311 ~ p.314
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Buccal Transport of Paclitaxel using Ethanol and Glyceryl Monooleate
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Lee Yoon-Jin
Kang Myung-Joo
Park Young-Mi
Choi Young-Wook
Lee Jae-Hwi
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Abstract
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Paclitaxel (PTX) is an antineoplastic agent approved for the treatment of ovarian and breast carcinomas. However, the use of paclitaxel as an anticancer drug is limited by its extremely poor water solubility (below ). Furthermore, it has very low bioavailability when administered orally because paclitaxel is a substrate of P-glycoprotein (P-gp) efflux pump. In this study, buccal delivery of PTX was investigated as one of the alternatives for PTX delivery. Ethanol and glyceryl monooleate (GMO) were selected as permeation enhancing agents to increase solubility and permeation across buccal mucosa of PTX. At the different concentrations of ethanol solution (), PTX permeation was studied, followed effects of GMO in the concentration range of with ethanol vesicle. The transbuccal ability of PTX was evaluated in vitro using Franz diffusion cells mounted with rabbit buccal mucosa. As a result, incorporation of PTX into ethanol vesicle with GMO significantly enhanced the PTX permeation in rabbit buccal mucosa. Particularly, the mixtures of ethanol:water:GMO at the ratio of 50:47.5:2.5 showed the most excellent enhancing ability. The results showed a promising possibility for buccal delivery of PTX.
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KEYWORD
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Paclitaxel, Buccal delivery system, Glyceryl monooleate, Permeation
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