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Current Drug Delivery


ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

5-Fluorouracil Buccal Tablets for Locoregional Chemotherapy of Oral Squamous Cell Carcinoma: Formulation, Drug Release and Histological Effects on Reconstituted Human Oral Epithelium and Porcine Buccal Mucosa

Author(s): Libero Italo Giannola, Viviana De Caro, Giulia Giandalia, Maria Gabriella Siragusa, Carlo Paderni, Giuseppina Campisi and Ada Maria Florena

Volume 7, Issue 2, 2010

Page: [109 - 117] Pages: 9

DOI: 10.2174/156720110791011792

Price: $65


5-Fluorouracil (5-FU) is currently used for treatment of oral squamous cell carcinoma (OSCC). 5-FU is given by i.v. although the systemic administration is associated with severe toxic effects and no topical formulations of 5-FU for buccal drug delivery have been reported. In this study we would report the development of buccal tablets suitable for direct application of low-doses of 5-FU on cancer lesions. The topical administration could be effective on tumor area while systemic undesired side effects are avoided. Preliminarily, the limited tendency of 5-FU to cross the buccal tissue was established using reconstituted human oral epithelium (RHOE, in vitro) and porcine buccal mucosa (ex vivo) as mucosal models. The values of steady-state flux and permeability coefficient suggested the scarce aptitude of 5-FU to reach the systemic circulation. Matrix buccal tablets, were designed for 5-FU local delivery, developed and prepared. Release tests showed a highly reproducible Higuchian drug discharge. After tablet administration on buccal tissue specimens, the occurrence of histomorphological effects of 5-FU was highlighted. Apoptotic events were registered in all samples treated while only negligible amounts of 5-FU permeated the buccal membrane and reached the simulated plasma. The results suggest that loaded matrix tablets containing 5% of 5-FU could be a useful means in topical treatment of OSCC.

Keywords: 5-Fluorouracil, Locoregional drug delivery, Porcine buccal mucosa, Reconstituted human oral epithelium, Oral squamous cell carcinoma, Buccal tablets

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