Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies

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• 作者：Maria Nieddu ; Giovanna Rassu ; Gianpiero Boatto ; Paolo Bosi ; Paolo Trevisi ; Paolo Giunchedi ; Antonio Carta ; Elisabetta Gavini
• 关键词：Thymol ; Cyclodextrin ; Sealed-heating ; Palatability improvement ; Pharmacokinetic study
• 刊名：Carbohydrate Polymers
• 出版年：15 February, 2014
• 年：2014
• 卷：102
• 期：Complete
• 页码：393-399
• 全文大小：694 K

文摘

Thymol, an effective agent for microbial diseases, has a low aqueous solubility and a strong bitter/irritating taste. These physicochemical characteristics need to be improved to develop pharmaceutical preparations. This study evaluates whether 尾-cyclodextrin and a copolymer based on dimethylaminoethyl methacrylate (DMAEMA) interact with thymol in order to control powderization, solubilization, and taste-masking properties. The thymol-尾-cyclodextrin complex was prepared by co-precipitation and sealed-heating methods. The DMAEMA copolymer was mixed with the complex using a new approach, instead of spray coating, to decrease thymol volatility. In vivo studies were performed. Sealed-heating is a suitable method for including thymol in 尾-cyclodextrin with a good loading efficiency; thymol volatility control is achieved by mixing the complex with the DMAEMA copolymer. 尾-Cyclodextrin accelerates the in vivo thymol absorption rate compared with the free drug; the thymol half-life is still long. Therefore, a low number of administrations per day are required. Although bioavailability is unchanged with respect to free thymol, high doses could be administered of a selected formulation without compromising the compliance. Furthermore, thymol that is not absorbed is held along the intestine, where it can useful in the treatment and/or prevention of intestinal bacterial diseases.