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 p-cyclodextrin and a copolymer based on dimethylaminoethyl methacrylate (DMAEMA) interact with thymol in order to control powderization, solubilization, and taste-masking properties. The thymol-p-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 P-cyclodextrin with a good loading efficiency; thymol volatility control is achieved by mixing the complex with the DMAEMA copolymer. P-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. (C) 2013 Elsevier Ltd. All rights reserved.

Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies / Nieddu, M; Rassu, Giovanna; Boatto, Gianpiero; Bosi, P; Trevisi, P; Giunchedi, Paolo; Carta, Antonio; Gavini, Elisabetta. - In: CARBOHYDRATE POLYMERS. - ISSN 0144-8617. - 102:1(2014), pp. 393-399. [10.1016/j.carbpol.2013.10.084]

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

RASSU, Giovanna;BOATTO, Gianpiero;GIUNCHEDI, Paolo;CARTA, Antonio;GAVINI, Elisabetta
2014-01-01

Abstract

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 p-cyclodextrin and a copolymer based on dimethylaminoethyl methacrylate (DMAEMA) interact with thymol in order to control powderization, solubilization, and taste-masking properties. The thymol-p-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 P-cyclodextrin with a good loading efficiency; thymol volatility control is achieved by mixing the complex with the DMAEMA copolymer. P-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. (C) 2013 Elsevier Ltd. All rights reserved.
2014
Improvement of thymol properties by complexation with cyclodextrins: In vitro and in vivo studies / Nieddu, M; Rassu, Giovanna; Boatto, Gianpiero; Bosi, P; Trevisi, P; Giunchedi, Paolo; Carta, Antonio; Gavini, Elisabetta. - In: CARBOHYDRATE POLYMERS. - ISSN 0144-8617. - 102:1(2014), pp. 393-399. [10.1016/j.carbpol.2013.10.084]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11388/46540
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