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

Nieddu, Maria and Rassu, Giovanna and Boatto, Gianpiero and Bosi, Paolo and Trevisi, Paolo and Giunchedi, Paolo and Carta, Antonio and Gavini, Elisabetta (2014) Improvement of thymol properties by complexation with cyclodextrins: in vitro and in vivo studies. Carbohydrate Polymers, Vol. 102 , p. 393-399. ISSN 0144-8617. eISSN 1879-1344. Article.

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DOI: 10.1016/j.carbpol.2013.10.084

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 β-cyclodextrin and a copolymer based on dimethylaminoethyl methacrylate (DMAEMA) interact with thymol in order to control powderization, solubilization, and taste-masking properties. The thymol–β-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 β-cyclodextrin with a good loading efficiency; thymol volatility control is achieved by mixing the complex with the DMAEMA copolymer. β-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.

Item Type:Article
ID Code:9859
Status:Published
Refereed:Yes
Uncontrolled Keywords:Thymol, cyclodextrin, sealed-heating, palatability improvement, pharmacokinetic study
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier
ISSN:0144-8617
eISSN:1879-1344
Deposited On:09 Jun 2014 12:44

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