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Molecules 2012, 17(4), 4612-4624; doi:10.3390/molecules17044612

Hydrogel of Ketoconazole and PAMAM Dendrimers: Formulation and Antifungal Activity

1
Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland
2
Department of Microbiological Diagnostics, Faculty of Pharmacy, Medical University of Białystok, Kilińskiego 1, 15-089 Białystok, Poland
*
Author to whom correspondence should be addressed.
Received: 21 February 2012 / Revised: 30 March 2012 / Accepted: 9 April 2012 / Published: 18 April 2012
(This article belongs to the Special Issue Dendrimers - from Synthesis to Applications)
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Abstract

Ketoconazole (KET), an imidazole derivative with well-known antifungal properties, is lipophilic and practically insoluble in water, therefore its clinical use has some practical disadvantages. The aim of the present study was to investigate the influence of PAMAM-NH2 and PAMAM-OH dendrimers generation 2 and generation 3 on the solubility and antifungal activity of KET and to design and evaluate KET hydrogel with PAMAM dendrimers. It was shown that the surface charge of PAMAM dendrimers strongly affects their influence on the improvement of solubility and antifungal activity of KET. The MIC and MFC values obtained by broth dilution method indicate that PAMAM-NH2 dendrimers significantly (up to 16-fold) increased the antifungal activity of KET against Candida strains (e.g., in culture Candida albicans 1103059/11 MIC value was 0.008 μg/mL and 0.064 μg/mL, and MFC was 2 μg/mL and 32 μg/mL for KET in 10 mg/mL solution of PAMAM-NH2 G2 and pure KET, respectively). Antifungal activity of designed KET hydrogel with PAMAM-NH2 dendrimers measured by the plate diffusion method was definitely higher than pure KET hydrogel and than commercial available product. It was shown that the improvement of solubility and in the consequence the higher KET release from hydrogels seems to be a very significant factor affecting antifungal activity of KET in hydrogels containing PAMAM dendrimers.
Keywords: PAMAM dendrimer; ketoconazole; hydrogel; antifungal activity; aqueous solubility PAMAM dendrimer; ketoconazole; hydrogel; antifungal activity; aqueous solubility
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Winnicka, K.; Wroblewska, M.; Wieczorek, P.; Sacha, P.T.; Tryniszewska, E. Hydrogel of Ketoconazole and PAMAM Dendrimers: Formulation and Antifungal Activity. Molecules 2012, 17, 4612-4624.

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