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A new controlled release system of chlorhexidine and chlorhexidine:βcd inclusion compounds based on porous silica

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Abstract

The purpose of this study was to prepare and characterize a controlled release system based on porous silica loaded with chlorhexidine (Cx) and its inclusion compounds in β-cyclodextrin (βcd), and to evaluate its antimicrobial activity. Acetate chlorhexidine (CxA), gluconate chlorhexidine (CxG), βcd:chlorhexidine acetate 2:1 (βcd:CxA) and βcd:chlorhexidine gluconate 2:1 (βcd:CxG) were incorporated into porous silica. Drug loading was characterized by FTIR, powder X-ray diffraction, thermal analysis and BET, and was shown to be in an amorphous state and porous matrix. The kinetics release parameter of the drug was established, which showed that the Cx systems release profile followed zero order release until 400 h and Higuchi model release until 750 h, after the burst effect at the first 8 h. Chlorhexidine therapeutic range was reached near first hour for all systems. The chlorhexidine porous silica system was biologically active against Enterococcus faecalis and Candida albicans in vitro. The systems showed an efficient Cx controlled release modulated by the presence of the β-cyclodextrin and by the porous silica matrices, providing effective antimicrobial activity.

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Acknowledgements

The authors acknowledge the financial support given from the Brazilian agencies CNPq (Pronex and the INCT-Nanobiofarma), and FAPEMIG.

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Authors and Affiliations

  1. Departament of Chemistry, Universidade Federal de Minas Gerais, UFMG, Avenida Antônio Carlos 6627, Belo Horizonte, MG, 31270-901, Brazil

    Eliete Marçal Guimarães Raso, Nelcy Della Santina Mohallem & Ruben Dario Sinisterra

  2. Departament of Restorative Dentistry, Universidade Federal de Minas Gerais, UFMG, Avenida Antônio Carlos 6627, Belo Horizonte, MG, 31270-901, Brazil

    Maria Esperanza Cortes & Karina Imaculada Teixeira

  3. Centro de Desenvolvimento da Tecnologia Nuclear, Avenida Antônio Carlos 6627, Belo Horizonte, MG, 31270-901, Brazil

    Milton Batista Franco

  4. Faculdade de Odontologia da Pontifícia, Universidade Católica de Minas Gerais, Rua Dom José Gaspar 500, Belo Horizonte, MG, 30535-610, Brazil

    Eliete Marçal Guimarães Raso

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  1. Eliete Marçal Guimarães Raso
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  2. Maria Esperanza Cortes
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Correspondence to Ruben Dario Sinisterra.

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Raso, E.M.G., Cortes, M.E., Teixeira, K.I. et al. A new controlled release system of chlorhexidine and chlorhexidine:βcd inclusion compounds based on porous silica. J Incl Phenom Macrocycl Chem 67, 159–168 (2010). https://doi.org/10.1007/s10847-009-9692-9

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  • DOI: https://doi.org/10.1007/s10847-009-9692-9

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