ABSTRACT
Purpose
To develop tooth-binding micelle formulations of triclosan for the prevention and treatment of dental caries.
Methods
Alendronate (ALN) was conjugated to the chain termini of different Pluronic copolymers to confer tooth-binding ability to the micelles. Using 3 different formulation methods, Pluronics and ALN-modified Pluronics were used to prepare triclosan-loaded tooth-binding micelles. The formulation parameters were optimized for triclosan solubility, particle size, hydroxyapatite (HA) binding capability and in vitro drug release profile. The optimized formulation was tested on an in vitro biofilm model.
Results
Direct dissolution was selected as the best formulation method. Triclosan-loaded tooth-binding micelles were able to inhibit initial biofilm growth of Streptococcus mutans UA159 by 6-log CFU/HA disc compared to the untreated control. These tooth-binding micelles were also able to reduce the viability of preformed biofilm by 4-log CFU/HA disc compared to the untreated control.
Conclusions
Triclosan-loaded tooth-binding micelle formulations have been successfully developed and optimized in this study. These micelle formulations demonstrated promising anti-cariogenic bacteria capabilities and may find applications in the prevention and treatment of dental caries.
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ACKNOWLEDGMENT
This work was supported in part by NIH grants R03 DE019179 (KCR), R01 AI038901 (KWB) and R01 AR053325 (DW). We also acknowledge partial support of NIH COBRE grant RR021937 (Nebraska Center for Nanomedicine).
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Chen, F., Rice, K.C., Liu, XM. et al. Triclosan-Loaded Tooth-Binding Micelles for Prevention and Treatment of Dental Biofilm. Pharm Res 27, 2356–2364 (2010). https://doi.org/10.1007/s11095-010-0119-5
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DOI: https://doi.org/10.1007/s11095-010-0119-5