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Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment

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Abstract

Eudragit RS (ERS), a quaternary polyacrylate positively charged polymer, exhibits a very low permeability and swells in aqueous media independently of pH without dissolving. Owing to its high solubility in N-methyl pyrrolidone (NMP), it was interesting to apply as polymer matrix for solvent-exchanged in situ forming gel. The aim of this research was to prepare in situ forming gels from ERS to deliver the antimicrobial agents (doxycycline hyclate, metronidazole, and benzoyl peroxide) for periodontitis treatment. They were evaluated for viscosity and rheology, gel formation, syringeability, drug release, and antimicrobial activities. The solvent exchange between NMP and an external aqueous simulated gingival crevicular fluid stimulated the dissolved ERS transforming into the opaque rigid gel. Antimicrobial agent loaded ERS systems exhibited Newtonian flow with acceptable syringeability. The higher-loaded ERS promoted the more prolongation of drug release because of the retardation of water diffusion into the precipitated matrix. Antimicrobial activities against Staphylococcus aureus, Escherichia coli, Candida albicans, Streptococcus mutans, and Porphyromonas gingivalis depended on type of drugs and test microorganisms. Doxycycline hyclate loaded ERS systems showed these activities greater than the others; however, all of them could inhibit all test microorganisms. Thus, the solvent exchange-induced in situ forming gels comprising ERS-antimicrobial drugs exhibited potential use as localized delivery systems for periodontitis treatment.

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Acknowledgments

This research work was supported by the Research and Development Institute, Silpakorn University (grant no. SURDI 57/01/42). We would like to thank Juree Charoenteeraboon for her comment and help. This research work was also facilitated by the Faculty of Pharmacy, Silpakorn University, Thailand.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand

    Thawatchai Phaechamud & Takron Jantadee

  2. Pharmaceutical Intelligence Unit Prachote Plengwittaya, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand

    Jongjan Mahadlek

  3. Department of Biopharmacy, Faculty of Pharmacy, Silpakorn University, Nakorn Pathom, 73000, Thailand

    Purin Charoensuksai

  4. Faculty of Pharmaceutical Sciences and Medical Products Innovations from Polymers in Clinical Use Research Unit, Prince of Songkla University, Songkhla, 90112, Thailand

    Wiwat Pichayakorn

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  1. Thawatchai Phaechamud
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Phaechamud, T., Jantadee, T., Mahadlek, J. et al. Characterization of Antimicrobial Agent Loaded Eudragit RS Solvent Exchange-Induced In Situ Forming Gels for Periodontitis Treatment. AAPS PharmSciTech 18, 494–508 (2017). https://doi.org/10.1208/s12249-016-0534-y

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