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Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels

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Abstract

The objectives of present research were to develop and characterize thermosensitive and mucoadhesive polymer-based sustained release moxifloxacin in situ gels for the treatment of periodontal diseases. Poloxamer- and chitosan-based in situ gels are in liquid form at room temperature and transform into gel once administered into periodontal pocket due to raise in temperature to 37 °C. Besides solution-to-gel characteristic of polymers, their mucoadhesive nature aids the gel to adhere to mucosa in periodontal pocket for prolonged time and releases the drug in sustained manner. These formulations were prepared using cold method and evaluated for pH, solution-gel temperature, syringeability and viscosity. In vitro drug release studies were conducted using dialysis membrane at 37 °C and 50 rpm. Antimicrobial studies carried out against Aggregatibacter actinomycetemcomitans (A.A.) and Streptococcus mutans (S. Mutans) using agar cup-plate method. The prepared formulations were clear and pH was at 7.01–7.40. The viscosity of formulations was found to be satisfactory. Among the all, formulations comprising of 21% poloxamer 407 and 2% poloxamer 188 (P5) and in combination with 0.5% HPMC (P6) as well as 2% chitosan and 70% β-glycerophosphate (C6) demonstrated an ideal gelation temperature (33–37 °C) and sustained the drug release for 8 h. Formulations P6 and C6 showed promising antimicrobial efficacy with zone of inhibition of 27 mm for A.A. and 55 mm for S. Mutans. The developed sustained release in situ gel formulations could enhance patient’s compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis.

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Acknowledgements

The authors would like to thank International Medical University (IMU), Kuala Lumpur, Malaysia for providing the research grant (BDS I1-12(01)2015) and laboratory facilities to carry out this research work.

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Authors and Affiliations

  1. School of Pharmacy, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia

    Ravi Sheshala & Venkata Srikanth Meka

  2. Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi MARA Selangor, Puncak Alam Campus, 42300, Puncak Alam, Kuala Selangor, Malaysia

    Ravi Sheshala

  3. School of Dentistry, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia

    Soo Ying Quah, Giok Choo Tan & Naveen Jnanendrappa

  4. School of Medicine, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia

    Priyadarshi Soumyaranjan Sahu

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  1. Ravi Sheshala
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Correspondence to Ravi Sheshala.

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Sheshala, R., Quah, S.Y., Tan, G.C. et al. Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels. Drug Deliv. and Transl. Res. 9, 434–443 (2019). https://doi.org/10.1007/s13346-018-0488-6

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  • DOI: https://doi.org/10.1007/s13346-018-0488-6

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