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Optimization of metronidazole SR buccal tablet for gingivitis using genetic algorithm.

Sobia Razzaq1, Muhammad Ali Syed1, Muhammad Irfan2

  • 1Faculty of Pharmacy, The University of Lahore, Lahore, Pakistan.

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|January 17, 2022
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Summary
This summary is machine-generated.

This study developed a sustained-release metronidazole (MTZ) buccal tablet for gingivitis. Optimized formulation F17 showed 96% MTZ release in 8 hours, offering a promising localized drug delivery system.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Polymer Science

Background:

  • Gingivitis requires prolonged local antibiotic concentration for effective treatment.
  • Conventional delivery methods often fail to achieve sustained and localized drug levels.
  • Mucoadhesive buccal tablets offer a potential solution for localized and extended drug release.

Purpose of the Study:

  • To formulate and evaluate mucoadhesive buccal tablets for sustained and localized delivery of metronidazole (MTZ).
  • To investigate the impact of various mucoadhesive polymers on drug release and tablet properties.
  • To optimize the formulation using a genetic algorithm for enhanced therapeutic efficacy.

Main Methods:

  • Formulation of 16 different mucoadhesive buccal tablet blends (F1-F16) using hydroxypropylmethyl cellulose (HPMC), Carbopol 940 (CP), carboxymethylcellulose (CMC), and ethyl cellulose (EC).
  • Direct compression method for tablet manufacturing.
  • Evaluation of physical characteristics (weight variation, friability), mucoadhesive strength, swelling index, and in vitro drug release.
  • Optimization using a genetic algorithm and validation of the predicted formulation (F17).
  • Analysis of drug release kinetics using the Korsmeyer-Peppas model.

Main Results:

  • Tablets exhibited acceptable physical properties within USP limits.
  • Formulation F14 demonstrated maximum mucoadhesive strength (28.47g) and duration (12 hr).
  • Formulations F15 and F16 achieved near-complete in vitro metronidazole release (97-100%) within 8 hours.
  • The optimized formulation (F17) showed excellent physical characteristics and predicted 96% drug release at 8 hours.
  • Metronidazole release kinetics followed non-Fickian diffusion (Korsmeyer-Peppas model).

Conclusions:

  • Mucoadhesive buccal tablets containing a blend of HPMC, CP, CMC, and EC are effective for sustained and localized metronidazole delivery.
  • The optimized formulation (F17) provides a promising approach for managing gingivitis through prolonged drug release in the buccal cavity.
  • This delivery system offers an alternative to conventional treatments, potentially improving patient compliance and therapeutic outcomes.