Oral Mucoadhesive Buccal Film of Ciprofloxacin for Periodontitis: Preparation and Characterization

Wan Wu,Wei Chen,Qiong Jin

doi:10.4314/tjpr.v15i3.3

Abstract

Purpose: To prepare and characterise ciprofloxacin mucoadhesive buccal films for localised, improved drug delivery in periodontitis. Methods: Ciprofloxacin-loaded buccal films containing 50 mg ciprofloxacin were prepared mucoadhesive polymers sodium cellulose (SCMC) and sodium alginate, using a solvent evaporation method. The films were evaluated in terms of thickness, weight, folding endurance, surface pH, drug content, swelling, mucoadhesive properties, release characteristics, and in vivo anti-periodontitis activity, using ampicillin as the standard. Results: The buccal films showed good drug loading (94.50 ± 0.04 to 99.69 ± 0.21 %) and significant mucoadhesion in terms of in vitro residence time, as well as significant swelling (38.20 ± 1.62 to 54.42 ± 2.32 %). In addition to the good physicochemical properties of the films, ex vivo drug release was high (83.22 ± 1.42 to 90.24 ± 2.01 after 12 h. The films displayed potent anti-periodontitis activity, as indicated by a significant reduction in the bacterial count in a periodontitis model. The samples treated with BFC4 formulation (containing 3:1 SCMC and sodium alginate) exhibited the lowest growth of colonies (57 ± 2.02 CFU/mL) compared with those treated with the BFC3 formulation (69 ± 2.41 CFU/mL) and the standard (80 ± 5.22 CFU/mL). Conclusion: Formulation BFC4 has suitable physicochemical, drug release, and anti-periodontitis activity for buccal administration. Keywords: Periodontitis, Ciprofloxacin, Buccal film, Mucoadhesive, Periodontitis, Sodium carboxymethyl cellulose, Sodium alginate

Highlights

Drug delivery via an oral route is preferred for the treatment of a variety of local and systemic diseases
We evaluated the weight (a 2 × 2 cm piece using a digital balance), thickness, surface pH, swelling percentage, folding endurance, and drug content (a film was dissolved in 100 mL methanol, stirred for 4 h, and quantified at 272 nm in a ultraviolet (UV) spectrophotometer) (n=3) [13,14]
The films were evaluated in terms of their thickness, weight, folding endurance, surface pH, drug content, swelling, mucoadhesive properties, release characteristics and in vivo antiperiodontitis activity

Summary

INTRODUCTION

Drug delivery via an oral route is preferred for the treatment of a variety of local and systemic diseases. Ciprofloxacin hydrochloride is a secondgeneration fluoroquinolone is an antibiotic that is against a wide range of Gram-negative and Gpositive facultative bacteria, including periodontal pathogens. It has a biological half-life of 3~4 h, requiring frequent dosing [10,11,12]. Ciprofloxacin mucoadhesive buccal films were formulated using sodium carboxymethyl cellulose (SCMC) and sodium alginate polymers. In microspheres, these mucoadhesive polymers prolong the residence time of the dosage form in the gastrointestinal tract and are more suitable as matrix material for oral controlled release

Evaluation of the physicochemical properties

RESULTS

DISCUSSION

CONCLUSION