<p>Periodontitis is a chronic inflammatory disease leading to progressive destruction of periodontal tissues. This study presents the formulation and evaluation of a Moxifloxacin hydrochloride (MH)-loaded proliposomal gel designed for sustained localized delivery to periodontal sites. MH-loaded proliposomes were fabricated by the film dispersion freeze-drying technique and optimized using a response surface design to achieve high entrapment efficiency and controlled particle size. The entrapment efficiency ranged from 70.1% to 91.4%; batch PL4 showed the highest MH entrapment. The optimized formulation exhibited an average particle size of 215.2&#xa0;nm, a PDI of 0.139, and a zeta potential of − 21.7&#xa0;mV, confirming colloidal stability. Transmission electron microscopy revealed spherical bilayered vesicles. Incorporation of proliposomes into a Carbopol® 934P gel yielded a bioadhesive matrix with optimal viscosity, pH compatibility, and uniform drug distribution. In-vitro studies demonstrated sustained MH release over 12&#xa0;h, following Higuchi kinetics, whereas ex-vivo permeation across porcine buccal mucosa showed an increase in flux compared with the conventional gel. The optimized formulation (PLG8) exhibited significant antibacterial activity against <i>Staphylococcus aureus</i> and <i>Escherichia coli</i>, with no irritation in the HET-CAM assay, confirming its biocompatibility. Stability analysis over six months verified physicochemical integrity under ICH conditions. These findings suggest that the developed proliposomal gel offers a stable, safe, and effective nanocarrier system for localized and sustained delivery of MH in periodontitis management.</p> Graphical Abstract <p></p>

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Moxifloxacin Hydrochloride Loaded Proliposomal Gel: Formulation, Characterization and Therapeutic Evaluation of Periodontitis

  • Rushikesh Vishwas Lavhate,
  • Rakesh Pandit Dhavale,
  • Dnyaneshwar Mahadev Mane,
  • Girija Abhijit Gatade,
  • Prafulla Balkrishna Choudhari,
  • Vishal Hindurao Thorat

摘要

Periodontitis is a chronic inflammatory disease leading to progressive destruction of periodontal tissues. This study presents the formulation and evaluation of a Moxifloxacin hydrochloride (MH)-loaded proliposomal gel designed for sustained localized delivery to periodontal sites. MH-loaded proliposomes were fabricated by the film dispersion freeze-drying technique and optimized using a response surface design to achieve high entrapment efficiency and controlled particle size. The entrapment efficiency ranged from 70.1% to 91.4%; batch PL4 showed the highest MH entrapment. The optimized formulation exhibited an average particle size of 215.2 nm, a PDI of 0.139, and a zeta potential of − 21.7 mV, confirming colloidal stability. Transmission electron microscopy revealed spherical bilayered vesicles. Incorporation of proliposomes into a Carbopol® 934P gel yielded a bioadhesive matrix with optimal viscosity, pH compatibility, and uniform drug distribution. In-vitro studies demonstrated sustained MH release over 12 h, following Higuchi kinetics, whereas ex-vivo permeation across porcine buccal mucosa showed an increase in flux compared with the conventional gel. The optimized formulation (PLG8) exhibited significant antibacterial activity against Staphylococcus aureus and Escherichia coli, with no irritation in the HET-CAM assay, confirming its biocompatibility. Stability analysis over six months verified physicochemical integrity under ICH conditions. These findings suggest that the developed proliposomal gel offers a stable, safe, and effective nanocarrier system for localized and sustained delivery of MH in periodontitis management.

Graphical Abstract