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Syringeable atorvastatin loaded eugenol enriched PEGylated cubosomes in-situ gel for the intra-pocket treatment of periodontitis: statistical optimization and clinical assessment

In plain language

Researchers have developed and evaluated a syringeable in-situ gel designed for the intra-pocket treatment of periodontitis. The system delivers atorvastatin using eugenol-enriched PEGylated cubosomes, which were statistically optimised using a Box-Behnken design. The optimised cubosome formulation demonstrated high solubilisation efficiency, a nanoscale particle size, sustained drug release over 12 hours, and physical stability for up to 30 days. When incorporated into the final gel, the formulation gelled at body temperature within 46 seconds and sustained drug release over 72 hours. In clinical evaluations, administration of the gel led to significant improvements in clinical periodontal parameters, including substantial reductions in probing depth, bleeding index, plaque index, and gingival levels of the inflammatory marker transforming growth factor-beta 1, showing its utility in reducing periodontal inflammation.

Key takeaways

  • An optimised cubosome formulation achieved a 97.71 percent solubilisation efficiency and maintained stability for 30 days.
  • The resulting in-situ gel set at 34 degrees Celsius within 46 seconds and released roughly 75 percent of the drug across 72 hours.
  • Clinical testing showed marked reductions in probing depth, bleeding, plaque, and gingival transforming growth factor-beta 1 levels.

Why it matters

Periodontitis is a serious inflammatory gum disease that damages oral tissues. Delivering therapeutics directly into periodontal pockets via a liquid that quickly turns into a gel at body temperature allows sustained local drug release. This approach offers a targeted way to reduce gum inflammation, control bacterial plaque, and enhance clinical healing without relying solely on systemic drug administration.

Commercialisation angle

This formulation offers an applied intra-pocket therapy for dental professionals treating periodontitis. Because the system has been tested clinically and demonstrated significant reductions in disease markers, it represents an applied, clinically evaluated technology. Commercial developers or dental pharmaceutical manufacturers could explore scaling the syringeable formulation for direct clinical use in periodontal treatment programmes.

AI-generated from the published abstract. Always read the original work before citing.

Abstract

Box-Behnken design was used to generate eugenol enriched PEGylated cubosomes. Based on the desirability function, the optimized formulation (OEEPC) was selected exhibiting a solubilization efficiency (SE%) of 97.71 ± 0.49%, particle size (PS) of 135.20 ± 1.11 nm, polydispersity index (PDI) of 0.09 ± 0.006, zeta potential (ZP) of -28.30 ± 1.84 mV and showing a sustained drug release over 12 h. It displayed a cubic structure under the transmission electron microscope, furthermore, it was stable upon storage for up to 30 days. Hence, it was loaded into an optimum syringeable in-situ gel (ISG) which displayed the desired periodontal gelation temperature (34 ± 0.70 °C) and an adequate gelation time (46 ± 2.82 sec), it also released approximately 75% of the drug within 72 h. Clinical evaluation of the ISG showed a promising percentage reduction of about 58.33% in probing depth, 90% in the bleeding index, 81.81% in the plaque index, and 70.21% in gingival levels of transforming growth factor-β1. This proved that the formulated syringeable intra-pocket delivery system of ATV is an efficient candidate for diminishing inflammation in periodontitis.

Research topics

  • Oral microbiology and periodontitis research
  • Advanced Drug Delivery Systems
  • Streptococcal Infections and Treatments

Sustainable Development Goals

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DOI: 10.1080/10717544.2022.2162159

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