Formulation and Investigation of a Lipid Based Delivery System Containing Antimicrobials for the Treatment of Periodontal Disease

Curr Drug Deliv. 2018;15(6):887-897. doi: 10.2174/1567201815666180116092354.

Abstract

Background: Periodontitis is a chronic inflammatory disease, which affects the supporting tissues of the teeth, and without proper treatment it may lead to tooth loss. Antibiotics - administered orally - have been widely used in the treatment of periodontitis. With the conventional administration routes, adequate drug levels cannot be reached in the periodontal pockets and oral application of antimicrobials could lead to side effects. Drug delivery systems containing antibiotics, administered at the site of infection, could possibly help eliminate pathogen bacteria and treat periodontitis.

Objective: The aim of the recent study was to create a locally swellable, biodegradable, biocompatible, mucoadhesive, lipophilic drug delivery system containing antimicrobial drugs which softens at body temperature, accommodate to the shape of the periodontal pocket and can provide extended drug release for at least one week.

Methods: During the formulation, thermoanalytical, consistency, wettability, swelling, degradation and drug release studies were applied to determine the ideal ratios of lipid bases, structure-building components and surface active agent concentrations.

Results and discussion: The structure-building component cetostearyl alcohol appeared to be the most convenient, thanks to its wettability and mechanical properties, which led to controlled drug release. With the use of ideal concentrations of components (10% surfactant, 40% structure-building component, 32 % lipid base, 15% antimicrobial agent and 3% polymer), sustained drug release can be provided up to nearly 3 weeks.

Keywords: Lipid drug delivery; antimicrobial therapy; degradation; periodontal pocket; periodontitis; sustained drug release; swelling..

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Calorimetry, Differential Scanning
  • Drug Compounding*
  • Drug Delivery Systems*
  • Humans
  • Lipids / chemistry*
  • Microbial Sensitivity Tests
  • Periodontal Diseases / drug therapy*
  • Periodontal Diseases / microbiology
  • Streptococcus mutans / drug effects*
  • Wettability

Substances

  • Anti-Bacterial Agents
  • Lipids