Periodontal thermoresponsive, mucoadhesive dual antimicrobial loaded in-situ gel for the treatment of periodontal disease: Preparation, in-vitro characterization and antimicrobial study

Abstract

<div class="section"> <a class="named-anchor" id="d10518236e201"> <!-- named anchor --> </a> <h5 class="section-title" id="d10518236e202">Background</h5> <p id="d10518236e204">This study aimed to formulate and characterize <i>in-situ</i> gel containing levofloxacin and metronidazole to release drugs in controlled manner for treatment of periodontitis. </p> </div><div class="section"> <a class="named-anchor" id="d10518236e209"> <!-- named anchor --> </a> <h5 class="section-title" id="d10518236e210">Material and Methods</h5> <p id="d10518236e212">Medicated <i>in-situ</i> gel with levofloxacin (10% w/v), metronidazole (25% w/v) and vehicle <i>in-situ</i> gel without drugs having poloxamer 407 (20% w/v) and chitosan (0.5%, 1%, 1.5%, 2.0% 2.5% w/v) were prepared and characterized for physicochemical, mechanical properties, stability and <i>in-vitro</i> drug release. Fourier transform infrared spectroscopy and differential scanning calorimetery studies were done. Optimized formulation was evaluated by scanning electron microscope (SEM) and <i>in-vitro</i> antimicrobial activity against 5 bacterial strains. </p> </div><div class="section"> <a class="named-anchor" id="d10518236e226"> <!-- named anchor --> </a> <h5 class="section-title" id="d10518236e227">Results</h5> <p id="d10518236e229">The results revealed that drugs and polymers were compatible to formulate. All formulations were light yellow, clear and syringeable except formulation having 2.5% w/v chitosan. pH was in the range of 6.20 to 6.74. 1.0% w/v and 1.5% w/v chitosan formulations showed gelation temperature 37 ± 0.32 °C and 34 ± 0.21 °C. Further, mucoadhesive strength indicated mucoadhesivity of gel. <i>In-vitro</i> release study of 1.5% w/v chitosan formulation showed initial burst where about 55–60% MZ and 60–70% LVF got released within 6–7 hrs followed by sustained release upto 48 hrs. SEM images of 1.5% w/v chitosan optimized medicated <i>in-situ</i> and vehicle <i>in-situ</i> gel appeared similar indicating homogeneous mixing of polymers with drugs. <i>In-vitro</i> antimicrobial study showed that medicated <i>in-situ</i> gel was more effective than vehicle. </p> </div><div class="section"> <a class="named-anchor" id="d10518236e246"> <!-- named anchor --> </a> <h5 class="section-title" id="d10518236e247">Conclusions</h5> <p id="d10518236e249">In conclusion, optimized 1.5% w/v chitosan <i>in-situ</i> gel was thermoresponsive, mucoadhesive, syringeable, and released drugs in slow and controlled manner with effectiveness against broad range of microbes. </p> </div>