FORMULATION AND EVALUATION OF QUERCETIN LOADED CHITOSAN-HYDROXY-APATITE BIO COMPOSITE MICROSPHERES FOR PERIODONTITIS

Periodontitis is a group of inflammatory pathological conditions involving periodontal ligaments and supporting alveolar bone which may result in the degeneration of supporting structures of teeth ultimately leading to tooth loss. Present research work is focused on the formulation, optimization and evaluation of chitosan microspheres and chitosan- hydroxyapatite biocomposite microspheres to have controlled release of herbal drug quercetin, of which anti-microbial, anti-inflammatory and wound healing properties are well proven. Mucoadhesive chitosan would retain the drug-loaded microspheres at the affected site and hydroxyapatite used in its combination would improve mechanical strength, osteoconductivity and sustain the release of the drug. Microspheres were formulated by solvent-free precipitation technique using the alkaline solution (NaOH solution). These microspheres were optimized using 3² factorial design using design expert software. Optimized chitosan microspheres (QC5) and chitosan-hydroxyapatite microspheres (QCH5) were characterized for surface morphology by SEM and were found to be spherical with a particle size of 5.56 µm and 7.22 µm and entrapment efficiency of 80.74 and 82.97% respectively. The entrapment of drug in microspheres was also confirmed by DSC studies. Change in the zeta potential of QC5 and QCH5 indicated an interaction between chitosan and hydroxyapatite. Antimicrobial activity of microspheres against Gram-positive S. aureus and Gram-negative E. coli was proved. Developed biocomposite microspheres showed mucoadhesion on porcine buccal mucosa using in-vitro wash off test. The introduction of hydroxyapatite sustained the release of drug up to 6 days in contrast to drug release from QC microspheres in 24 h. These results demonstrate that these stable, biocompatible biocomposite microspheres can be successfully utilized for treating periodontitis.