FABRICATION AND CHARACTERIZATION OF MINOCYCLINE LOADED CHITOSAN MICROSPHERES BY CENTRAL COMPOSITE DESIGN FOR THE LOCAL DELIVERY IN PERIODONTAL POCKETS

Abstract

This study was aimed to prepare, optimize and characterize cost-effective and mucoadhesive dental minocycline microspheres for the treatment of periodontitis. There is a need and scope for a cost-effective novel formulation of minocycline for periodontitis that can be delivered to the base of the pockets and is biodegradable, bioadhesive, and non-toxic. The Central composite design (CCD) was utilized to study the effects of process variables (5 levels) on the responses including size (R1), drug-entrapment (R2), mucoadhesion (R3), and percent in-vitro drug release (R4). Chitosan-minocycline microspheres were prepared by W/O emulsion technique using glutaraldehyde and sodium tripolyphosphate as different cross-linking agents. Results indicated that the concentration of polymer, drug, cross-linking agent, and cross-linking method significantly affected drug incorporation efficiencies and microsphere characteristics. The minocycline release from the microspheres provided a retarded release up to 8 h and all concentrations were observed to be more than the minimum inhibitory concentration (MIC) required for inhibiting the growth of Staphylococcus aureus. The study concluded that the microspherical system provides advantages over systemic drug administration, including reduction of systemic side effects and dramatic increase in sustained drug concentrations in the gingival cervicular fluid. Local delivery by means of microspheres has several advantages over systemic drug intake including lesser systemic side effects, reduction of dose, mucoadhesiveness, and cost-effectiveness.