Formulation and Evaluation of Floating Polymeric Nanoparticles of Linagliptin in Capsules

Objectives: Linagliptin is a BCS class III drug used in treatment of diabetes. In the present study floating polymeric nanoparticles of linagliptin are formulated to increase the residence time of drug in stomach by controlling drug delivery over a prolonged period of time and to increase permeability by nanosized particles, there by bioavailability can be increased. Methods: Polymeric nanoparticles were prepared by desolvation and ion gelation method. The prepared polymeric nanoparticles were evaluated for entrapment efficiency, drug content, percentage yield, diffusion studies and dissolution studies. Results: Among various formulations, GF2 formulation by ion gelation method, CF5 by desolvation (continuous addition) method and IF1 by desolation (intermittent addition) method have shown % drug release of 91.8±0.50%, 92.8±0.33% and 91.5±31% in 210min respectively. GF2 was considered as the optimized formulation based on its high entrapment efficiency of 88.6±1.09%, cumulative amount permeated of 997.0±2.15µg/cm2 for 4hrs, Zeta potential (-20.3mV), particle size (396 nm) and SEM (spherical and smooth surface). The GF2 formulation was converted into floating drug delivery system with sodium bicarbonate and different concentration of ethyl cellulose, HPMC E15M. GF2 (1:2 ratio of drug:ethyl cellulose) was optimized as it showed prolonged drug release by retaining drug through mucosa of goat with % drug release (53.1±0.50 % at 5.5 hrs) in comparison with pure drug (99.8±0.19% at 1 hr) and it was stable as per ICH guidelines. Conclusion: Hence the drug release has been retarded, permeation has been enhanced and residence time of drug in the stomach has been extended by floating polymeric nanoparticles.