Formulation and characterization of controlled release bioadhesive nanoparticles encapsulated with Neostigmine Bromide

Abstract

In the recent days targeted drug delivery has gained more prominence for various advantages like site specific delivery and controlled release from the formulations. Amongst the plethora of avenues explored for targeted drug delivery, bioadhesive nanoparticles backed foremost attention offering local drug delivery and controlled drug release solving problems like tissue damage and drug wastage. Formulating nanoparticles with mucoadhesive polymers may provide a significant increase in the gastrointestinal residence time. Neostigmine bromide is a cholinesterase inhibitor used for the treatment of Myasthenia Gravis and is given by conventional routes like oral and intra venous. Bioadhesive nanoparticles of Neostigmine Bromide using synthetic and semi synthetic polymers like Carbopol, HPMC and ethyl cellulose were prepared by emulsification solvent evaporation method. The nanoparticles were characterized for their preformulation and post formulation parameters like compatibility, particle size, zeta potential, encapsulation efficiency, surface morphology, in vitro mucoadhesion, in vivo bioavailability, drug release and stability studies. Out of six, formulations F-1 and F-4 showed the best results for different evaluated parameters of nanoparticles. Entrapment efficiency was found to be within the range of 66.37% and 94.82%. Percentage mucoadhesion was within the range of 71.38% and 99.41%. In vitro dissolution was carried out for 10 hours and the percentage drug release for all the formulations were in the range of 98.93% and 89.71%. In vitro studies conclude that carbopol based nanoparticles are better than HPMC based nanoparticles for the delivery of Neostigmine Bromide. In vivo studies showed that the formulations F1 and F4 showed promising bioavailability compared to orally administered tablet.