DOI: 10.5176/2345-783X_PHARMA14.33
Authors: D.Nagasamy Venkatesh
Abstract:
Ranolazine an anti-anginal drug, used for the treatment of angina, exhibiting poor aqueous solubility resulting in low oral bioavailability. Therefore, in the present study ranolazine loaded chitosan nanoparticles were formulated to overcome the drawbacks associated with the conventional therapy. The ranolazine loaded chiosan nanoparticles were prepared by ionic gelation method using tripolyphosphate. Different batches of nanoparticles formulations were prepared employing different concentrations of polymer to drug ratio. The formulated nanoparticles were evaluated for its particle size, zeta potential, drug content, drug loading, entrapment efficiency, in vitro drug release, kinetic studies and in vivo oral bioavailability studies. The infrared spectra and differential scanning calorimetry thermographs showed stable character of ranolazine and chitosan mixture and revealed the absence of drug-polymer interactions. The chitosan nanoparticles of optimized batch exhibited a mean particle size of 374.6 nm and a zeta potential of 6.95 mV, highest drug content of 4.81mg, drug loading of 48.1{6e6090cdd558c53a8bc18225ef4499fead9160abd3419ad4f137e902b483c465}, and entrapment efficiency of 19.53{6e6090cdd558c53a8bc18225ef4499fead9160abd3419ad4f137e902b483c465}. The in vitro release behavior from the chitosan nanoparticles found to follow first order kinetics offering a sustained release over a period of 24 h. In vivo oral bioavailability studies indicated that, there was more than 1.81 times fold increase in oral bioavailability in case of nanoparticles as compared to ranolazine solution. These results indicated that bioavailability is enhanced significantly by employing nanoparticles formulations of ranolazine using chitosan offer a new approach to improve the oral bioavailability of poorly soluble drugs.
Keywords: Chitosan nanoparticles, ionic gelation, in vitro, oral bioavailability
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