Study on encapsulation of Ranolazine in bees wax microspheres:  Preparation, characterization and release kinetics of microspheres 

By D.V. Gowda, Manjunatha M., Balmurlidhara V, Mohammed S. Khan 
 
 

ABSTRACT

The objective of this work to prepare and evaluate beeswax microspheres loaded with ranolazine and minimizes the unwanted side effects of ranolazine by controlled release of drug. Evidence has shown in the recent years that waxes have the physical properties suitable to prepare gastro resistant, biocompatible, biodegradable microspheres to release the entrapped drug in the intestinal lumen.  Ranolazine was entrapped into gastro resistant, biodegradable beeswax wax microspheres using meltable emulsified dispersion cooling induced solidification technique utilizing a wetting agent. Solid, discrete, reproducible free flowing microspheres were obtained. The yield of the microspheres was up to 93 %. More than 96.0 % of the isolated microspheres were of particle size range 115 to 855 mm.   The obtained angle of repose, % Carr’s index and tapped density values were well within the limits, indicating had smooth surface, free flowing and good packing properties for the prepared microspheres. Scanning Electron Microscopy photographs and calculated sphericity factor confirms that the prepared formulations are spherical in nature and size range 345-355. Drug loaded in wax microspheres was stable and compatible, as confirmed by DSC and FTIR studies. The prepared formulations were analyzed quantitatively for the amount of encapsulated drug. It was observed that, there is no significant release of drug at gastric pH. The drug release was controlled more than 8hr. Intestinal drug release from wax microspheres was studied and compared with the release behavior of commercially available oral formulation CarozaÒ500 tablet. The release kinetics followed different transport mechanisms. The drug release performance was greatly affected by the material used in microsphere preparations, which allows absorption in the intestinal tract. 

Key words: Ranolazine, Beeswax microspheres, Characterization, Release kinetics 

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