Fexofenadine HCl microspheres with HPMC K100 MCR Polymer Springerplus Open Access

Posted: 9 months ago

Arefin et al. SpringerPlus (2016) 5:691
DOI 10.1186/s40064-016-2322-2


The aim of the current study was to formulate Fexofenadine hydrochloride loaded
sustained release microspheres using HPMC K100 M CR, a release retardant hydrophilic
polymer by solvent evaporation method. The effect of different drug loading on drug
content, drug encapsulation efficiency and release of drug was monitored. The studies
on in vitro release mechanism were performed using USP paddle method with 900 ml
of phosphate buffer (pH 6.8) for 10 h at 100 rpm. The mechanism of the drug release
was determined by fitting in vitro release data to various release kinetic models such
as the zero order, first order, Higuchi, Hixson Crowell and Korsemeyer–Peppas model
and finding R2 values for the release profile corresponding to each model. The results
confirm that the release rate of the drug from the microspheres is highly affected by
the drug to polymer ratio. The study finds that Higuchi release kinetics, Korsmeyer–
Peppas release kinetics and Hixson–Crowell release kinetics were the major release
mechanism. The release mechanism was found to be non-Fickian with increase of
polymer content. Scanning electron microscopic technique was performed to obtain
the morphological changes due to different drug loading. Differential scanning calorimetry
and Fourier transform infra-red spectroscopy was performed to determine any
interaction of drug with the polymer. A statistically significant variation in release rate
was observed for variation in the amount of HPMC K100 M CR. In the present study, a
series of sustained release formulations of Fexofenadine hydrochloride were developed
with different drug loading so that these formulations could further be evaluated from
the in vivo studies. The formulations were found to be stable and reproducible.
Keywords: Emulsification-solvent evaporation, Fexofenadine HCl, Microsphere