The Evaluation and Various Development of Mucoadhesive Microspheres System of Simvastatin |

ABSTRACT:

The objective of the present study was to prepare andevaluate the mucoadhesive microspheres of Simvastatin. Simvastatin microsphereswere prepared by orifice-ionotropic gelation method using polymers such as HPMC(K 100 M), carbopol 940P, sodium CMC, guar gum, sodium alginate, ethylcellulose, methyl cellulose and xanthan gum. Totally 15 different formulationsof Simvastatin were prepared by using the above polymers. The microspheres werecharacterized for drug content, entrapment efficiency, mucoadhesive property byin vitro wash-off test and in-vitro drug release. Theformulation F10 was selected as an ideal formulation based on the in vitro release profile which showsan extended drug release of 97.11% upto 8 hours in phosphate buffer of pH 7.0.Surface morphology (SEM analysis) and drug-polymer interaction studies (FT-IRanalysis) were performed only for the ideal formulation, F10. The microsphereswere smooth and elegant in appearance showed no visible cracks as confirmed bySEM and FT-IR studies indicated the lack of drug-polymer interactions in theideal formulation, F10. The in vitro releasedata of all microsphere formulations were plotted in various kinetic equationsto understand the mechanisms and kinetics of drug release. The idealformulation, F10 followed Higuchi kinetics and value of "n," iscalculated to be 0.86 indicated that the drug release shows non-Fickiandiffusion. The microspheres were evaluated for particle size andshape and surface morphology by SEM, drug loading, drug incorporationefficiency, In vitro mucoadhesion,and In vitro drug releasestudy. Particle size was found to be in the range of 29.48 to 37.08 μm, whichis favourable for intranasal absorption. Mucoadhesion had been a topic of interest in the designof drug delivery system to prolong the residence time of the dosage form withthe underlying absorption surface to improve and enhance the bioavailability ofdrugs.