ABSTRACT

The objective of the current investigation was to formulate mucoadhesive microspheres loaded with dabigatran utilizing Eudragit RL100 as the mucoadhesive polymer and stabilizing the particles with magnesium stearate so that the formulation could control the release of the drug thereby reducing its dosing frequency and improving the bioavailability. The microspheres were prepared using emulsion coacervation method and the micromeritic features were evaluated. The angle of repose for all formulations was found to be within the range from 23.54 ± 0.122 to 25.47 ± 0.0721°. This indicates that good flow property of powder blend. The bulk density and tapped density values were found to be within the range from 0.37 ± 0.01 to 0.61 ± 0.01 g/cm3 and 0.44 ± 0.005 to 0.73 ± 0.01 g/cm3 respectively. The values of Hausner’s ratio ranged from 1.16 to 1.20 whereas the Carr’s Index ranged from 13.46 to 20.29. The yield of all the batches of microspheres was found to be reasonably good ranging from 53.69% to 74.18%. The drug loading was found to be 73.81 ± 0.345% to 74.44 ± 0.313 % while the size of microspheres ranged from 13.28 ± 0.170 to 17.26 ± 0.255 ?m. Swelling study was performed on all the formulation for 24 h and swelling index ranged from 2.93 to 4.18. The mucoadhesion time of the microspheres ranged from 2h41min to 6h 45min. All the formulations were able to sustain the release of dabigtran for more than 12h. Keywords: Gastroretentive, microspheres, mucoadhesion, swelling, Eudragit RL 100
Publication date: 01/03/2024

https://ijbpas.com/pdf/2024/March/MS_IJBPAS_2024_7900.pdf

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https://doi.org/10.31032/IJBPAS/2024/13.3.7900