ABSTRACT The current study focused on the formulation of tenofovir disoproxil fumarate (TDF)‐loaded alginate‐karaya gum (KG) beads for pH‐responsive sustained release. In this work, TDF‐loaded alginate‐KG beads were prepared via ionic gelation technique using Ca +2 and Ba +2 cations (where 10% w/v CaCl 2 and BaCl 2 aqueous solutions were used as ionic crosslinking solutions, respectively). These TDF‐loaded alginate‐KG beads showed 60.26 ± 2.98% to 88.08 ± 3.87% of drug encapsulation efficiency (%) and 902.16 ± 20.48 µm to 1300.12 ± 20.54 µm of particle size. Ba +2 ions‐crosslinked alginate‐KG beads loaded with TDF exhibited higher drug encapsulation and smaller particle size than Ca +2 ions‐crosslinked alginate‐KG beads loaded with TDF. These TDF‐loaded alginate‐KG beads were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, X‐ray diffraction, and thermogravimetric analysis. The sodium alginate to KG ratio and divalent cations (Ca +2 and Ba +2 ) exhibited pronounced effects on the TDF release (in vitro) from TDF‐loaded alginate‐KG beads. Both the in vitro TDF‐releasing and swelling behavior of alginate‐KG beads loaded with TDF were found to be considerably increased when the media pH was increased. Regardless of pH, Ba +2 ions‐crosslinked alginate‐KG beads loaded with TDF exhibited more sustained drug release (in vitro) and decreased swelling (in vitro) as compared to those of Ca +2 ions‐crosslinked alginate‐KG beads loaded with TDF, indicating their suitability for sustained release oral delivery of TDF.
Pal et al. (Thu,) studied this question.