This study examined a novel
alendronate formulation that was developed to overcome the shortcomings of
alendronate, such as its low bioavailability and gastric adverse effects.
Alendronate microparticles were prepared using mucoadhesive
polymers such as
chitosan for improving the intestinal cellular absorption of
alendronate and also using a gastric-resistant
polymer such as
Eudragit L100-55 for reducing the gastric
inflammation of
alendronate.
Alendronate microparticles including
chitosan showed a threefold increase in
alendronate uptake (6.92 ± 0.27%) in Caco-2 cells when compared with the uptake of
alendronate solution (2.38 ± 0.27%) into Caco-2 cells. Most interestingly,
alendronate microparticles including
chitosan showed 2.80 x 10⁻⁶ cm/s of an apparent permeability coefficient across Caco-2 cells and caused a significant 42.4% enhancement compared with that of
alendronate solution across Caco-2 cells. The morphology of the Caco-2 cells treated with
alendronate microparticles including
chitosan was similar to that of the untreated cells and
alendronate microparticles exhibited a negative effect to propodium
iodide with some
annexin-V fluorescence isothiocyante positive effect. It was proposed that the novel
alendronate microparticles could possess the potential of an increased intestinal absorption and fewer adverse effects of
alendronate.