Objective: The purpose of this study was to develop lipid-water based drug delivery system
of Alendronate Sodium (ALD) in liquid and solid form obtained by using spray drying method and
compare these two forms with radioactive cell culture studies.
Methods: This study included the development of liquid and solid form obtained by spray drying method,
radiolabelling of ALD with 99mTc, preparation of formulations containing 99mTc -ALD and evaluation
of their permeability with Caco-2 cell. The liquid formulations have been developed by using various
surfactants, co-surfactants, oil and water phases. Physicochemical characterizations like droplet
size, polydispersity index (PDI) and zeta potential measurements and short term stability studies were
Results: According to the measurement results, two oil in water formulations (F1-L and F2-L) were
selected and spray dried with Buchi mini spray dryer apparatus to provide solid formulations (F1-S and
F2-S). ALD was labeled with 99mTc and added to formulations. The effect of experimental conditions on
radiolabeling efficiency of ALD and stability of all formulations containing 99mTc-ALD were investigated
through Radio Thin Layer Chromatography (RTLC). It was observed that the labeling efficiency
of ALD was greater than 90% and all formulations were found to be stable up to 6 h at room temperature.
Permeability of radiolabeled ALD from all formulations was performed by using Caco-2 cells.
According to the cell culture studies, permeability from spray dried formulations of ALD was found
higher than liquid formulations.
Conclusion: As a conclusion, spray dried formulations could be a promising drug delivery system for
enhancing the permeability of ALD. Furthermore, this study is a good example of the use of radiolabeled
compounds in drug development.