Development and Evaluation of Liquid and Solid Lipid Based Drug Delivery Systems Containing Technetium-99m-Radiolabeled Alendronate Sodium

Abstract

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 investigated.

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.

Keywords: RTLS; Spray drying method; alendronate sodium; lipid-water based drug delivery system; radiolabeling; technetium-99m..