In vitro Testing to Investigate Effects of Excipients in Drug Formulation

Abstract

The formulation of drugs requires active pharmaceutical ingredients (API), which can be combined with some excipients, which are not considered pharmacologically active and could have different roles in a drug formulation. Glukofen, a generic name as a biguanide antidiabetic, is used for treating type 2 Diabetes Mellitus, mainly in overweight patients when dietary management and exercise do not help in adequate glycemic control. In Glukofen formulation, metformin-HCl as an API and some excipients such as povidone, magnesium stearate, hypromellose, and titanium dioxide are combined. The goal of this study is in vitro investigation of the effects of Glukofen and metformin-HCl on the human bronchial epithelial cell line (Beas-2b). To observe and compare their toxic effects and uptake into cells, cytotoxicity assay and flow cytometry experiments were carried out. The obtained results from this study showed that any toxic effects of both Glukofen and metformin-HCl on Beas-2b cells were not obtained. In addition, uptake of Glukofen into cells was observed more than metformin-HCl. It is evident that the incorporation of excipients to metformin-HCl results in a significant rise in cell proliferation and uptaking into cells.