Objectives: Nitrofurantoin is widely used in the prophylaxis of urinary-tract infections. The
aim of this study was to develop and characterize innovative transdermal formulations of nitrofurantoin,
to increase the patient compliance and decrease the adverse effects such as nausea and vomiting which
limit the drug use in long-term.
Methods: Nitrofurantoin loaded microemulsion, gel (hydrogel, lipogel and DMSO gel) and film formulations
were prepared and characterized via several parameters. Ex-vivo drug permeation studies were
performed to determine the amount of drug permeated through the rat skin. In in-vivo studies, in order
to detect nitrofurantoin in urine, the selected formulations were applied to male Wistar rats transdermally.
Also, skin irritation tests (transepidermal water loss and erythema) were performed.
Results: All nitrofurantoin loaded formulations were prepared successfully and were stable at +4°C for
3 months. 13%, 16%, 32.5%, 36.5% and 39% of drugs permeated through the rat skin in the 168th hour
for hydrogel, lipogel, film, microemulsion and DMSO gel, respectively. Only with film and DMSO gel
formulations, nitrofurantoin was detected in urine. Transepidermal water loss was increased compared
to basal level in film type formulations (p<0.05). However, in erythema experiments there was no difference
Conclusion: There is no approved transdermal formulation of nitrofurantion on the market. Therefore,
the prepared film formulations could be an alternative due to their high penetration through the rat skin,
the presence of nitrofurantoin in urine and because they cause no irritation on the skin.