Article Details


A New Application Route of Nitrofurantoin: Preparation and Characterization of Novel Transdermal Formulations

[ Vol. 14 , Issue. 3 ]

Author(s):

Mesut Arici, Salih Kavukcu, Sakine Tuncay Tanriverdi, Aylin Arici, Sedef Gidener, Ayse Gelal and Ozgen Ozer   Pages 394 - 405 ( 12 )

Abstract:


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 (p>0.05).

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.

Keywords:

Film formulations, gel formulations, microemulsions, nitrofurantoin, transdermal drug delivery, urinary tract infections.

Affiliation:

Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Izmir,, Dokuz Eylul University, School of Medicine, Department of Pediatrics, Izmir,, Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 35100, Bornova, Izmir-, Dokuz Eylul University, School of Medicine, Department of Medical Pharmacology, Izmir,, Dokuz Eylul University, School of Medicine, Department of Medical Pharmacology, Izmir,, Dokuz Eylul University, School of Medicine, Department of Medical Pharmacology, Izmir,, Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Izmir

Graphical Abstract:



Read Full-Text article