Development of topical hydrogels of terbinafine hydrochloride and evaluation of their antifungal activity

Celebi N., Ermis S., Ozkan S.

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, vol.41, no.4, pp.631-639, 2015 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 41 Issue: 4
  • Publication Date: 2015
  • Doi Number: 10.3109/03639045.2014.891129
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.631-639
  • Keywords: Antifungal activity, hydrogels, in vitro release, microemulsion-based gel, terbinafine hydrochloride, DRUG-DELIVERY, IN-VITRO, PERCUTANEOUS-ABSORPTION, MICROEMULSIONS, CHITOSAN, RELEASE, GEL, FORMULATION, SUSCEPTIBILITY, DERMATOPHYTES
  • Gazi University Affiliated: Yes


The purpose of this study was to prepare hydrogels and microemulsion (ME)-based gel formulations containing 1% terbinafine hydrochloride (TER-HCL) and to evaluate the use of these formulations for the antifungal treatment of fungal infections. Three different hydrogel formulations were prepared using chitosan, Carbopol (R) 974 and Natrosol (R) 250 polymers. A pseudo-ternary phase diagram was constructed, and starting from ME formulation, a ME gel form containing 1% Carbopol 974 was prepared. We also examined the characteristic properties of the prepared hyrogels. The physical stability of hydrogels and the ME -based gels were evaluated after storage at different temperatures for a period of 3 months. The release of TER-HCL from the gels and the commercial product (Lamisil (R)) was carried out by using a standard dialysis membrane in phosphate buffer (pH 5.2) at 32 degrees C. The results of the in vitro release study showed that the Natrosol gel released the highest amount of drug, followed by Carbopol gel, chitosan gel, commercial product, and the microoemulsion-based gel in that order. In vitro examination of antifungal activity revealed that all the prepared and commercial products were effective against Candida parapsilosis, Penicillium, Aspergillus niger and Microsporum. These results indicate that the Natrosol (R)-based hydrogel is a good candidate for the topical delivery of TER-HCL.