Ocular tolerance of sertaconazole gel

Abstract

The in vitro and in vivo tolerance of sertaconazole gel, a new topical azole antifungal, was studied. Ketoconazole gel (Panfungol) was used as a reference substance. The methods applied for tolerance assessment were the bovine corneal opacity and permeability test for the in vitro assay and a modified Draize test for the in vivo assay. The results obtained show that both substances can be classified as slightly irritant and with acceptable tolerance. However, unlike ketoconazole gel, sertaconazole gel did not cause a positive lesion index in vivo. Ketoconazole was 5.25 times more irritant in vitro than sertaconazole gel, whose effect was similar to that of saline solution. Consequently, the negligible irritant effect of sertaconazole gel on a type of epithelium that is extremely sensitive, i.e. the cornea, confirms the good tolerance of this new antifungal gel on other structures such as the skin and mucous membranes.

Solutol HS15 based binary mixed micelles with penetration enhancers for augmented corneal delivery of sertaconazole nitrate: optimization, in vitro, ex vivo and in vivo characterization

“…Sertaconazole nitrate (STZ) is a new antifungal agent of the imidazole class with antifungal activity against wide range of pathogenic fungi, some of which are Fusarium , Aspergillus , and yeasts (Croxtall and Plosker, 2009 ), which are the most common contributory factors for fungal ocular diseases (He et al., 2016 ). STZ is reported to have good ocular tolerance (Romero et al., 1996 ), which makes it an excellent candidate for the treatment of keratomycosis. However, the extreme poor aqueous solubility of STZ acts as an obstacle that limits its ocular clinical efficacy (Albet et al., 1992 ), and urges for the development of new delivery systems capable of enhancing its aqueous solubility, and improving its ocular penetration and retention.…”

Transient Band-like Keratopathy After Treatment for Seborrheic Dermatitis

“…1 Ketoconazole is a mild irritant for ocular mucous membranes. 2 Foster studied the ocular toxicity of topical anti-fungal agents and reported that ketoconazole 1% produced modest changes including superficial punctate keratopathy. 3 The deposits in our patient were in a band-like distribution in the palpebral fissure and appeared elevated and clumpy.…”

Commentary: Considering intrauterine location in a model of fetal growth restriction after maternal titanium dioxide nanoparticle inhalation

“…An endpoint termed "normalized" or "adjusted" fetal weight is not described in regulatory guidance documents (e.g., USEPA, 1998;OECD, 2018). An inverse relationship between fetal body weight and litter size in polytocous species (although not absolute) has been recognized for many years (Romero et al, 1992) and should serve as the basis for developing methods that adjust fetal weights. The potential impact of uterine position on the distribution of nutrients and toxicants (and ultimately fetal health) has also been the subject of numerous investigations over the past 50 years (e.g., Barr et al, 1969;Barr et al, 1970;Ward et al, 1977;Norman and Bruce, 1979a;Norman and Bruce, 1979b;Padmanabhan and Singh, 1981).…”