Nanolipidgel for Enhanced Skin Deposition and Improved Antifungal Activity

Abstract

Abstract. The purpose of the research was to prepare and evaluate a topical nanolipidgel (NLH) of terbinafine hydrochloride (TRB), an antimycotic agent, for enhanced skin deposition and improved antifungal activity. Topical solid lipid nanoparticles (SLN) based nanolipidgel was formulated and evaluated. TRB-loaded SLNs were formulated by high-pressure homogenization technique. The stable TRB SLN dispersion was incorporated into a gel using 1% Carbopol 980 NF. Rheological evaluation and texture analysis of the TRB NLH was carried out. Skin permeation, skin deposition, antifungal activity, and occlusivity studies of the nanolipidgel formulation were carried out. The safety of the TRB NLH gel was evaluated using acute skin irritation test on New Zealand White rabbits. The SLN dispersion containing 10% of glyceryl monostearate, 3% of Tween 80, and 1% Plurol Oleique was the most stable. The optimized TRB SLN had a particle size and zeta potential value of 148.6 ± 0.305 nm and −20.4 ±1.2 mV, respectively. TRB NLH had excellent rheological and texture properties to facilitate its topical application. TRB NLH showed increased skin deposition of the drug over plain (3-fold) and marketed TRB formulation (2-fold). TRB NLH had significantly enhanced antifungal activity against Candida albicans. TRB NLH showed efficient occlusivity and was non-irritant to the rabbit skin with no signs of erythema or edema. Solid lipid nanoparticles-based topical nanolipidgel of terbinafine can be an efficient, industrially scalable, and cost-effective alternative to the existing conventional formulations.KEY WORDS: in vitro antifungal activity; rheological analysis of gel; solid lipid nanoparticles; terbinafine; texture analysis of gel.

Effects of Carbopol^® 934 proportion on nanoemulsion gel for topical and transdermal drug delivery: a skin permeation study

“…Similar studies also reported that droplets moved more slowly from the inner phase to the outer phase in CG than in NG, probably because the droplets were larger in CG. 33,34 Ter and cIT accumulation in the sc and epidermis/dermis…”

“…33,34 Moreover, differences in fluorescence signals among the NGs showed that the proportion of CP934 influenced the skin permeation rates by altering the main skin permeation routes. There are three major routes for drug penetration into the subepidermal tissue: hair follicles together with their sebaceous glands, sweat ducts, and the SC (including transcellular and intercellular routes).…”

Novel lecithin-integrated liquid crystalline nanogels for enhanced cutaneous targeting of terconazole: development, in vitro and in vivo studies

“…The sample was placed between the gap of the cone and plate, and the gap was closed gradually. 37 Then the sample was subjected to a dynamic shear rate ranging from 7.5 to 45 S −1 (1-6 rpm) where shear stress and viscosity were measured. All the measurements were performed at isothermal condition at room temperature (25°C±2°C).…”

“…Female Swiss albino mice of 20-25 g were selected for these studies. The negative control group was treated with normal saline 45 while formalin was used as a standard irritant 20,37 for the positive control group. The dorsal region of mice was shaved 24 h prior to the application of the formulations 52 using a hair remover cream (Veet ® , Reckitt Benchiser).…”

“…Nonionic and cationic surfactants were suggested to have antifungal activity due to the inhibition of the steroidal component of the fungi, which forms an integral part of its cell wall by their surface-tension-lowering activity. 37,67 Moreover, capryol 90 contains 10% capric acid, which was reported to have antifungal activity. 68 Therefore, it is worthy to note that …”