Development and Evaluation of New Microemulsion-Based Hydrogel Formulations for Topical Delivery of Fluconazole

Abstract

Abstract. The aim of the present investigation was to develop and evaluate microemulsion-loaded hydrogels (MEHs) for the topical delivery of fluconazole (FZ). The solubility of FZ in oils, surfactants and cosurfactants was evaluated to identify the components of the microemulsion. The pseudo-ternary phase diagrams were constructed using the novel phase diagram by micro-plate dilution method. Carbopol EDT 2020 was used to convert FZ-loaded microemulsions into gel form without affecting their structure. The selected microemulsions were assessed for globule size, zeta potential and polidispersity index. Besides this, the microemulsion-loaded hydrogel (MEH) formulations were evaluated for drug content, pH, rheological properties and in vitro drug release through synthetic membrane and excised pig ear skin in comparison with a conventional hydrogel. The optimised MEH FZ formulations consisting of FZ 2%, Transcutol P 11.5% and 11%, respectively, as oil phase, Lansurf SML 20-propyleneglycol 52% and 50%, respectively, as surfactant-cosurfactant (2:1), Carbopol EDT 2020 1.5% as gelling agent and water 34.5% and 37%, respectively, showed highest flux values and high release rate values, and furthermore, they had low surfactant content. The in vitro FZ permeation through synthetic membrane and excised pig ear skin from the studied MEHs was best described by the zero-order and first-order models. Finally, the optimised MEH FZ formulations showed similar or slightly higher antifungal activity as compared to that of conventional hydrogel and Nizoral® cream, respectively. The results suggest the potential use of developed MEHs as vehicles for topical delivery of FZ, encouraging further in vitro and in vivo evaluation.

Colloidal nanocarriers for the enhanced cutaneous delivery of naftifine: characterization studies and in vitro and in vivo evaluations

“…Microemulsions have been extensively explored for a variety of pharmaceutical applications, including dermal and transdermal drug delivery. [6][7][8][9] The use of these nanocarriers in skin drug delivery has been frequently exploited and has proven highly successful for the delivery of both hydrophilic and lipophilic compounds. 10 Most of the studies demonstrated that more pronounced cutaneous drug localization in skin layers rather than percutaneous permeation can be obtained with microemulsions.…”

Alkyl polyglucoside vs. ethoxylated surfactant-based microemulsions as vehicles for two poorly water-soluble drugs: physicochemical characterization and in vivo skin performance

“…In contrast, alkyl polyoxyethylenes usually differ in sizes of both parts of the molecule, i.e., the hydrophilic and the lipophilic ones, resulting in different HLB values. It is well known that for optimal solubilization capability, a mixture of surfactant and cosurfactant should have a suitable HLB value, within the range required for the preparation of microemulsions (3,26). In our case, both APG (P810) and ethylene oxide-based (P80) surfactants, which produced a wider monophasic area, had HLB values around 15.…”

“…Also, as previously reported (1,26), the enhanced skin penetration and maximum flux in dermal drug delivery are not usually obtained with formulations that contain maximum surfactant concentration.…”

“…However, higher solubility of the selected model drugs in EV may be considered advantageous (Table I). This may allow the concentration of the surfactant to be reduced in the final drug-loaded formulation, which in turn increases the biocompatibility of the microemulsion system (15,25,26).…”

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

“…61,62 Drug content homogeneity of the chosen liquid crystalline organogel was determined by a validated UV spectrophotometric assay at λ=243 nm (y =0.0263x +0.0391, R²=0.9993, the precision (%RSD) ranged from 0.10% to 0.69% and 0.44% to 2.13% for intraday and inter-day, respectively, the accuracy (% recovery) of intra-day and inter-day ranged from 98.80% to 101.52% and 98.48% to 101.72%, respectively. The drug content was calculated from the calibration curve and expressed as (mean % ± standard deviation [SD]), n=3 and compared with that obtained from the HPMC hydrogel.…”