Clotrimazole multiple W/O/W emulsion as anticandidal agent: Characterization and evaluation on skin and mucosae

Soriano-Ruiz, José L.; Suñer-Carbó, Joaquim; Calpena, Ana Cristina; Febrer, Nuria Bozal-de; Bellowa, Lyda Halbaut; Boix-Montañés, Antonio; Souto, Eliana B.; Clares, Beatriz

doi:10.1016/j.colsurfb.2018.11.070

Cited by 23 publications

(20 citation statements)

References 36 publications

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“…As is shown in Figure 4a, the steady shear viscosity sharply decreases and there is an increase in shear rate from 0 to 100 s −1 . The determination of the disturbance of the W 1 /O/W 2 emulsion microstructure during the shearing process of rheological behaviour (Figure 4b) was evaluated by measuring the area of hysteresis loop (Pa/s) called “apparent thixotropy” [17,49,50]. The thixotropic area provides qualitative information about flow time dependence [51].…”

Section: Discussionmentioning

confidence: 99%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming its limited water solubility and its required long-lasting duration of treatments. In this paper, a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention, minimize its skin permeation, and maintain an acceptable level of being harmless in vivo. The formulations were pharmaceutically characterized and application properties were assessed based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration was additionally evaluated. Respective skin permeation was lower than values obtained with a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility of increasing its current 24 h administration frequency more likely. Eventual alterations of skin integrity caused by the formulations were examined with epidermal histological analysis and in vivo preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin integrity descriptors were considered as negligible.

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Section: Discussionmentioning

confidence: 99%

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

et al. 2019

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“…Emulsions are colloidal dispersions in which one immiscible liquid is dispersed in another immiscible liquid in the form of small droplets [1]. There are usually three types of emulsion, including oil in water (O/W), water in oil (W/O), and mixed system (water in oil in water (W/O/W) or oil in water in oil (O/W/O)) [2]. Emulsions are extensively used in food, pharmaceutical, cosmetics, and other fields because of its diversity of types [3,4].…”

Section: Introductionmentioning

confidence: 99%

Food-Grade Gelatin Nanoparticles: Preparation, Characterization, and Preliminary Application for Stabilizing Pickering Emulsions

Feng

Dai

et al. 2019

Foods

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In this paper, the food-grade gelatin nanoparticles (GNPs) were prepared by a two-step desolvation method and using genipin as a cross-linker. The GNPs with narrow size distribution and good dispersion could be obtained only at pH 12. The effect of the genipin dosage (8–12 wt%) on the GNPs was systematically investigated. The results showed that the cross-linking degree of the GNPs increased with the increasing dosage of genipin, thus leading to a more obvious cross-linking morphology observed from scanning electron microscope (SEM). The obtained GNPs showed a good dispersibility with a size range of 386–438 nm. However, the GNPs cross-linked by 8 wt% genipin dosage revealed a relatively higher size because of the aggregation induced by hydrogen bond. The 10 wt% group had good thermal stability and storage stability. The optical microscopy results showed that the Pickering emulsions (30–50 vol% internal phase) stabilized by the GNPs had good uniformity and stability, even after 30 days of storage time, suggesting that the stable GNPs had great potential in food-grade Pickering emulsions.

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“…On the other hand, the pH of topical formulations plays an important role with significant implications [52]. The pH of PLX/CS/HA-VM was 5.0 ± 0.1.…”

Section: Discussionmentioning

confidence: 99%

Endogenous Antioxidant Cocktail Loaded Hydrogel for Topical Wound Healing of Burns

et al. 2020

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The main goal of this work is the study of the skin wound healing efficacy of an antioxidant cocktail consisting of vitamins A, D, E and the endogenous pineal hormone melatonin (MLT), with all of these loaded into a thermosensitive hydrogel delivery system. The resulting formulation was characterized by scanning electron microscopy. The antioxidant efficacy and microbiological activity against Gram positive and Gram negative strains were also assayed. The skin healing efficacy was tested using an in vivo model which included histological evaluation. Furthermore, atomic force microscopy was employed to evaluate the wound healing efficacy of rat skin burns through the determination of its elasticity at the nanoscale using force spectroscopy analysis. The resulting hydrogel exhibited sol state at low temperature and turned into a gel at 30 ± 0.2 °C. The hydrogel containing the antioxidant cocktail showed higher scavenging activity than the hydrogel containing vitamins or MLT, separately. The formulation showed optimal antimicrobial activity. It was comparable to a commercial reference. It was also evidenced that the hydrogel containing the antioxidant cocktail exhibited the strongest healing process in the skin burns of rats, similar to the assayed commercial reference containing silver sulfadiazine. Histological studies confirmed the observed results. Finally, atomic force microscopy demonstrated a similar distribution of Young’s modulus values between burned skin treated with the commercial reference and burned skin treated with hydrogel containing the antioxidant cocktail, and all these with healthy skin. The use of an antioxidant cocktail of vitamins and MLT might be a promising treatment for skin wounds for future clinical studies.

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Clotrimazole multiple W/O/W emulsion as anticandidal agent: Characterization and evaluation on skin and mucosae

Cited by 23 publications

References 36 publications

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery

Food-Grade Gelatin Nanoparticles: Preparation, Characterization, and Preliminary Application for Stabilizing Pickering Emulsions

Endogenous Antioxidant Cocktail Loaded Hydrogel for Topical Wound Healing of Burns

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