4 research outputs found
Ex-Vivo and In-Vivo Assessment of Cyclamen europaeum Extract After Nasal Administration
Rhinosinusitis is a prevalent disorder with a severe impact on the health-related quality of life. Saponins of Cyclamen europaeum exert a clinically proven curative effect on rhinosinusitis symptoms when instilled into the nasal cavity, however, more extensive preclinical assessment is required to better characterize the efficacy of this botanical extract. This work evaluates the potential use of a natural freeze-dried extract of C. europaeum given as topical nasal administration. Permeation experiment on porcine nasal mucosa was performed with Franz diffusion cells. Experiments in rabbits were performed to test for any toxicological, hematological, biochemical or histological evidence of systemic action. No theoretical levels of saponins were found in the receptor chamber of Franz diffusion cells. Hematological data did not show significant differences between control and experimental animals (p > 0.05). Histological studies also showed that enhanced secretory activity in response to intranasal administration was not accompanied by any visible signs of injury. An examination of the brain, lungs, liver, kidneys, spleen, and gastrointestinal organs did not reveal any abnormality. The absence of mucosal permeation of saponins and negligible probability of C. europaeum saponins absorption in the course of a therapeutic application was demonstrated
Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
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.There are no specific funding sources or universitary fellowship for this experimental work.
Article processing charges were partially supported by University of Barcelona