“Plurethosome” as Vesicular System for Cutaneous Administration of Mangiferin: Formulative Study and 3D Skin Tissue Evaluation

Abstract

Human skin is dramatically exposed to toxic pollutants such as ozone. To counteract the skin disorders induced by the air pollution, natural antioxidants such as mangiferin could be employed. A formulative study for the development of vesicular systems for mangiferin based on phosphatidylcholine and the block copolymer pluronic is described. Plurethosomes were designed for mangiferin transdermal administration and compared to ethosome and transethosome. Particularly, the effect of vesicle composition was investigated on size distribution, inner and outer morphology by photon correlation spectroscopy, small angle X-ray diffraction, and transmission electron microscopy. The potential of selected formulations as vehicles for mangiferin was studied, evaluating encapsulation efficiency and in vitro diffusion parameters by Franz cells. The mangiferin antioxidant capacity was verified by the 2,2-diphenyl-1-picrylhydrazyl assay. Vesicle size spanned between 200 and 550 nm, being influenced by phosphatidylcholine concentration and by the presence of polysorbate or pluronic. The vesicle supramolecular structure was multilamellar in the case of ethosome or plurethosome and unilamellar in the case of transethosome. A linear diffusion of mangiferin in the case of ethosome and transethosomes and a biphasic profile in the case of plurethosomes indicated the capability of multilamellar vesicles to retain the drug more efficaciously than the unilamellar ones. The antioxidant and anti-inflammatory potential effect of mangiferin against pollutants was evaluated on 3D human skin models exposed to O3. The protective effect exerted by plurethosomes and transethosomes suggests their possible application to enhance the cutaneous antioxidant defense status.

Ethosomes and Transethosomes as Cutaneous Delivery Systems for Quercetin: A Preliminary Study on Melanoma Cells

“…The aliquot of QT in the water phase is in agreement with the findings about localization of the molecule within the bilayer at the polar–nonpolar interface ( Figure S3 ), forming reversible physico-chemical complexes with PC [ 53 ]. This QT position could alter the packing density of the bilayers, softening the membrane, finally affecting the EC, as previously found for mangiferin-loaded ETO and T-ETO [ 41 , 52 ]. Nonetheless, the highest EC obtained in the case of T-ETO 2.7 -QT suggests that the presence of T80 can better stabilize the vesicles based on PC 2.7%, possibly improving QT interaction with PC, thus maintaining the drug associated to the bilayer supramolecular structure, as tentatively depicted in Figure S4 .…”

“…With regard to the different lamellar organization of ETO and T-ETO observed by cryo-TEM, it should be mentioned that a disordering of the lamellar organization can be the result of the intercalation of the T80 oleate chain within the lipid bilayer. In addition, the polar terminal groups of the polyoxyethylene oxide chains could affect the aqueous compartment swelling [ 52 ].…”

Vesicular Nanocarriers for Phytocompounds in Wound Care: Preparation and Characterization

“…Afterward, the “ethosomes effect” occurs, by the opening of new pathways due to the malleability and fusion of these nanovesicles with skin lipids, enhancing the inter-lipid penetration and permeation. Thus, the result consists of the deposition and release of PCs into the deep layers of intact or damaged skin, revealing the potential of ethosomes in wound-healing applications [ 11 , 12 , 42 , 61 , 79 , 80 , 81 , 82 ].…”

“…In wound-healing applications, ethosomes encapsulating Fraxinus angustifolia [ 27 ] extract, PCs such as curcumin [ 80 ], or drugs such as piroxicam [ 79 ] have been previously reported. Currently, ethosomes are primarily used for efficient topical delivery into deep layers of the skin or across the skin for both local and systemic delivery [ 11 , 12 , 42 , 61 , 79 , 80 , 81 , 82 ].…”

“…They have been developed by combining ethanol and a surfactant, employed as an edge activator to improve the deformability of vesicles. The characteristics of transethosomes are the increased flexibility and the major transdermal potential [ 41 , 82 , 83 ] even though some authors reported negative effects on human skin, such as inflammation induced by these surfactant-based nanocarriers [ 59 ].…”