Development and Percutaneous Permeation Study of Escinosomes, Escin-Based Nanovesicles Loaded with Berberine Chloride

Abstract

Escin is a natural saponin, clinically used for the anti-edematous and anti-inflammatory effects. The aim of the study was to explore the possibility of converting escin into vesicle bilayer-forming component. The hyaluronidase inhibition activity of escin was evaluated after its formulation in escinosomes. Berberine chloride, a natural quaternary isoquinoline alkaloid isolated from several medicinal plants that is traditionally used for various skin conditions was loaded in the vesicles. The developed nanovesicles were characterized in terms of diameter, polydispersity, ζ-potential, deformability, recovery, encapsulation efficiency, stability, and release kinetics. Nanovesicle permeation properties through artificial membranes and rabbit ear skin were investigated using skin-PAMPATM and Franz cells were also evaluated. Escinosomes, made of phosphatidylcholine and escin, were loaded with berberine chloride. These nanovesicles displayed the best characteristics for skin application, particularly optimal polydispersity (0.17) and deformability, high negative ζ-potential value, great encapsulation efficiency (about 67%), high stability, and the best release properties of berberine chloride (about 75% after 24 h). In conclusion, escinosomes seem to be new vesicular carriers, capable to maintain escin properties such as hyaluronidase inhibition activity, and able to load other active molecules such as berberine chloride, in order to enhance or expand the activity of the loaded drug.

<p>Berberine-Loaded Thiolated Pluronic F127 Polymeric Micelles for Improving Skin Permeation and Retention</p>

“…Recently, to increase the skin bioavailability of berberine, Giulia Vanti and his research group prepared berberine-loaded escinosomes, and they proved that hydrogels formulated with berberine-loaded escinosomes had the highest berberine skin absorption both in terms of absorbed dose and of dose retained inside the skin. 6,7 Therefore, a novel formulation that improves the skin permeability and retention of BH would greatly increase the antibacterial effects of the drug and the compliance of patients.…”

Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression

“…The nanoliposomes were prepared according to the thin layer evaporation method as previously reported [ 22 ]. Two phospholipids, namely natural P90G and P100H, and cholesterol were used for the preparation of the vesicles, testing different combinations and gravimetric ratios, as reported in Table 1 .…”

Nanovesicles Loaded with Origanum onites and Satureja thymbra Essential Oils and Their Activity against Food-Borne Pathogens and Spoilage Microorganisms

“…Successively, the two systems loaded with OOEO plus STEO were observed by transmission electron microscope, TEM (CM12 TEM, PHILIPS, Eindhoven, The Netherlands) equipped with an OLYMPUS Megaview G2 camera, with an accelerating voltage of 80 kV. A drop of sample, 5-folds diluted in water, was applied and dried by desiccation on a carbon film copper grid and it was counterstained with 1% w / v of phosphotungstic acid solution for 3 min [ 40 ]. Then, the sample was examined at different amplifications.…”