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Open AccessArticle

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

1
Department of Chemistry, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino (FI), Italy
2
Department of Experimental and Clinical Medicine, University of Florence, Viale Pieraccini 6, 50139 Firenze, Italy
3
Centro di Microscopie Elettroniche “Laura Bonzi” (Ce.M.E.), ICCOM, National Research Council (CNR), Via Madonna del Piano 10, 50019 Sesto Fiorentino (FI), Italy
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 682; https://doi.org/10.3390/pharmaceutics11120682
Received: 8 November 2019 / Revised: 9 December 2019 / Accepted: 13 December 2019 / Published: 15 December 2019
(This article belongs to the Special Issue Emergent Strategies for Natural Products Delivery)
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. View Full-Text
Keywords: vesicles; berberine chloride; escin; dermatological use; rabbit ear skin; human abdominal skin vesicles; berberine chloride; escin; dermatological use; rabbit ear skin; human abdominal skin
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MDPI and ACS Style

Vanti, G.; Bani, D.; Salvatici, M.C.; Bergonzi, M.C.; Bilia, A.R. Development and Percutaneous Permeation Study of Escinosomes, Escin-Based Nanovesicles Loaded with Berberine Chloride. Pharmaceutics 2019, 11, 682.

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