The study was focused on the development of nanovesicles based on phosphatidylcholine, cholesterol and Escin (ESN) and loaded with Berberine Chloride (BRB HCl), to obtain a therapeutic synergism. Hence, ESN was selected for both structural and functional activity. ESN exhibits many pharmacological activities, such as anti-inflammatory, anti-edematous and veno-tonic properties [1]. BRB HCL, a natural isoquinoline alkaloid, is used in medicine because of numerous activities, principally cardiovascular, anti-inflammatory, antimicrobial, and anti-cancer effects [2]. Diverse nanovesicles were developed using different combinations of these compounds, in order to select the formulation with the best biopharmaceutical parameters. All the developed nanovesicles were fully characterized in terms of dimension and morphology, zeta potential, polydispersion and drug loading as previously reported [3,4]. The optimized nanovesicles enclose were prepared with phosphatidylcholine, ESN and BRB HCl in the ratio 33:5:1.3 mg/ml, respectively. The nanovesicles displayed an average diameter of 208 nm, polydispersity index was 0.18, ΞΆ potential was -24.8. Vesicles had spherical shape. In vitro release of BRB HCl showed an initial burst effect, followed by a prolonged release for 24 h.
Vesicles subjected to in vitro permeation studies, using a system of parallel artificial membranes (PAMPA ) had a better permeation profile in comparison with free BRB HCl, also confirmed by an ex vivo permeation assay performed with rabbit ear skin.
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[4] Leto I, Coronnello M, Righeschi C, Bergonzi MC, Mini E, Bilia AR. ChemMedChem. 2016, 11(16):1745-51.