Planta Med 2019; 85(18): 1453
DOI: 10.1055/s-0039-3399807
Main Congress Poster
Poster Session 1
© Georg Thieme Verlag KG Stuttgart · New York

Development of escin-based nanovesicles loaded with berberine chloride and percutaneous permeation study

G Vanti
1   University of Florence,, Department of Chemistry “Ugo Schiff”, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), ItalY
,
D Bani
2   University of FlorencE,, Department of Experimental and Clinical Medicine, Viale Pieraccini 6, 50139 Florence, Italy
,
M Wang
3   Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine,, Tianjin 300193, China
,
Z Liu
3   Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine,, Tianjin 300193, China
4   Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of education, Tianjin University of Traditional Chinese Medicine,, Tianjin 300193, China
,
V Piazzini
1   University of Florence,, Department of Chemistry “Ugo Schiff”, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), ItalY
,
L Risaliti
1   University of Florence,, Department of Chemistry “Ugo Schiff”, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), ItalY
,
MC Bergonzi
1   University of Florence,, Department of Chemistry “Ugo Schiff”, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), ItalY
,
AR Bilia
1   University of Florence,, Department of Chemistry “Ugo Schiff”, Via U. Schiff 6, 50019 Sesto Fiorentino (FI), ItalY
› Author Affiliations
Further Information

Publication History

Publication Date:
20 December 2019 (online)

 

Escin (ESN) is the major active constituent isolated from the Aesculus hippocastanum. ESN is clinically used as anti-inflammatory and anti-oedema agent, as well as to increase venous wall tone [1]. Due to its chemical structure, it was selected in order to study its ability in replacing cholesterol inside the liposome bilayer. The obtained new liposome was tested for its carrier properties, loading a natural active molecule, berberine chloride (BRB HCl). BRB is an isoquinoline alkaloid used in the Traditional Chinese Medicine from the ancient times, because of its several therapeutic properties [2]. Different liposomes made of ESN and loaded with BRB HCl were prepared according to the thin-layer evaporation method. All liposomes showed an high ζ-potential, a low polydispersity index and spherical shape, by light scattering analysis and microscope observation, respectively. The dialysis bag method, followed by HPLC-DAD analysis, was used in order to determine the Encapsulation Efficiency (EE) and to investigate the in vitro release of BRB HCl and ESN, with the following results: the EE was approximately 67% for BRB HCl and 94% for ESN. Liposomes chemical-physical stability was monitored for a month, at 4°C and the deformability was evaluated by extrusion. Successively, the cutaneous absorption was studied by skin-PAMPA (parallel artificial membrane permeation assay) and the in vitro permeation assay on rabbit ear skin, using vertical diffusion Franz cells. The passive transport through the skin was comparable for the ESN liposome and the conventional cholesterol liposome. Moreover liposome loaded with ESN and BRB HCl showed an higher permeation for ESN and BRB HCl, compared to the free molecules. Finally, the in vivo irritation test on rats proved the suitability of this co-delivering formulation for dermatological applications.

 

  • References

  • 1 Sirtori CR. Aescin: pharmacology, pharmacokinetics and therapeutic profile. Pharmacol Res, 44 (03) , 183-193 2001;
    CrossrefPubMedGoogle Scholar
  • 2 Imanshahidi M, & Hosseinzadeh H. Pharmacological and therapeutic effects of Berberis vulgaris and its active constituent, berberine. Phytotherapy res 2008; 22 (08) : 999-1012
    CrossrefPubMedGoogle Scholar