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Planta Med 2018; 84(12/13): 976-984
DOI: 10.1055/a-0611-6203
Formulation and Delivery Systems of Natural Products
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Enhanced Solubility and Permeability of Salicis cortex Extract by Formulating as a Microemulsion[*]

Vieri Piazzini
1   Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Elisabetta Bigagli
2   NEUROFARBA, Department of Neurosciences, Psychology, Drug Research and Child Health, Section of Pharmacology and Toxicology, University of Florence, Florence, Italy
,
Cristina Luceri
2   NEUROFARBA, Department of Neurosciences, Psychology, Drug Research and Child Health, Section of Pharmacology and Toxicology, University of Florence, Florence, Italy
,
Anna Rita Bilia
1   Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Maria Camilla Bergonzi
1   Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
› Author Affiliations
Further Information

Publication History

received 08 January 2018
revised 29 March 2018

accepted 13 April 2018

Publication Date:
24 April 2018 (online)

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Abstract

A microemulsion system was developed and investigated as a novel oral formulation to increase the solubility and absorption of Salicis cortex extract. This extract possesses many pharmacological activities, in particular, it is beneficial for back pain and osteoarthritic and rheumatic complaints. In this work, after qualitative and quantitative characterization of the extract and the validation of an HPLC/diode array detector analytical method, solubility studies were performed to choose the best components for microemulsion formulation. The optimized microemulsion consisted of 2.5 g of triacetin, as the oil phase, 2.5 g of Tween 20 as the surfactant, 2.5 g of labrasol as the cosurfactant, and 5 g of water. The microemulsion was visually checked, characterized by light scattering techniques and morphological observations. The developed formulation appeared transparent, the droplet size was around 40 nm, and the ζ-potential result was negative. The maximum loading content of Salicis cortex extract resulted in 40 mg/mL. Furthermore, storage stability studies and an in vitro digestion assay were performed. The advantages offered by microemulsion were evaluated in vitro using artificial membranes and cells, i.e., parallel artificial membrane permeability assay and a Caco-2 model. Both studies proved that the microemulsion was successful in enhancing the permeation of extract compounds, so it could be useful to ameliorate the bioefficacy of Salicis cortex.

Key words

icroemulsion - Salix species - Salicaceae - oral delivery - PAMPA - Caco-2 cells

* Dedicated to Professor Dr. Robert Verpoorte in recognition of his outstanding contribution to natural products research.


Supporting Information

    Retention time, UV data, and MS fragmentors of two naringenin derivatives are available as Supporting Information.

  • Supporting Information
 

  • References

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