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Planta Med 2017; 83(14/15): 1184-1193
DOI: 10.1055/s-0043-110052
Pharmacokinetic Investigations
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Prediction of Permeation and Cellular Transport of Silybum marianum Extract Formulated in a Nanoemulsion by Using PAMPA and Caco-2 Cell Models[*]

Vieri Piazzini
1   Department of Chemistry, University of Florence, Sesto Fiorentino, Florence, Italy
,
Chiara Rosseti
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 26 January 2017
revised 12 April 2017

accepted 22 April 2017

Publication Date:
04 May 2017 (online)

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Abstract

The present study explores the potential of nanoemulsion, a lipid drug delivery system, to improve solubility and oral absorption of Silybum marianum extract. The optimized formulation contained 40 mg/mL of commercial extract (4 % w/w) and it was composed of 2.5 g labrasol (20 %) as the oil phase, 1.5 g cremophor EL as the surfactant, and 1 g labrafil as the cosurfactant (mixture surfactant/cosurfactant, 20 %).

The system was characterized by dynamic light scattering, transmission electron microscopy, and HPLC-DAD analyses in order to evaluate size, homogeneity, morphology, and encapsulation efficiency. Physical and chemical stabilities were assessed during 40 days at 4 °C and 3 months at 25 °C. Stability in simulated gastric fluid followed by simulated intestinal conditions was also considered.

In vitro permeation studies were performed to determine the suitability of the prepared nanoemulsion for oral delivery. Different models such as the parallel artificial membrane permeability assay and Caco-2 cell lines were applied.

The nanoemulsion showed a good solubilizing effect of the extract, with a pronounced action also on its permeability, in respect to a saturated aqueous solution. The Caco-2 test confirmed the parallel artificial membrane permeability assay results and they revealed the suitability of the prepared nanoemulsion for oral delivery.

Key words

Silybum marianum L. Gaertn. - Asteracee - nanoemulsion - solubility - PAMPA - Caco-2

* Dedicated to Professor Dr. Max Wichtl in recognition of his outstanding contribution to pharmacognosy research.


Supporting Information

    An HPLC profile of SM extract and TEM images of empty and extract loaded NE are available as Supporting Information.

  • Supporting Information
 

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