Planta Med 2018; 84(09/10): 736-742
DOI: 10.1055/a-0589-0474
Formulation and Delivery Systems of Natural Products
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Lipid Nanocarriers for Oral Delivery of Serenoa repens CO2 Extract: A Study of Microemulsion and Self-Microemulsifying Drug Delivery Systems

Clizia Guccione
Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Maria Camilla Bergonzi
Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Khaled M. Awada
Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Vieri Piazzini
Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
,
Anna Rita Bilia
Department of Chemistry, University of Florence, Sesto Fiorentino (Florence), Italy
› Author Affiliations
Further Information

Publication History

received 29 November 2017
revised 05 March 2018

accepted 06 March 2018

Publication Date:
15 March 2018 (online)

Abstract

The aim of this study was the development and characterization of lipid nanocarriers using food grade components for oral delivery of Serenoa repens CO2 extract, namely microemulsions (MEs) and self-microemulsifying drug delivery systems (SMEDDSs) to improve the oral absorption. A commercial blend (CB) containing 320 of S. repens CO2 extract plus the aqueous soluble extracts of nettle root and pineapple stem was formulated in two MEs and two SMEDDSs. The optimized ME loaded with the CB (CBM2) had a very low content of water (only 17.3%). The drug delivery systems were characterized by dynamic light scattering, transmission electron microscopy, and high-performance liquid chromatography (HPLC) with a diode-array detector analyses in order to evaluate the size, the homogeneity, the morphology, and the encapsulation efficiency. β-carotene was selected as marker for the quantitative HPLC analysis. Additionally, physical and chemical stabilities were acceptable during 3 wk at 4 °C. Stability of these nanocarriers in simulated stomach and intestinal conditions was proved. Finally, the improvement of oral absorption of S. repens was studied in vitro using parallel artificial membrane permeability assay. An enhancement of oral permeation was found in both CBM2 and CBS2 nanoformulations comparing with the CB and S. repens CO2 extract. The best performance was obtained by the CBM2 nanoformulation (~ 17%) predicting a 30 – 70% passive oral human absorption in vivo.

Supporting Information