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Int J Pharm. 2014 Aug 25;471(1-2):173-81. doi: 10.1016/j.ijpharm.2014.05.026. Epub 2014 May 22.

Phyto-liposomes as nanoshuttles for water-insoluble silybin-phospholipid complex.

Author information

1
Department of Agricultural, Environmental and Food Sciences (DIAAA), University of Molise, via De Sanctis, Campobasso I-86100, Italy; Consorzio per lo sviluppo dei Sistemi a Grande Interfase (CSGI), Florence, Italy. Electronic address: angelico@unimol.it.
2
Department of Agricultural, Environmental and Food Sciences (DIAAA), University of Molise, via De Sanctis, Campobasso I-86100, Italy; Consorzio per lo sviluppo dei Sistemi a Grande Interfase (CSGI), Florence, Italy.
3
Department of Life Sciences, University of Trieste, Trieste, TS I-34127, Italy.
4
Department of Chemistry, University of Bari and CSGI, via Orabona 4, Bari 70126, Italy; Consorzio per lo sviluppo dei Sistemi a Grande Interfase (CSGI), Florence, Italy.
5
Liver Unit, I.R.C.C.S. Casa Sollievo della Sofferenza Hospital, San Giovanni Rotondo, FG, Italy.

Abstract

Among various phospholipid-mediated drug delivery systems (DDS) suitable for topic and oral administration, phytosome technology represents an advanced innovation, widely used to incorporate standardized bioactive polyphenolic phytoconstituents into phospholipid molecular complexes. In order to extend their potential therapeutic efficiency also to other routes of administration, we proposed a novel phytosome carrier-mediated vesicular system (phyto-liposome) as DDS for the flavonolignan silybin (SIL), a natural compound with multiple biological activities related to its hepatoprotective, anticancer and antioxidant (radical scavenging) effects. We screened the optimum fraction of its phytosome, available in the market as Siliphos™, into liposomes prepared by extrusion, such that vesicle sizes and charges, monitored through dynamic light scattering and laser doppler velocimetry, satisfied several quality requirements. Special emphasis was placed on the study of host-guest interaction by performing UV-vis absorption, spectrofluorimetry and NMR experiments both in aqueous and non-polar solvents to probe the effect of the presence of phospholipids on the electronic properties of SIL and its propensity to engage H bonding with the lipid headpolar groups. Finally, fluorescence microscopy observations confirmed the ability of phyto-liposomes to be internalized in human hepatoma cells, which was promising for their potential application in the treatment of acute or chronic liver diseases.

KEYWORDS:

Physicochemical properties; Phyto-liposome; Phytosome; Silybin; Silybin–phospholipids interactions

PMID:
24858381
DOI:
10.1016/j.ijpharm.2014.05.026
[Indexed for MEDLINE]

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