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

Ruggero Angelico, Andrea Ceglie, Pasquale Sacco, Giuseppe Colafemmina, Maria Ripoli, Alessandra Mangia

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)173-181
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume471
Issue number1-2
DOIs
Publication statusPublished - Aug 25 2014

Keywords

  • Physicochemical properties
  • Phyto-liposome
  • Phytosome
  • Silybin
  • Silybin-phospholipids interactions

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Medicine(all)

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