Nanoemulsions of cancer chemopreventive agent benzyl isothiocyanate display enhanced solubility, dissolution, and permeability

Hussaini Syed Sha Qhattal, Shu Wang, Tri Salihima, Sanjay K. Srivastava, Xinli Liu

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

Abstract

Benzyl isothiocyanate (BITC), a compound found in cruciferous vegetables, is an effective chemopreventive agent. The objective of this study was to develop nanoemulsion formulations for the oral delivery of BITC. Optimized oil-in-water BITC nanoemulsions were prepared by a spontaneous self-nanoemulsification method and a homogenization-sonication method. Both nanoemulsions entrapped high amounts of BITC (15-17 mg/mL), with low polydispersity and good colloidal stability. The BITC nanoemulsions showed enhanced solubility and dissolution compared to pure BITC. These formulations markedly increased the apical to basolateral transport of BITC in Caco-2 cell monolayers. The apparent permeability values were 3.6 × 10 -6 cm/s for pure BITC and (1.1-1.3) × 10 -5 cm/s for BITC nanoemulsions. The nanoemulsions were easily taken up by human cancer cells A549 and SKOV-3 and inhibited tumor growth in vitro. This work shows for the first time that BITC can be formulated into nanoemulsions and may show promise in enhancing absorption and bioavailability.

Original languageEnglish
Pages (from-to)12396-12404
Number of pages9
JournalJournal of Agricultural and Food Chemistry
Volume59
Issue number23
DOIs
StatePublished - Dec 14 2011

Keywords

  • Benzyl isothiocyanate
  • Caco-2 permeability
  • chemoprevention
  • dissolution
  • nanoemulsion
  • self-nanoemulsifying drug delivery system

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