期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 59, 期 23, 页码 12396-12404出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf202612b
关键词
benzyl isothiocyanate; chemoprevention; nanoemulsion; self-nanoemulsifying drug delivery system; dissolution; Caco-2 permeability
资金
- Texas Tech University Health Sciences Center (TTUHSC) School of Pharmacy
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 x 10(-6) cm/s for pure BITC and (1.1-1.3) x 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.
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