A novel lipid-based solid dispersion for enhancing oral bioavailability of Lycopene - In vivo evaluation using a pig model

作者：Faisal Waleed; Ruane O' Hora Therese; O' Driscoll Caitriona M; Griffin Brendan T^*

来源：International Journal of Pharmaceutics, 2013, 453(2): 307-314.

DOI：10.1016/j.ijpharm.2013.06.027

• Lycopene bioavailability
• Lipid-based formulation
• SEDDS
• Solid dispersions
• Gelucire 44/14
• Pig model

Lycopene is a potent anti-oxidant, which has been widely reported for its potential benefits at reducing the risks of certain types of cancer e.g. prostate cancer. The oral bioavailability of this highly lipophilic carotenoid is low and highly influenced by the extent of intestinal lymphatic uptake. The aim of this study was to develop an optimised formulation, which allows for efficient absorption following oral administration. A self-emulsifying drug delivery system (SEDDS) and solid dispersion of Lycopene were developed initially. Subsequently, a novel lipid based solid dispersion (LBSD) was designed. Processing via a solid dispersion approach was found to alter the solid state characteristics of Lycopene, as determined by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The bioavailability of Lycopene was significantly increased after oral administration of LBSD to fasted pigs, relative to the commercial product (Lycovit (R)). A clear distinction in terms of C-max and AUC was observed between Lycovit and LBSD. In conclusion, a novel LBSD formulation was developed to enhance the oral bioavailability of the model lipophilic compound, Lycopene, by enhancing dissolution in the gastrointestinal tract and promoting intestinal lymphatic uptake utilising digestible lipid excipients.

• 出版日期2013-9-10