Peer-Reviewed Journal Details
Mandatory Fields
Faisal, W;Ruane-O'Hora, T;O'Driscoll, CM;Griffin, BT
2013
September
International Journal of Pharmaceutics
A novel lipid-based solid dispersion for enhancing oral bioavailability of Lycopene - In vivo evaluation using a pig model
Validated
Optional Fields
INTESTINAL LYMPHATIC TRANSPORT DRUG-DELIVERY SYSTEMS PROSTATE-CANCER TOMATO PRODUCTS FORMULATIONS DOGS SOLUBILITY RELEASE RATS HALOFANTRINE
453
307
314
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. (C) 2013 Elsevier B.V. All rights reserved.
AMSTERDAM
0378-5173
10.1016/j.ijpharm.2013.06.027
Grant Details