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Development of self-microemulsifying liquid for oral delivery of tetrahydrocurcumin (THC)
Curcumin, extracted from the rhizomes of turmeric, has been reported to possess anti-oxidative, anti-inflammatory and anti-carcinogenic activities. Tetrahydrocurcumin (THC) is one of curcumin metabolites. THC exhibits similar pharmacological activities as curcumin; nevertheless, it shows the more potent antioxidant than curcumin [1, 2]. However, the pharmacological effect of THC is limited due to its low aqueous solubility. Self-microemulsifying drug delivery systems (SMEDDS) have been used for the improvement of oral bioavailability of insoluble lipophilic compounds. SMEDDS are isotropic mixtures of oils and surfactants that form fine oil-in-water microemulsions upon mild agitation in aqueous media such as GI fluids . The optimized SMEDDS used for THC formulations in liquid form contained 70% mixtures of two surfactants: Cremophor EL and Labrasol (1:1), and 30% mixtures of oil: Labrafac PG and Capryol 90 (1:1). The liquid THC-SMEDDS rapidly formed fine oil-in water-microemulsions, with particle size of less than 50nm. The in vitro rate and extend of release of THC from liquid-SMEDDS was about 16- fold higher than that of unformulated THC. Our studies demonstrated the potential use of self-microemulsifying drug delivery system for the delivery of hydrophobic compounds, such as THC by the oral route.
Acknowledgements: Financial support from Thailand Research Fund under the Royal Golden Jubilee Ph.D. programme (PHD/0150/2549) and the Royal Thai Government through Prince of Songkla University.
References: 1. Anand, P. et al. (2008) Molec. Pharm. 4:807–818.
2. Yoysungnoen, P. et al. (2008) World J. Gastroenterol. 14:2003–2009.
3. Constantinides P.P. (1997) Int. J. Pharm. 158:57–68.