Development and evaluation of self-microemulsifying liquid and pellet formulations of curcumin, and absorption studies in rats.

This study describes the development and characterization of self-microemulsifying drug delivery systems (SMEDDS) in liquid and pellet forms that result in improved solubility, dissolution, and in vivo oral absorption of the poorly water-soluble compound curcumin. Solubility of curcumin was determined in various vehicles, including oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were constructed to identify the most efficient self-emulsification region. The optimized SMEDDS used for curcumin formulations in liquid and pellet forms 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 curcumin-SMEDDS in liquid and pellet formulations rapidly formed fine oil-in-water microemulsions, with particle size ranges of 25.8-28.8 nm and 29.6-32.8 nm, respectively. The in vitro rate and extent of release of curcumin from liquid SMEDDS and SMEDDS pellets was about 16-fold higher than that of unformulated curcumin. Plasma concentration-time profiles from pharmacokinetic studies in rats dosed with liquid and pelleted SMEDDS showed 14- and 10-fold increased absorption of curcumin, respectively, compared to the aqueous suspensions of curcumin. Curcumin-SMEDDS liquid and curcumin-SMEDDS pellets were found to be stable up to 6 months under intermediate and accelerated conditions. These studies demonstrate that the new self-microemulsifying systems in liquid and pellet forms are promising strategies for the formulation of poorly soluble lipophilic compounds with low oral bioavailability.

Setthacheewakul S ，Mahattanadul S ，Phadoongsombut N ，Pichayakorn W ，Wiwattanapatapee R ... -  《-》

Enhancement of oral absorption of curcumin by self-microemulsifying drug delivery systems.

Cui J ，Yu B ，Zhao Y ，Zhu W ，Li H ，Lou H ，Zhai G ... -  《-》

Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs.

Kang BK ，Lee JS ，Chon SK ，Jeong SY ，Yuk SH ，Khang G ，Lee HB ，Cho SH ... -  《INTERNATIONAL JOURNAL OF PHARMACEUTICS》

Enhanced oral bioavailability of tacrolimus in rats by self-microemulsifying drug delivery systems.

Wang Y ，Sun J ，Zhang T ，Liu H ，He F ，He Z ... -  《-》

Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability.

Wu X ，Xu J ，Huang X ，Wen C ... -  《-》