Floating Alginate Beads as Carriers for Self-Emulsifying System Containing Tetrahydrocurcumin

摘要

Tetrahydrocurcumin (THC), one of the curcumin metabolites, exhibits pharmacological activities such as antioxidant, anti-inflammatory and anti-carcinogenic properties. However, the pharmacological effect of THC is limited due to its low aqueous solubility. Floating alginate beads containing self-emulsifying drug delivery system (SEDDS) of THC were developed to increase drug solubility and prolong gastric residence time. Use of different weight proportions of sodium alginate (Na-alg.), calcium chloride (CaCl_2) and water soluble pore former (Polyvinylalcoholpolyethylene glycol copolymer; Kollicoat IR) in bead formulations had different effects on the floating abilities and in vitro rate of THC release. The release profile of the optimized THC-SEDDS floating alginate beads (D3) indicated a significant increase in the dissolution rate of THC and provided a controlled release of THC over an 8 h period in a simulated gastric fluid. The release of about 80% of THC from the optimized beads as an o/w microemulsion with a particle size of less than 50 nm, compared to only 30% by an aqueous suspension from the unformulated THC could be considerable greater absorbed. The self-emulsifying floating alginate beads may provide a useful solid dosage form for oral delivery of THC and other hydrophobic compounds.