title: Development, characterization and permeability assessment based on caco-2 monolayers of self-microemulsifying floating tablets of tetrahydrocurcumin.
abstract: Novel self-microemulsifying floating tablets were developed to enhance the dissolution and oral absorption of the poorly water-soluble tetrahydrocurcumin (THC). Their physicochemical properties and THC permeability across Caco-2 cell monolayers were assessed. The self-microemulsifying liquid containing THC was adsorbed onto colloidal silicon dioxide, mixed with HPMC, gas-generating agents (sodium bicarbonate and tartaric acid), lactose and silicified-microcrystalline cellulose and transformed into tablets by direct compression. The use of different types/concentrations of HPMC and sodium bicarbonate in tablet formulations had different effects on the floating characteristics and in vitro THC release. The optimum tablet formulation (F2) provided a short floating lag time (∼23 s) together with a prolonged buoyancy (>12 h). About 72% of THC was released in 12 h with an emulsion droplet size in aqueous media of 33.9±1.0 nm while that of a self-microemulsifying liquid was 29.9±0.3 nm. The tablet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. The THC released from the self-microemulsifying liquid and tablet formulations provided an approximately three- to fivefold greater permeability across the Caco-2 cell monolayers than the unformulated THC and indicated an enhanced absorption of THC by the formulations. The self-microemulsifying floating tablet could provide a dosage form with the potential to improve the oral bioavailability of THC and other hydrophobic compounds.
authors: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand.
authors: Namfa
authors: N
authors: Sermkaew
authors: Kamonthip
authors: K
authors: Wiwattanawongsa
authors: Wichan
authors: W
authors: Ketjinda
authors: Ruedeekorn
authors: R
authors: Wiwattanapatapee
mesh_terms: D018938:Caco-2 Cells; D002851:Chromatography, High Pressure Liquid; D003474:Curcumin / Q000031:analogs & derivatives* / Q000737:chemistry; D004655:Emulsions; D006801:Humans; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D010539:Permeability; D013607:Tablets
chemical_list: D004655:Emulsions; D013607:Tablets; C096277:tetrahydrocurcumin; D003474:Curcumin