Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin

Abstract

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.

Alginate-Based Composite Sponges as Gastroretentive Carriers for Curcumin-Loaded Self-Microemulsifying Drug Delivery Systems

“…This finding confirmed that sponge preparation using lyophilization did not affect the emulsion droplet size, similar to other S-SMEDDS formulations as pellets [11], tablets [12], and other sponges [14]. …”

“…Dynamic light scattering measurements were obtained at a fixed angle of 90° and a temperature of 25 °C [12]. Triplicate samples were each analyzed for 1 min, and for each measurement ran, 12 sub-runs were performed.…”

“…Numerous drug delivery system designs have been investigated with the aim of improving the oral bioavailability of curcumin, including nanoparticles [ 9 ] and liposomes [ 10 ]. Self-microemulsifying drug delivery systems (SMEDDS) have been studied extensively for enhancing the oral bioavailability of highly lipophilic compounds, such as curcumin and tetrahydrocurcumin [ 11 , 12 , 13 , 14 ]. Self-microemulsifying drug delivery systems are typically produced in liquid form but are recognized as having several limitations, such as leakage from capsules and drug precipitation during storage, which reduces the effective dose contained within the microemulsion [ 15 ].…”

“…Self-microemulsifying drug delivery systems are typically produced in liquid form but are recognized as having several limitations, such as leakage from capsules and drug precipitation during storage, which reduces the effective dose contained within the microemulsion [ 15 ]. Solid SMEDDS (S-SMEDDS) have been developed to overcome the limitations of liquid formulations by combining SMEDDS with various pharmaceutical excipients to create solid dosage forms, such as tablets [ 12 ], pellets [ 11 ], powders [ 16 ], granules [ 17 ], beads [ 13 ], and microcapsules [ 18 ].…”

Preparation and in vitro-in vivo evaluation of acyclovir floating tablets

“…Similar result was obtained by Sermkaew, et al . (20) who studied floating tablets of tetrahydrocurcumin.…”