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

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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.

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ACKNOWLEDGEMENTS

Financial support was granted by the Thailand Research Fund under the Royal Golden Jubilee Ph.D. programme (PHD/0080/2551) and the Royal Thai Government through Prince of Songkla University (PHA540093S). We also wish to thank Dr. Brian Hodgson for assistance with the English.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand

    Namfa Sermkaew, Wichan Ketjinda & Ruedeekorn Wiwattanapatapee

  2. Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand

    Kamonthip Wiwattanawongsa

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  1. Namfa Sermkaew
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  2. Kamonthip Wiwattanawongsa
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  4. Ruedeekorn Wiwattanapatapee
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Correspondence to Ruedeekorn Wiwattanapatapee.

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Sermkaew, N., Wiwattanawongsa, K., Ketjinda, W. et al. Development, Characterization and Permeability Assessment Based on Caco-2 Monolayers of Self-Microemulsifying Floating Tablets of Tetrahydrocurcumin. AAPS PharmSciTech 14, 321–331 (2013). https://doi.org/10.1208/s12249-012-9912-2

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