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Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

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Abstract

The objectives of this study were to develop and evaluate a novel self-emulsifying floating drug delivery system (SEFDDS) that resulted in improved solubility, dissolution, and controlled release of the poorly water-soluble tetrahydrocurcumin (THC). The formulations of liquid self-emulsifying drug delivery system (SEDDS; mixtures of Labrasol, Cremophor EL, Capryol 90, Labrafac PG) were optimized by solubility assay and pseudo-ternary phase diagram analysis. The liquid SEDDS was mixed with adsorbent (silicon dioxide), glyceryl behenate, pregelatinized starch, sodium starch glycolate, and microcrystalline cellulose and transformed into pellets by the extrusion/spheronization technique. The resulting pellets with 22% liquid SEDDS had a uniform size and good self-emulsification property. The microemulsions in aqueous media of different self-emulsifying floating pellet formulations were in a particle size range of 25.9–32.5 nm. Use of different weight proportions of glyceryl behenate and sodium starch glycolate in pellet formulations had different effects on the floating abilities and in vitro drug release. The optimum formulation (F2) had a floating efficiency of 93% at 6 h and provided a controlled release of THC over an 8-h period. The release rate and extent of release of THC liquid SEDDS (80% within 2 h) and self-emulsifying floating pellet formulation (80% within 8 h) were significantly higher than that of unformulated THC (only 30% within 8 h). The pellet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. Controlled release from this novel SEFDDS can be a useful alternative for the strategic development of oral solid lipid-based formulations.

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Acknowledgments

Financial support was received from the Thailand Research Fund under the Royal Golden Jubilee Ph.D. program (PHD/0150/2549) and the Royal Thai Government through Prince of Songkla University. We also wish to thank Professor L.A. Damani and Dr. Brian Hobson for editing our manuscript.

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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

    Saipin Setthacheewakul, Wichan Kedjinda, Duangkhae Maneenuan & Ruedeekorn Wiwattanapatapee

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  1. Saipin Setthacheewakul
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  2. Wichan Kedjinda
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  3. Duangkhae Maneenuan
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  4. Ruedeekorn Wiwattanapatapee
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Correspondence to Ruedeekorn Wiwattanapatapee.

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Setthacheewakul, S., Kedjinda, W., Maneenuan, D. et al. Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS). AAPS PharmSciTech 12, 152–164 (2011). https://doi.org/10.1208/s12249-010-9568-8

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