Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Formulation Development

Background:

• Self-emulsifying drug delivery systems (SEDDS) improve oral bioavailability of poorly water-soluble drugs.
• Solid SEDDS (s-SEDDS) offer enhanced drug stability, ease of administration, and production.
• Traditional s-SEDDS often use solid excipients and high surfactant concentrations.

Purpose of the Study:

• To develop a novel solid self-emulsifying drug delivery system (s-SEDDS) using a tocotrienol-rich fraction (TRF) as the model liquid active substance.
• To evaluate the self-emulsification properties, powder flow, and emulsion characteristics of the developed s-SEDDS.
• To assess the in vivo oral bioavailability enhancement of the s-SEDDS compared to a liquid formulation.

Main Methods:

• A simple adsorption method was employed to create the s-SEDDS.
• Magnesium aluminosilicate was used as the carrier, with TRF (70%) and a blend of poloxamer and Labrasol® (30%) as surfactants.
• Particle size analysis, powder flowability tests, and in vivo pharmacokinetic studies in rats were conducted.

Main Results:

• The developed s-SEDDS exhibited excellent self-emulsification efficiency, forming stable emulsions with droplet sizes ranging from 210-277 nm.
• The formulation demonstrated good powder flowability.
• The s-SEDDS with combined surfactants showed a 3.4-3.8 times higher oral bioavailability in fasted rats compared to a non-self-emulsifying oily preparation.

Conclusions:

• A high-TRF content s-SEDDS was successfully developed using magnesium aluminosilicate and a surfactant blend.
• The s-SEDDS formulation offers improved oral bioavailability and the advantages of a solid dosage form.
• This approach provides a promising alternative for enhancing the delivery of poorly water-soluble drugs.