Abstract
Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol®). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210–277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol®) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4–3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form.
Highlights
Accepted: 14 October 2021It is estimated that 70 to 90% of newly discovered drugs suffer from poor aqueous solubility [1,2]
Results from the present study show that silicate type of excipients were able to hold the highest amount of liquid
Comparing to other tocotrienol powder products, the present study showed that the adsorption method on a solid carrier could provide an alternative approach to obtain a solid tocotrienol powder
Summary
Accepted: 14 October 2021It is estimated that 70 to 90% of newly discovered drugs suffer from poor aqueous solubility [1,2]. An SEDDS is an isotropic mixture of oil and surfactant(s) that is able to produce fine dispersion upon aqueous dilution in the gastrointestinal tract, which is aided by the gentle agitation provided by the gut motility [4,5]. It has the attributes of emulsions in terms of enhancing oral drug bioavailability, with an improved physical stability as the aqueous phase is only introduced in the gastrointestinal tract upon ingestion [5]. Liquid formulations may have material compatibility issues, potential leakage problem, and migration of excipients into a capsule shell [10]
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