Lee, You Zhuan
(2020)
Formulation Of Solid Self-Emulsifying
Drug Delivery System Using Mixedtocotrienols
As The Model Drug.
PhD thesis, Perpustakaan Hamzah Sendut.
Abstract
The present study was conducted to develop and evaluate the formulation of a
solid self-emulsifying system for enhancing the oral bioavailability of a poorly
water-soluble liquid active compound, namely tocotrienols. A suitable solid carrier
with high liquid holding capacity was selected. Various properties of several solid
self-emulsifying formulations including emulsification efficiency, emulsion droplet
size, desorption and powder flow properties were investigated. A solid selfemulsifying
formulation with the desired properties was successfully developed,
using magnesium aluminosilicate (Neusilin US2) as the solid carrier, containing 65
to 70% TRF and 30 to 35% surfactants (poloxamer and Labrasol) with sodium lauryl
sulphate as wetting agent. The formulation showed good self-emulsification
efficiency with stable emulsion formed, demonstrated excellent powder flowability,
complete desorption of tocotrienols from carrier, and small emulsion droplet size of
210 to 303 nm. Subsequent in vivo studies using Sprague-Dawley rats showed that
the formulation with a combination of surfactants (poloxamer and Labrasol) had a
faster rate of absorption compared to using only single surfactant (either poloxamer
or Labrasol). In a following in vivo study, the solid self-emulsifying preparation with
combined surfactants (D4) showed enhanced oral bioavailability (3.4 to 3.8 times
higher) compared to the non self-emulsifying oily liquid preparation when
administered at fasted state in rats. The formulation which was in a dry powder form
was further developed into a hard gelatin capsule dosage form, containing 100 mg
tocotrienols in each capsule.
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