Abstract:
The present investigation was aimed to develop self-nanoemulsifying tablets (SNETs) as novel
nanosized solid oral dosage forms for Irbesartan (IRB). In the first part of the investigation,
IRB-loaded self-nanoemulsifying drug delivery systems (SNEDDS) were developed using
Capryol 90 – Cremophor RH40 – Transcutol P as three component (oil – surfactant –
cosurfactant) SNEDDS system. On the basis of ternary phase diagram IRB-loaded SNEDDS were
optimized by using Design of Experiments (DoE) and Principal component analysis (PCA) with
amount of oil and surfactant: cosurfactant ratio (Km) as factors. The optimized batch of IRBloaded SNEDDS comprised of 31.62% w/w of Capryol 90 as oil phase, 49.90% w/w Cremophor
RH40 as surfactant and 18.48% w/w of Transcutol P as cosurfactant exemplified a mean globule
size as 23.94 nm. Further, with an aim to provide enhanced patient compliance the optimized
batch of liquid SNEDDS was transformed into SNETs by liquisolid compaction technique. Solid
state characterization of IRB-loaded liquisolid mixtures revealed a decrease in the magnitude of
crystallinity of IRB. The results of in vitro drug release study of optimized batch of IRB-loaded
SNET illustrated a remarkable improvement in the dissolution rate as compared to marketed
tablets (Avapro 75). The results of in vivo pharmacokinetic study on Wister rats revealed 1.78-
fold enhancement in oral bioavailability for IRB-loaded SNETs against marketed tablets. The
present study proposed SNEDDS as one of the suitable approach for developing nanosized
solid oral dosage forms of poorly water soluble drugs like Irbesartan.
