Background:
Irbesartan is an anti-hypertensive BCS class II drug exhibiting poor aqueous
solubility, which makes it highly challenging for delivery through the oral route. Based on this fact, a
self-microemulsifying drug delivery system (SMEDDS) was designed and characterized for augmenting
the aqueous solubility and dissolution rate of irbesartan.
Methods:
Several blends of oil (Capmul MCM EP), surfactant (Tween 80) and co-surfactant (PEG 600)
were screened from the preliminary solubility and pseudo-ternary phase diagram studies. Systematic optimization
of the SMEDDS was carried out using 3-factor 3-level Box-Behnken design.
Results:
The optimized formulation was identified by numerical optimization technique, which revealed
faster emulsification time, high percent transmittance and drug content, lower globule size < 100 nm,
zeta potential and excellent thermodynamic stability. The optimal formulation unveiled more than
93.3% drug release in vitro within 60 minutes, while the pure drug exhibited only 20% drug release, respectively.
Conclusion:
Ex vivo permeability and in situ intestinal absorption of drugs was improved nearly 2 to 3-
fold by the optimal SMEDDS formulation against the pure drug alone (p < 0.001). Overall, the proposed
SMEDDS formulation of irbesartan exhibited a superior biopharmaceutical performance.
Researchers are facing challenges to develop robust formulation and to enhance the bioavailability of poorly water-soluble drugs towards clinical applications. The development of new drug molecule alone is not adequate to assure ample pharmacotherapy of various diseases. Considerable results obtained from in vitro studies are not supported by in vivo data due to inadequate plasma drug concentrations. This may occur due to limited drug solubility and absorption. To resolve these problems, development of new drug delivery systems will be a promising approach. One of the promising pharmaceutical strategies is the use of lipospheres drug delivery system to deliver the poorly water-soluble drugs. Therefore, the present review described the methodology for manufacturing of lipospheres and factors influencing the formulation to deliver the drugs to the targeted site. Apart from that, this review also enlisted briefly the various applications of liposphers in medical and biomedical fields and critically discussed the recent patent system.
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