Development of self-microemulsifying drug delivery system and solid-self-microemulsifying drug delivery system of telmisartan.

OBJECTIVE

Self-microemulsifying drug delivery system (SMEDDS) and solid-SMEDDS of telmisartan was aimed at overcoming the problems of poor solubility and bioavailability.

METHODOLOGY

The formulation strategy included selection of oil phase based on saturated solubility studies and surfactant and co-surfactant screening on the basis of their emulsification ability. Ternary phase diagrams were constructed to identify the self-emulsifying region using a dilution method. The prepared formulations of SMEDDS were evaluated for their drug content, loading efficiency, morphology, globule size determination. Solid-SMEDDS were prepared by adsorption technique using microcrystalline cellulose (1% w/w) and were evaluated for micromeritic properties, scanning electron microscopy, differential scanning calorimetry, X-ray diffraction.

RESULTS

The formulation containing telmisartan (20 mg), castor oil (30% w/w), tween 20 (55% w/w), propylene glycol (15% w/w) was concluded to be optimized. The optimized SMEDDS and solid-SMEDDS exhibited 100% in vitro drug release up to 120 min, which was significantly higher (P < 0.05, t-test) than that of the pure drug. Solid-SMEDDS may be considered as a better solid dosage form as solidified formulations are more ideal than liquid ones in terms of its stability.

CONCLUSION

These results suggest the potential use of SMEDDS and solid-SMEDDS to improve the dissolution and hence oral bioavailability of poorly water-soluble drugs like telmisartan through oral route.