Abstract:
Nanosuspension is an emerging and promising approach for the increasing solubility
and dissolution rate. The aim of this work was to develop Telmisartan nanosuspension
with a view to enhance its dissolution and saturated solubility. Telmisartan, a poorly
water soluble angiotensin receptor antagonist used as antihypertensive agent. Due to
less bioavailability which is only 43% of Telmisartan, an attempt was made to
develope and optimize nanosuspension formulation. Nanosuspension was prepared by
emulsification method. In FTIR studies, it was observed that there was no interaction
of drug and excipients in the final formulation. Various process and formulation
parameters were screened like stirring speed, type of stabilizer & surfactant,
concentration of stabilizer and surfactant. They were characterized for particle size,
zeta potential, dissolution study. Two different stabilizers and three different
surfactants were tried. Among them Poloxamer 188 & Tween 80 yielded
nanosuspension with particle size in range of 150 – 350 nm. As per the screening
study Poloxamer 188 & Tween 80 was selected for further study. Optimization of
concentration of Poloxamer 188 & Tween 80 was carried out using 32 full factorial
design. The optimized formula contained 3% Poloxamer 188 & 3% Tween 80.
Saturation solubility of optimized batch F8 showed 16 times higher than that of pure
drug. Moreover optimized batch F8 was found to be stable over a period of one month
at 40 ±2°C/75±5% RH as per ICH guideline. The outcome of this study revealed the immense potential of nanosuspension for delivery of Telmisartan by improving its
saturation solubility and enhancement of dissolution rate.
