Preparation and Optimization of Esomeprazole Nanosuspension using Evaporative Precipitation– Ultrasonication|
Agarwal, Vijay & Bajpai, Meenakshi
Purpose: To prepare and optimize esomeprazole nanosuspension to enhance drug dissolution rate.
Methods: Esomeprazole nanosuspensions were prepared by evaporative precipitation-ultrasonication
method using F68 (Poloxamer 188) and F127 (Poloxamer 407) as stabilizers. Formulation and process
variables (concentration of stabilizers and drug, power input and duration of ultrasonication) affecting
the characteristics of nanosuspensions were optimized. The nanosuspensions were characterized for
particle size, shape, zeta potential, stability and in vitro drug release study.
Results: For optimization of esomeprazole nanosuspension, the effect of some important parameters,
including concentration of F68, concentration of esomeprazole, precipitation temperature, duration of
ultrasonication and power input, on particle size were investigated, and the optimal values were 0.4%
w/v, 3.5 mg/ml, 4°C, 20 min and 60% W, respectively. Particle size was in the range of 125 - 184 nm
with good zeta potential (15.9 - 25.5 mV). In vitro dissolution rate of esomeprazole was enhanced 4-fold
(100% in 60 min) compared with crude esomeprazole (24% in 60 min), and this was due to decrease in
particle size. The stability results indicate that nanoformulations stored at 4°C for two months showed
Conclusion: The results indicate the suitability of evaporative-precipitation-ultrasonication method for
preparation of nanosuspensions of poorly soluble drugs with improved in vitro dissolution rate, thus
potentially capable of enhancing fast onset of therapeutic activity, and bioavailability.
Agglomeration; Esomeprazole; Ultrasonification; Nanosuspension; Drug release; Solubility; Stability