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Original Research Article
Preparation and
Optimization of Esomeprazole Nanosuspension using
Evaporative Precipitation–Ultrasonication
Vijay Agarwal1,2*
and Meenakshi Bajpai3
1Department of Pharmacy,
NIMS University, Shobha Nagar, Delhi highway, Jaipur,
Rajasthan, 2College of Pharmaceutical
Sciences, Rajkumar Goel Instutute of Technology, Delhi
Meerut Road, Ghaziabad (U.P.), 3Department of
Pharmacy, Uttarakhand Technical University, Dehradun,
Uttarakhand, India
*For correspondence:
Email:
vagarwal5@rediffmail.com;
Tel.: +91 9891383464
Received: 4 April 2013
Revised accepted: 23
February 2014
Tropical
Journal of Pharmaceutical Research, April 2014;
13(4):
497-503
http://dx.doi.org/10.4314/tjpr.v13i4.2
Abstract
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, 4oC,
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 4oC
for two months showed maximum stability.
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.
Keywords: Agglomeration,
Esomeprazole, Ultrasonification, Nanosuspension, Drug
release, Solubility, Stability |
