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
Highlights
Nanosuspension is the colloidal dispersion of solid drug particles in a liquid phase having particle size below 1μm [1,2]
In vitro release of ESP from different nanosuspension formulations were studied by dialysis method using a dialysis membrane of molecular weight cutoff of 12 KDa
Esomeprazole nanosuspension has been successfully prepared by evaporative precipitation – ultrasonication method
Summary
Nanosuspension is the colloidal dispersion of solid drug particles in a liquid phase having particle size below 1μm [1,2]. At present time about 40% of the drugs in the development pipelines and 60% of the drugs coming directly from synthesis are poorly soluble [3]. These poorly soluble drugs require some innovative formulation approaches by which they can reach up to a sufficiently high bioavailability. There are many formulation approaches used for poorly soluble drugs, nanosuspension is one of them. Preparation of drug in the form of nanosuspension was shown a technically simpler alternative, for poorly soluble drugs [4,5,6]. In nanoformulation it is necessary that the drug particles be rendered into nanosize domains, but they must be stabilized and formulated rigorously to retain the nature and properties of the nanoparticles [8]
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