Abstract
Objective: The objective of this study was to formulate and evaluate of the poorly soluble drug, azilsartan medoxomil into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspension of azilsartan medoxomil was prepared using solvent-antisolvent precipitation method using PVP-K30 as a stabilizer. Eight formulations were prepared to show the effect of different parameters in which four formulations show the effect of stabilizer concentration, three formulations show the effect of stirring speed and two formulations prepare to show the effect of the addition of co-stabilizer such as sodium lauryl sulphate (SLS) and tween 80. All these formulation are evaluated for their particle size and entrapment efficiency. The selected one was evaluated for zeta potential, scanning electron microscope (SEM), saturation solubility, and in vitro drug release.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: stabilizer ratio 1:1 and optimum stirring speed was 300 rpm. Dramatic effect on the particle size reduction was found by the addition of co-stabilizer (SLS) in formulation F3 that has P. S 157±0.0 nm. The selected formula F3 showed an enhanced dissolution profile compared to the pure drug at all-time intervals.Conclusion: The results show that the formulation that contain drug: PVP-K30: SLS in ratio 1:0.75:0.25 is the best one and can be utilized to formulate azilsartan medoxomil nanosuspension.
Highlights
Drug solubility refers to the maximum amount of solute dissolved in the solvent under the specific condition of temperature, pressure and pH
The constructed calibration curves of azilsartan medoxomil in methanol, water, HCl buffer pH 1.2 with 0.5% Tween80, and Phosphate buffer pH 6.8 are shown in fig
The poor solubility of azilsartan medoxomil that determined is in agreement with published researches as shown in table 2, the results shows that an increase in pH resulted in an increase in the solubility of azilsartan medoxomil as showing in the figure; this is because it is an acidic drug
Summary
Drug solubility refers to the maximum amount of solute dissolved in the solvent under the specific condition of temperature, pressure and pH. The water solubility of a drug plays an important role in the absorption of the drug after oral administration. It is useful in manipulating and testing of drug properties during the drug design and development process. It is critically important when the dissolution time is limited [2]. Some of the conventional approaches are micronization, use of penetration enhancer or co-solvents, surfactant dispersion method, salt formation, etc., but the major problems of these techniques are limited advantages in solubility enhancement for poorly soluble drugs. Toxicity and altered pharmacological activity are another disadvantages of the conventional strategies [3,4,5]
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