Abstract
Objective: This study was designed to prepare and characterize oil in water (o/w) nanoemulsion of candesartan cilexetil for oral administration. Preparation of candesartan cilexetil as nanoemulsion could increase its water solubility and thus could enhance its bioavailability.
 Methods: Aqueous titration method was used to construct the pseudo-ternary phase diagrams of nanoemulsion (NE) consisting of oil, various weight ratios of surfactant and co-surfactant (S mix), and deionized water. Different characterization techniques were conducted on the prepared nanoemulsions to obtain the optimized formula.
 Results: Characterizations of formula NE-4 (consists of 0.16% of candesartan cilexetil, 10% of garlic oil, 35 % of S mix (3:1) and 54.84% of deionized water) revealed the following characteristics: droplet size range (95-139 nm), polydispersity index (0.14), zeta potential value (-41.06 mV) and pH value (6.71), which are suitable for oral administration. Candesartan cilexetil in vitro release from this formula was significantly high (P<0.05) and scanning probe microscopy (SPM) study confirmed that the optimized formula (NE-4) was in nano-scale.
 Conclusion: Nanoemulsion formula 4 (NE-4) of candesartan cilexetil is the optimized formula and it could be a promising formula for improving the water solubility of candesartan cilaxetil.
Highlights
Oral conventional dosage forms are designed to provide a rapid onset via an immediate release of the active ingredient after administration
Based on permeability and water solubility, four classes of drugs are classified by Biopharmaceutics Classification System (BCS) into class I includes drugs with high permeability and high water solubility, class II includes drugs with high permeability and low water solubility, class III includes drugs that possess low permeability and high water solubility and class IV includes drugs with low permeability and low water solubility [2]
The melting point of candesartan cilexetil was found in the range of (171–172)
Summary
Oral conventional dosage forms are designed to provide a rapid onset via an immediate release of the active ingredient after administration. The desired therapeutic action, which can be achieved from these conventional drug delivery system, is based on the bioavailability of drugs. Enhancing water solubility of drugs belonging to class II using different techniques, such as self-emulsification, particle size reduction, and nanotechnology approaches, have the potential to improve absorption and enhance oral bioavailability of these drugs [3]. An example of these techniques is a nanoemulsion, which is a colloidal dispersion system consisting of oil, water, and surfactant and co-surfactant [4]. Examples of successful implementation of nanoemulsion in enhancing water solubility have been reported previously, which were; oral nanoemulsion of rosuvastatin, rifampicin, and pterostilbene [6,7,8]
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