Abstract
Abstract
 Itraconazole is a triazole antifungal given orally for the treatment of oropharyngeal and vulvovaginal candidiasis, for systemic infections including aspergillosis, candidiasis, and for the prophylaxis of fungal infections in immunocompromised patients.
 The study aimed to formulate a practical water-insoluble Itraconazole, with insufficient bioavailability as nanosuspension to increase aqueous solubility and improve its dissolution and oral bioavailability.
 Itraconazole nanosuspension was produced by a solvent-antisolvent nanoprecipitation method in the presence of different stabilisers (Poloxamer-188, HPMCE5) at different ratios with the drug alone or combination with surfactant(tween 80, SLS).
 The results exhibit that the particle sizes of all prepared itraconazole formulations were in the nano size. The best formula (F6) has a particle size. ( 42 ) nm and Zeta potential of (- 21.86 ) mV. In vitro cumulative release from the nanosuspension was (88 %) at (30) min when compared to the pure drug (13%) and lyophilized nanoparticles (98.2%) at (30)min. Effect of different parameters was investigated.
 Fourier transforms infrared spectroscopy(FTIR), Differential scanning calorimetry (DSC) and X-ray diffraction (XRD), Scanning electron microscope( SEM) was done for the optimized nanoparticles prepared by lyophilization technique
 Thus, Nanosuspension appears to be an encouraging approach to formulate Itraconazole nanosuspension with high solubility and dissolution rate.
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 Keywords: Itraconazole, Nanoprecipitation method, Nanosuspension
Highlights
Low bioavailability is one of the serious problems correlated with poorly soluble drugs
The objective of this study is to optimize and characterize the formulations prepared by the nanoprecipitation method for the preparation of ITZ nanosuspension
The mean particle size of various batches of nanosuspension prepared is depicted in table 2
Summary
Low bioavailability is one of the serious problems correlated with poorly soluble drugs. Various solubilization techniques have been used for the improvement of solubility and drug dissolution rates including a reduction of the particle size , by micronisation or Received: 27 / 5 /2019. Nanosuspension has shown to be a more cost-effective and technically simpler method. It can be defined as the dispersion of particles in the nanometer size range, where stabilization is accomplished by the addition of surfactants, stabilizer or a combination of both [2,3]. Nanosuspension consists of a poorly watersoluble drug without any matrix material suspended in dispersion resulting in the formulation having high dissolution velocity and increased saturation solubility [4]. It can be applied to several administration routes such as oral, parenteral, pulmonary, ophthalmic, and nasal routes [5]
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