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Formulation and Characterization of Itraconazole as Nanosuspension Dosage Form for Enhancement of Solubility
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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

         

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Publication Date
Sat Nov 01 2025
Journal Name
Journal Of Molecular Liquids
Chitosan salt as a dual-function agent for CO₂ sequestration and acidizing enhancement
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The utilization of carbon dioxide (CO₂) to enhance wellbore injectivity presents a cost-effective and sustainable strategy for mitigating greenhouse gas emissions while improving reservoir performance. This study introduces an environmentally friendly method employing a water-soluble chitosan salt (CS) that generates a carbonated-rich acid solution upon contact with dry CO₂ at 25 °C and 508 psi. CS solutions (100–2000 ppm) were prepared and evaluated for CO₂ uptake, acid generation, and rheological behavior. Results show that 1000 ppm achieves an optimal CO2 uptake (2612 mg/l), with moderate viscosity increase (from 1.52 to 3.37 cp), while higher concentrations exhibit a sharp rise due to polymer-like network formation. Core floodi

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Publication Date
Thu Jan 04 2018
Journal Name
International Journal Of Applied Pharmaceutics
FORMULATION AND IN VITRO EVALUATION OF BROMOCRIPTINE MESYLATE AS FAST DISSOLVING ORAL FILM
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Objective: The aim of this study was to formulate and in vitro evaluate fast dissolving oral film of practically insoluble bromocriptine mesylate to enhance its solubility and to improve its oral bioavailability by avoiding first pass effect as well as to produce an immediate release action of the drug from the film for an efficient management of diabetes mellitus type II in addition to an improvement of the patient compliance to this patient- friendly dosage form. Methods: The films were prepared by the solvent casting method using hydroxypropyl methylcellulose of grades (E3, E5, E15), polyvinyl alcohol (PVA), pectin and gelatin as film-forming polymers in addition to polyethene glycol 400 (PEG400), propylene glycol (PG) and glycerin were

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Publication Date
Wed Feb 01 2023
Journal Name
Colloid Journal
Application of Hydrophilic Lipophilic Difference Theory for Fenofibrate Formulation as a Self-Emulsifying Drug Delivery System
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Improved oral bioavailability of lipophilic substances can be achieved using self-emulsifying drug delivery systems. However, because the properties of self-emulsifying are greatly influenced by surfactant amount and type, type of oil used, droplet size, charge, cosolvents, and physiological variables, the synthesis of self-emulsifying is highly complex; consequently, only a small number of excipient self-emulsifying formulations has been developed so far for clinical use. This study reports a highly effective procedure for developing self-emulsifying formulations using a novel approach based on the hydrophilic-lipophilic difference theory. Microemulsion characteristics, such as the constituents and amounts of oil and surfactant electrolyte

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
In vitro MIC of Itraconazole Against Different Isolates of Candida albicans
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In vitro antifungal susceptibility test of itraconazole was carried out against 38 isolates from nails, skin, oral cavity, vagina and wounds, This study was done in Ramadi Teaching Hospital in period from January to August 2010. According to the National Committee for Clinical Laboratory Standard (NCCLS ) M 27- A by using the broth dilution method. Inoculum size was 1-5X103 CFU/ ml, while final concentrations of itraconazole ranged from 0.025 – 6.4 μg / ml by using RPMI – 1640 broth media and the fungus was incubated at 35 oC.  No resistant stain was recorded. MIC ranged from 0.05 – 6.4 μg / ml and the Mean ± SEM was 0.89 ± 0.28. MIC for nail isolates was 0.05 –

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Publication Date
Thu Jan 01 2026
Journal Name
Opennano
Formulation and characterization of dolutegravir sodium-loaded nanostructured lipid carrier in situ gel for targeted brain delivery via intranasal route
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Publication Date
Mon Apr 10 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Domperidone Nanoemulsions for Oral Rout
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          The aim of the present study is to formulate, evaluate and characterize the nanoemulsion of Domperidone a poorly water-soluble anti-emetic drug.

           Domperidone powder is white or almost white powder, photosensitive, practically insoluble in water, slightly soluble in ethanol and in methanol; soluble in dimethylformamide. It is used as an antiemetic for the short-term treatment of nausea and vomiting of various etiologies.

           Solubility studies were conducted to select the oil, surfactant and cosurfactant. Phase diagrams were constructed by aqueous phase

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Publication Date
Mon Dec 25 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Evaluation of Ketoprofen Nanosuspension Using Solvent Evaporation Technique
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The effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen     is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen     nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of differ

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Publication Date
Sun Dec 27 2020
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Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Ondansetron HCl Nanoparticles for Transdermal Delivery
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Ondansetron HCl (OND) is a potent antiemetic drug used for control of nausea and vomiting associated with cancer chemotherapy. It exhibits only 60 – 70 % of oral bioavailability due to first pass metabolism and has a relative short half-life of 3-5 hours. Poor bioavailability not only leads to the frequent dosing but also shows very poor patient adherence. Hence, in the present study an approach has been made to develop OND nanoparticles using eudragit® RS100 and eudragit® RL100 polymer to control release of OND for transdermal delivery and to improve patient compliance.

Six formulas of OND nanoparticles were prepared using nanoprecipitation technique. The particles sizes and zeta potential were measured

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Publication Date
Wed Dec 01 2021
Journal Name
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Variation of pH and Composite Dosage on the Photocatalytic Activity for ZnO/epoxy Nanocomposites
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In this research, Zinc oxide (ZnO)/epoxy nanocomposite was synthesized by simple casting method with 2wt. % ZnO concentration. The aim of this work was to study the effect of pH and composite dosage on the photocatalytic activity of ZnO/ epoxy nanocomposite. Scanning electron microscopy (SEM) technique images proof the homogeneous distribution of ZnO nanoparticles in epoxy. A synthesized nanocomposite samples were characterized by Fourier Transform Infrared spectrometer (FTIR) measurements. Two spectra for epoxy and 2wt.% ZnO/epoxy nanocomposites were similar and there are no new bonds formed from the incorporation of ZnO nanoparticles. Using HCl and NaOH were added to Methylene blue (MB) dye (5ppm) to gat pH values 3 and 8. The degradat

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Publication Date
Mon Dec 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Mass Transfer Enhancement Using Extensions as Turbulence Promoters
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Mass transfer was studied using a rotating cylinder electrode with different lengths of legs acting as turbulence promoters. Two types of rotating cylinder ,made of brass, were examined : an enhanced cylinder one, with four rectangular extensions 10 mm long, 10 mm wide, and 1mm thick, and an enhanced cylinder two with four longitudes 30 mm long,10 mm wide, and 1mm thick. The best performance was obtained for enhanced cylinder two at low rotation speeds while enhanced cylinder one was realized at high rotation speeds. The mass transfer enhancement as compared with a normal rotating cylinder electrode, devoid of promoters, is 53% or 58% higher. The enhancement percentage decreased as rotation speeds increased further, since, seemingly, ful

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