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Development of Lyophilized Ebastine-Loaded Novasome Tablets: Comprehensive Physicochemical Characterization and In Vitro/In Vivo Release Evaluation
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Introduction/Objective:

Ebastine, a second-generation H1 antihistamine, exhibits poor aqueous solubility and consequently low oral bioavailability, limiting its clinical therapeutic efficacy. Novasome is an advanced vesicular nanocarrier system that offers a promising approach to enhance the solubility and dissolution behavior of a poorly water solubility drug. Therefore, this study aimed to develop, optimize, and characterize ebastine-loaded novasomes and to compress them into tablets to enhance drug solubility, dissolution, and oral bioavailability.

Methods:

Ebastine-loaded novasomes were prepared and optimized, then converted into lyophilized tablets using a suitable cryoprotectant. The optimized formulation was characterized for Particle Size (PS), Polydispersity Index (PDI), Zeta Potential (ZP), and Entrapment Efficiency (EE). Solidstate properties were assessed via Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD), while drug-excipient compatibility was evaluated using Fourier-Transform Infrared Spectroscopy (FTIR). In-vitro release studies were performed under stimulated physiological conditions, and in-vivo pharmacokinetic evaluation was conducted in Wistar rats.

Results:

The selected ebastine-loaded novasome exhibited a mean particle size of 189.9nm, a polydispersity index of 0.31, and an entrapment efficiency of 86.19%. In-vitro release exceeded 90% over 12 hours, significantly surpassing the dissolution profile of pure ebastine. DSC and XRD analyses confirmed amorphization of the drug within the Novasomal matrix, while FTIR revealed no evidence of drug-excipient compatibility. In-vivo studies demonstrated a 493.88% increase in relative oral bioavailability compared to free drug suspension (p < 0.05).

Discussion:

The enhanced dissolution and bioavailability are attributable to drug amorphization, high surface area to volume ratio of the nanovesicles, and protective entrapment of ebastine within the bilayer structure, which together improved gastrointestinal solubilization and oral bioavailability.

Conclusion:

The lyophilized Ebastine-loaded novasome tablet constitutes a stable, effective, and pharmacokinetically superior oral dosage form, offering significant potential for enhance the oral bioavailability of poorly water-soluble drugs.

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Publication Date
Tue Mar 01 2016
Journal Name
Journal Of Pharmaceutical Sciences
Development and Evaluation of Biodegradable Particles Coloaded With Antigen and the Toll-Like Receptor Agonist, Pentaerythritol Lipid A, as a Cancer Vaccine
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Publication Date
Mon Jun 04 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Darifenacin Hydrobromide loaded nanostructured lipid carrier for oral administration
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Darifenacin hydrobromide is a selective ?3 receptor antimuscarinic drug and it is used in the management of urinary frequency, urgency, and incontinence in detrusor instability. It slightly soluble in water, undergoes extensive hepatic first-pass metabolism and has short elimination half-life (3–4 hours). Therefore, It has low bioavailability (15.4 % - 18.6 %). Darifenacin hydrobromide loaded NLCs were formulated by emulsification sonication using different ratios of solid lipid to liquid lipid, different types of surfactants, and different concentration of surfactants. Formula sixteen was considered as an optimized formula based on its particle size, PDI, zeta potential and entrapment efficiency. Formula sixteen subjected t

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Publication Date
Tue Dec 01 2020
Journal Name
Baghdad Science Journal
In Vitro Cytotoxicity Study of Pt Nanoparticles Decorated TiO2 Nanotube Array
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Titanium dioxide nanotubes were synthesized by anodizing Ti sheets in the ethylene glycol solution and were covered in Pt nanoparticles onto the surface of TiO2NTs using electrodeposition method from using five derivatives of Mannich base Pt complexes which have been used as precursor of platinum. The mean size, shape, elemental composition of the titanium dioxide nanotubes and platinum deposited on the template were evaluated by different techniques such as field emission scanning electron microscope (FE-SEM), transmission electron microscopy (TEM), X-ray diffraction pattern (XRD), and energy dispersive X-ray (EDX) technique. From all these analyses, the TiO2NTs prepared and Ptnanoparticles deposited on it were ide

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Publication Date
Thu Feb 01 2024
Journal Name
Journal Of Orthodontic Science
Antimicrobial behavior of nanocoated orthodontic micro-implants: An in vitro study
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OBJECTIVE:

The need to overcome the failure of orthodontic micro-implants which might reach to 30% has led to the development of different methods, one of which is nanoparticle deposition.

AIM OF STUDY:

To evaluate the anti-microbial efficiency of TiO2 and ZnO nanoparticles (NP) when used as a coating for orthodontic micro-implants.

METHODS:

Thirty titanium alloy micro-implants were used in the presented study. They were divided into three

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Publication Date
Tue Dec 01 2020
Journal Name
Baghdad Science Journal
In Vitro Cytotoxicity Study of Pt Nanoparticles Decorated TiO2 Nanotube Array
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Titanium dioxide nanotubes were synthesized by anodizing Ti sheets in the ethylene glycol solution and were covered in Pt nanoparticles onto the surface of TiO2NTs using electrodeposition method from using five derivatives of Mannich base Pt complexes which have been used as precursor of platinum. The mean size, shape, elemental composition of the titanium dioxide nanotubes and platinum deposited on the template were evaluated by different techniques such as field emission scanning electron microscope (FE-SEM), transmission electron microscopy (TEM), X-ray diffraction pattern (XRD), and energy dispersive X-ray (EDX) technique. From all these analyses, the TiO2NTs prepared and Ptnanoparticles deposited on it were identified. The diagnoses pr

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Publication Date
Sun Mar 02 2008
Journal Name
Baghdad Science Journal
In vitro antimicrobial activity of total sesquiterpene lactones and phenols isolated from some Iraqi plants
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The antimicrobial potency of the crude ethanolic extracts from different Iraqi plants were evaluated . Further more, total sesquiterpene lactones and phenolic compounds were isolated and their antimicrobial activity attempted. The results indicated that crude extracts have no activity except that of Callistemon lanceolatus. Also, the sesquiterpene lactones and phenolic compounds isolated from Callistemon lanceolatus were the most significant antimicrobial active constituents of the studied plants.

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Publication Date
Wed Aug 26 2020
Journal Name
Iraqi Journal Of Agricultural Sciences
EFFECT OF GAMMA RADIATION AND ETHYL METHANESULFONATE (EMS) ON POTATO SALT STRESS TOLERANCE IN VITRO
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An experiment was conducted in the Date Palm Research Units labs / College of Agricultural Engineering Sciences / University of Baghdad to assess the tolerance toward salinity stress in potato after two mutagens treatments in vitro. Potato cv. Arizona and Rivera nodal segments were irradiated with four dosages of gamma rays at 0, 10, 20, and 30 Gray and immersed in (EMS) with four concentrations included 0, 10, 20, and 30 mM. The survival rates after mutagenesis treatments were calculated and 449 lines were obtained. The lines were tested for salinity tolerance by growing in MS medium supplemented with four concentrations of NaCl at 0, 100, 150, and 200 mM and data were analyzed according to the CRD with 10 replicates and means were

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Publication Date
Thu Jun 01 2023
Journal Name
Baghdad Science Journal
Mesenchymal and stemness transdifferentiation via in-vitro infection of T24 cell line with Klebsiella pneumoniae
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Klebsiella pneumoniae has been found in the urinary tract of some bladder cancer patients. Bacterial presence within tumor tissue may affect the tumor-microenvironment and consequently influence cancer behavior, development, and treatment response. This study investigated mesenchymal and stemness transdifferentiation of bladder cancer cell line due to environmental stress of K. pneumoniae. Cultures of urothelial bladder cancer cell line (T24) were infected with K. pneumoniae with different multiplicity of infection (MOI) for two and four days. Transdifferentiation-associated features were morphologically assessed.

Moreover, transdifferentiation markers were estimated using Q-PCR and immunohistoc

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Publication Date
Tue Oct 13 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Quantitative assessment of Mutans Streptococci adhesion to coated and uncoated orthodontic archwires(In vitro study)
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Background: The development of orthodontic biomaterials that attract less biofilm has been a goal for decades. Adhesion and colonization of cariogenic streptococci are considered to play key roles in the development of enamel demineralization related to orthodontic materials. The aim of this study was to quantitatively evaluate the Mutans streptococci adhesion to coated orthodontic archwires (Epoxy and Teflon) and uncoated archwires (stainless steel and nickel-titanium) with respect to incubation time in the presence and absence of saliva. Material and Method: Six types of archwires stainless steel and nickel titanium with two type of coating (Epoxy, Teflon) were used in this study. Twelve specimens of each archwire were incubated in steri

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Publication Date
Sun Feb 01 2026
Journal Name
Journal Of The Iranian Chemical Society
Synthesis, spectroscopic characterization, thermodynamic studies, and anticancer, antioxidant evaluation of metal ion complexes derived from azo dye
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Synthesis of new Fe+3, Co+2, Cu+2, Ru+3, and Rh+3 complexes of azo ligand; [5-((2-(3 H-1 indol-3-yl) ethyl) diazenyl) quinolin-8-ol], of 1:2 (M: L) and characterized through various techniques. The complexes exhibited octahedral geometries. Thermogravimetric (TGA and DSC) analysis is utilized to study the thermal properties of various compounds and reveal the presence of coordinated water molecules in the complexes. The multi-stage thermal decomposition mechanisms, where the thermal breakdown is ended by the formation of metal oxide as the final stable residue. The antioxidant activity of the ligand and its metal complexes was evaluated using the DPPH free radical scavenging assay and Gallic acid as a standard substance. Among the tested co

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