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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 Jul 12 2016
Journal Name
World Journal Of Experimental Biosciences
Effect of honey and sodium bicarbonate on formation inhibition and removal of Staphylococcus aureus and Klebsiella pneumoniae biofilm in vitro
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Publication Date
Wed Feb 01 2023
Journal Name
International Journal Of Hydrogen Energy
Improvement of bioenergy generation using innovative application of food waste materials for coating carbon nanotubes-loaded bioanode in 3D-microbial fuel cells
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Publication Date
Thu Nov 17 2022
Journal Name
مجلة الدراسات الدولية
Iraq's strategic performance in achieving sustainable development after 2005: challenges and coping strategies
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The research discusses the obstacles that faced the Iraqi strategic performance in achieving sustainable development after the election of the first Iraqi government in 2005 and the most important strategies to overcome these obstacles.

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Publication Date
Tue Dec 09 2025
Journal Name
Hammurabi Journal For Studies
Technological Development and Water Resource Governance in Iraq: Strategies for Confronting Climate Change
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يواجه العراق تحديات مائية خطيرة نتيجة التغيرات المناخية، مثل انخفاض معدلات هطول الأمطار، ارتفاع درجات الحرارة، وزيادة معدلات الجفاف والتصحر، فهذه التحديات تتطلب إستراتيجيات فعالة لإدارة الموارد المائية بشكل مستدام، وهو ما يمكن تحقيقه من خلال تبني التطورات التكنولوجية الحديثة في مجال الحوكمة البيئية ، و يركز هذا البحث على دور التحول الرقمي والتقنيات الذكية في تعزيز كفاءة إدارة المياه، إذ يمكن لتطبيقا

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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of The Mechanical Behavior Of Materials
Concrete strength development by using magnetized water in normal and self-compacted concrete
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Abstract<p>The main objective of this work was to adopt an environmentally friendly technology with enhanced results. The technology of magnetic water (MW) treatment system can be used in concrete mixture production instead of potable water (PW) to improve both workability and strength. Two types of concrete were adopted: normal concreter production with two grades 25 and 35 MPa and the self-compacted concrete (SCC) with 35 MPa grade. The concrete mixes containing MW instead of PW results showed that, for 25 MPa grade, an improvement in a compressive strength of 15.1, 14.8, and 10.2% was achieved for 7, 28, and 90 days, respectively. For 35 MPa grade, an improvement of 13.6, 11.5, and </p> ... Show More
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Publication Date
Sat Jan 01 2022
Journal Name
Journal Of The Mechanical Behavior Of Materials
Concrete strength development by using magnetized water in normal and self-compacted concrete
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Abstract<p>The main objective of this work was to adopt an environmentally friendly technology with enhanced results. The technology of magnetic water (MW) treatment system can be used in concrete mixture production instead of potable water (PW) to improve both workability and strength. Two types of concrete were adopted: normal concreter production with two grades 25 and 35 MPa and the self-compacted concrete (SCC) with 35 MPa grade. The concrete mixes containing MW instead of PW results showed that, for 25 MPa grade, an improvement in a compressive strength of 15.1, 14.8, and 10.2% was achieved for 7, 28, and 90 days, respectively. For 35 MPa grade, an improvement of 13.6, 11.5, and </p> ... Show More
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Publication Date
Wed Jul 24 2024
Journal Name
Annals Of Parasitology
In vitro efficacy of different concentrations of lupeol on old world Leishmania donovani
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Leishmaniosis is a tropical neglected parasitic disease that is endemic in many countries, including Middle East, with no existing effective vaccines. The bite of female sand-fly transmits the causative agent, Leishmania spp., to humans. High toxicity, resistance and treatment failure of the available chemotherapy against visceral leishmaniosis demands the investigation of new anti-leishmanial compounds. Lupeol is a form of triterpene isolated from several medicinal plants and possesses an antimicrobial property. In this study, cytotoxic effect of lupeol was screened against the mammalian amastigotes form and insect promastigote form of Leishmania donovani, following three cycles of incubation at different concentrations by MTT assay. Resul

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Publication Date
Sat Jan 01 2011
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of the accuracy of a fifth generation apex locator (in vitro study)
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Background: The use of electronic apex locators for working length determination eliminates many of the problems associated with the radiographic measurements (interference of anatomical structures, errors in projection such as elongation or shortening, and lack of three-dimensional representation). Its most important advantage over radiography is that it measures the length of the root canal to the apical constriction, not to the radiographic apex. The aim of this study was to assess the accuracy of a new fifth generation apex locator (Joypex 5) in recording the apical constriction and comparing it with a third generation apex locator (Root ZX) in vitro. Materials and method: Twenty four single-rooted sound human premolars, extracted for t

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Publication Date
Wed Jun 01 2022
Journal Name
International Journal Of Early Childhood Special Education (int-jecs)
Building a comprehensive quality scale school sports activities from the standpoint of physical education teachers in the directorates of education in the Governorate of Baghdad
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The purpose of this paper is to building a comprehensive quality scale for school sports activities from the standpoint of physical education teachers in the directorates of education in the Governorate of Baghdad. The researchers used the descriptive approach with the survey method because it is the most appropriate to the nature of the problem and to achieve the objectives of the research .The good selection of the sample will reduce sampling errors, which enhances the honesty and accuracy of the data, which is representative of the research community and is always linked to its representation of the community and the possibility of generalizing its results to the group from which it was taken, as it represents the research community with

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Publication Date
Wed Oct 14 2026
Journal Name
Journal Of Baghdad College Of Dentistry
A Comparison between the Horizontal Condylar and Bennett Angles of Iraqi Full Mouth Rehabilitation Patients by Using Two Different Articulator Systems (An In-Vivo Study)
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Background: Errors of horizontal condylar inclinations and Bennett angles had largely affected the articulation of teeth and the pathways of cusps. The aim of this study was to estimate and compare between the horizontal condylar (protrusive) angles and Bennett angles of full mouth rehabilitation patients using two different articulator systems. Materials and Methods: Protrusive angles and Bennett angles of 50 adult males and females Iraqi TMD-free full mouth rehabilitation patients were estimated by using two different articulator systems. Arbitrary hinge axis location followed by protrusive angles and Bennett angles, estimation was done by a semiadjustable articulator system. A fully adjustable articulator system was utilized to locate th

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