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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
Fri Jun 16 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Assessment of Delayed/Slow-Release Diclofenac Sodium Edible Organogel Utilizing Low Molecular Weight Organogelators
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Organogel as a system was to estimate its capacity to delay and slow the drug release in the duodenum. The gelators, 12HSA (12-hydroxystearic acid), span 60. span 40 were used; the castor oil (CO) and anise oil (AO) also represented the liquid phase. To achieve the goal of this work was by using diclofenac sodium (DS). Organogels specifications were by estimating thermal attitude using tabletop rheology and differential scanning calorimetry (DSC). The organogel strength study was by applying oscillatory rheology tests the amplitude sweep and the frequency sweep. Realizing the morphology of the organogel was done utilizing an optical microscope. CO and AO binding capacity was also manifested. The transition temperatures for all organogels

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Publication Date
Wed Jul 01 2020
Journal Name
Journal Of Controlled Release
Breast intraductal nanoformulations for treating ductal carcinoma in situ I: Exploring metal-ion complexation to slow ciclopirox release, enhance mammary persistence and efficacy
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Publication Date
Tue Nov 12 2024
Journal Name
International Journal Of Social Science Humanity &amp; Management Research
Sustainable Development in Organization: A Literature Review
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The current study aimed to review previous scholarly efforts to understand the concept of sustainable development, its practices, and its significance for public institutions. The study focuses on the dimensions of sustainable development—environmental, social, and economic—within public institutions. Sustainable development allows these institutions to balance environmental protection, economic growth, and social justice, ensuring the prosperity of both current and future generations. Furthermore, sustainable development is crucial for maintaining organizational performance. The review bridges knowledge gaps related to sustainable development and utilizes an analytical approach, surveying previous studies on the topic. The sele

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Publication Date
Sun Feb 10 2019
Journal Name
Journal Of The College Of Education For Women
Education Development in Local Community Analysis Study
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Human resources are considered as strategic fortune for being the main driver of the development wheel in the society, and the field of education and learning is one of the main pillars of this fortune for its great effect in the process of economic and social progress of individuals. I was the subject of education to the concerns of many countries, as adopted national policies . And regional support and the reduction of constraints, so came our study (education hub for human development) to identify the role of education in human development and to identify the obstacles facing the education process and the extent of its impacts negatively on the process of human development also contribute to the knowledge of school enrollment and the

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
The political development in Moritania 1967-1934
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Publication Date
Fri Nov 30 2018
Journal Name
Iop Conference Series: Materials Science And Engineering
Stiffness to Weight Ratio of Various Mechanical and Thermal Loaded Hyper Composite Plate Structures
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In this study, several models of the rocket fins were made of hyper composite materials (with two or more reinforced materials) with different volume fractions of components used to produce isotropic composite plate structures. The reinforcement of polyester resin material was done in two ways, with fibre reinforcement and powder reinforcement. The types of fibresthat used were chopped glass fibre and chopped carbon fibre, and the type of powder used was carbon powder. A concentrated load was applied to the models in the form of a cantilever plate. The effect of adding carbon powder on the stiffness to weight ratio and the effect of temperature on this stiffness to weight ratio were studied and discussed. It was observed that hybridization

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Publication Date
Sun Nov 01 2020
Journal Name
Systematic Reviews In Pharmacy
Recent Development In Oxine Complexes And Their Medical Application: A Review.
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This review is concluded of 8-Hydroxyquinline (8HQ) compound and derivatives which has a very significant interests with a strong fluorescence , furthermore the relationship between divalent metal ions and characteristic of chelating . In the same way coordinated features have increase of its organic action and inorganic behavior by giving many samples of compounds which are a good chelating agents ligands with more capable of forming very stable complexes.Therefore, the role of (8HQ) is not limited on complexes only but its applications in different fields so this review will focus on demonstration preparation methods and properties of (8HQ) derivatives with their complexes and applications, hopefully that we will cover a part of scientifi

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Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
Educational Planning, it's Importance in the Social, Economical and Educational Development
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Educational Planning, it's Importance in the Social, Economical and Educational Development

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Publication Date
Sat Jun 01 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Investigate the effectiveness of investment in the electricity sector And its role in achieving sustainable development
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The provision of electric power is necessary for the advancement of the country's economy. It is the main engine of the economy and its various activities. It is an indicator of social welfare and it is considered as the basic pillars for achieving sustainable development (economic, social, environmental and institutional) by raising the levels of performance and meeting local needs. The problem of research was the absence of a program to audit the performance of the electricity sector contributes to ensure the application of sustainable development. The research was based on the hypothesis that the preparation of a proposed program to audit the performance of the electricity sector contributes to the achievement of The researchers sough

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Publication Date
Wed Jan 01 2020
Journal Name
Plant Archives
An analysis for adoption of subsurface irrigation technology and its role in agricultural development in Iraq
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