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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
Wed Dec 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of Black Cardamom Extracts on Mutans Streptococci in Comparison to Chlorhexidine Gluconate and De-ionized Water (In Vitro Study)
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Background: Spices and herbs have been used by many cultures to enhance the flavor and aroma of food and for their medicinal value. Black cardamom is one of these spices widely used in cooking because of its unique taste and powerful flavor. The aim of study was to test the effect of black cardamom on Mutans Streptococci in comparison to chlorhexidine gluconate (0.2%) and de-ionized water. Materials and methods: Dried fruits of black cardamom were extracted by using alcohol (70% ethanol). Saliva was collected from seven volunteers. Agar well technique with different concentrations of black cardamom extracts was used to test the sensitivities of Mutans Streptococci, as well black cardamom extracts effect on viable counts of Mutans Streptococ

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Publication Date
Wed May 01 2019
Journal Name
Iraqi Journal Of Science
In Vitro Regeneration of Pimpinella anisum L. Using Different Plant Growth Regulators
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Plant regeneration protocols were developed for medicinally important anise (Pimpinella anisum L.) that successfully achieved from seeds. Seeds were sterilized and inoculated on Murashige and Skoog (MS) medium with and without gibberellins (GA3) until full germination. The highest percentage of germination (100%) was recorded on MS medium treated with 2.0 mg/L GA3 after 7 days. For shoot proliferation, different concentrations of 6- benzyl adenine BA (1, 1.5, 2 mg/L) were used. To enhance shoot induction, 0.1 mg/L of naphthalene acetic acid (NAA) and 0.01 mg/L of thidiazuron (TDZ) were tested along with BA. Direct regenerated shoots were obtained on MS medium supplemented with BA alone (2mg/L) which gave (7shoot/explant), while the presence

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Scopus
Publication Date
Mon Mar 02 2015
Journal Name
Journal Of Baghdad College Of Dentistry
Antibacterial Effects of Green Tea Extracts on Aggregatibacter Actinomycetemcomitans: In-Vitro Study
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Publication Date
Thu Oct 01 2015
Journal Name
Journal Of Dental And Medical Sciences
Antibacterial effects of green tea extracts on Prophyromonas Gingivalis (In-Vitro study)
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Publication Date
Thu Sep 01 2011
Journal Name
Journal Of Baghdad College Of Dentistry
Push out bond strength of different obturation systems (An in vitro study)
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Background: The bond strength of the root canal sealers to dentin seems to be a very important property for maintaining the integrity and the seal of root canal filling. The aim of this study was to evaluate the shear bond strength of four different obturation systems using push-out test. Materials and methods: Forty straight palatal roots of the maxillary first molars teeth were used in this study, these roots were instrumented using crown down technique and ProTaper system, instrumentation were done with copious irrigation of 2.5% sodium hypochlorite and 17% buffered solution of EDTA was used as final irrigant followed by distilled water, roots were randomly divided into four groups according to the obturation system (ten teeth for each g

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Publication Date
Thu Dec 01 2016
Journal Name
Journal Of Baghdad College Of Dentistry
In Vitro Comparative Assessment of Composite Nanoleakage Using Various Dentine Surface Treatments
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Background: The treatment of dental tissues proceeding to adhesive procedures is a crucial step in the bonding protocol and decides the clinical success ofrestorations. This study was conducted in vitro, with the aim of evaluating thenanoleakage on the interface between the adhesive system and the dentine treated by five surface modalities using scanning electron microscopy and energydispersiveX-ray spectrometry. Materials and methods: Twenty five extracted premolars teeth were selected in the study. Standardized class V cavities were prepared on the buccal and lingual surfaces then the teeth divided into five main groups of (5 teeth in each group n=10) according to the type of dentine surface treatment that was used: Group (A): dentine was

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Publication Date
Wed Oct 14 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Antibacterial effects of green tea extracts on Aggregatibacter actinomycetemcomitans (In-Vitro study)
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Background: Green Tea is made from the leaf of the plant “Camellia sinensis”. Green tea is reported to contain thousands of bioactive ingredients including catechins which have shown great promise for having antimicrobial effects. Periodontal diseases represent one of the most prevalent diseases around the world and the main etiologic factor behind it, is plaque accumulation, in addition certain kinds of bacteria have been detected frequently in subjects suffering from periodontitis, Several studies suggested that the outcome of periodontal treatment is better if particular pathogens including Aggregatibacteractinomycetemcomitans can no longer be detected after therapy. Materials and Methods: plaque samples were collected from 2

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Publication Date
Wed Dec 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
In Vitro Comparative Assessment of Composite Nanoleakage Using Various Dentine Surface Treatments
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Background: The treatment of dental tissues proceeding to adhesive procedures is a crucial step in the bonding protocol and decides the clinical success ofrestorations. This study was conducted in vitro, with the aim of evaluating thenanoleakage on the interface between the adhesive system and the dentine treated by five surface modalities using scanning electron microscopy and energydispersiveX-ray spectrometry. Materials and methods: Twenty five extracted premolars teeth were selected in the study. Standardized class V cavities were prepared on the buccal and lingual surfaces then the teeth divided into five main groups of (5 teeth in each group n=10) according to the type of dentine surface treatment that was used: Group (A): dentine was

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Publication Date
Wed Oct 14 2026
Journal Name
Journal Of Baghdad College Of Dentistry
An in-vitro scan electron microscope comparative study of dentine-Biodentine interface
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Background: Restoration of the gingival margin of Class II cavities with composite resin continues to be problematic, especially where no enamel exists for bonding to the gingival margin. The aim of study is to evaluate the marginal leakage at enamel and cementum margin of class II MOD cavities using amalgam restoration and modern composite restorations Filtek™ P90, Filtek™ Z250 XT (Nano Hybrid Universal Restorative) and SDR bulk fill with different restoratives techniques. Materials and method: Eighty sound maxillary first premolar teeth were collected and divided into two main groups, enamel group and cementum group (40 teeth) for each group. The enamel group was prepared with standardized Class II MOD cavity with gingival margin (1 m

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Publication Date
Mon Jan 01 2018
Journal Name
World Journal Of Dentistry
In vitro Remineralization of Caries-affected Dentin after Selective Carious Tissue Removal
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Scopus (14)
Scopus