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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 Sep 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Salivary Physicochemical Characteristics in Relation to Oral Health Status Among Institutionalized Autistic Adolescents in Baghdad/Iraq
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Background: Autism spectrum disorder (ASD) is characterized by impairments in social interaction and communication, restricted patterns of behavior, and unusual sensory sensitivities. Saliva may provide an easily accessible sample for analysis. Some salivary constituents levels altered in adolescents with ASD including antioxidants . This study aimed to investigate salivary physicochemical characteristic in relation to oral health status among adolescent with ASD. Materials and methods: Two groups were included in this study: forty institutionalized autistic adolescents and forty apparently healthy school adolescents with age range (12-15 years old, only males) selected randomly from Baghdad. Each group subdivided into two groups according

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Publication Date
Thu Oct 01 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Ions release from fixed orthodontic appliance in two different mouthwashes
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Background: Metal ions can be released from metallic orthodontic appliances due to corrosion in the oral cavity; prophylactic mouthwashes may have an effect on ion release from orthodontic wires. Materials and Methods: Thirty six orthodontic sets of half maxillary fixed appliance with 2 types of arch wires SS and NiTi(Morelli) were constructed and immersed in 2 types of mouthwashes; Claradone (non-fluoridated) and Silver Care (fluoridated) for 28 days at 37°C, then the released Ni and Cr ionswere measured using atomic absorption spectrophotometer and compared statistically. Results: Ni ion release was higher from NiTi wire group than SS wire group for both mouthwashes and also was higher for Silver Care group than for Claradone group.

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Publication Date
Thu Oct 01 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of the cleaning efficiency of the isthmus using different rotary instrumentation techniques (In vitro study)
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Background: The aims of the study were to evaluate the unclean/clean root canal surface areas with a histopathological cross section view of the root canal and the isthmus and to evaluate the efficiency of instrumentation to the isthmus using different rotary instrumentation techniques. Materials and Methods:The mesial roots of thirty human mandibular molars were divided into six groups, each group was composed of five roots (10 root canals)which prepared and irrigated as: Group one A: Protaper system to size F2 and hypodermic syringe, Group one B: Protaper system to size F2 and endoactivator system, Group two A:Wave One small then primary file and hypodermic syringe, Group two B:Wave One small then primary file and endoactivator system, Gr

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Publication Date
Tue Jun 15 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Mutual Prodrugs of Secnidazole and Ciprofloxacin and study Their Physicochemical Properties
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  Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1

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Publication Date
Thu Oct 01 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Periodontal health status in relation to physicochemical characteristics of saliva among pre-menopausal and post-menopausal women in Baghdad city-Iraq
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Background: Menopause can bring oral health problems and also associated with significant adverse changes in the orofacial complex. After menopause, women become more susceptible to periodontal disease due to deficiency of estrogen hormone. Current study aimed to evaluate the periodontal health status in relation to salivary constituent including pH, flow rate and some elements (Magnesium, Calcium and inorganic phosphorus) of pre and post-menopause women. Materials and Methods: Periodontal health status of 52 women aged 48-50 years old (26 pre-menopause and 26 post-menopause) were examined including (gingival index, plaque index, calculus index, probing pocket depth and clinical attachment level). Salivary sample was collected for two women

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Publication Date
Wed Mar 18 2020
Journal Name
Baghdad Science Journal
In Vitro Bioremediation: A Development Process of Cadmium and Mercury Removal by Environmental Biotechnologies of UV-Mutated Escherichia coli K12 and Bacillus subtilis 168
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  1. coli K12 and B. subtilis 168 were investigated for their cadmium and mercury tolerance abilities. They were developed by UV mutagenesis technique to increase their tolerances either to cadmium or mercury, and their names then were designated depend on the name and concentration of metals. E. coli K12 Cd3R exhibited bioremediation amount of 6.5 mg Cd/g dry biomass cell. At the same time, its wild-type (E. coli K12 Cd3) was able to remove 5.2 mg Cd/g dry biomass cell in treatment of 17 mg Cd /L within 72 hours of incubation at 37 °C (pH=7) in vitro assays. The results show that E.coli K12 Hg 20 was able to remove 0.050 µg Hg/g dry biomass cell
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Publication Date
Mon Dec 11 2006
Journal Name
Iraqi Journal Of Laser
In vivo N2 Laser Effect on Lymphocyte Transformation Capacity and Phagocytosis Activity in Mice
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The objective of this in vivo study is to investigate the effects of 337.1 nm pulsed N2 laser on cellular immune response represented by lymphocyte transformation capacity and phagocytosis activity in laboratory animals. The samples include 60 adult male BALB/c mice, were divided into control group and experimental groups. The experimental groups were divided into two main groups according to the time period after N2 laser irradiation. Each group was divided into 9 subgroups which exposed to N2 laser radiation at different values of pulse repetition rates and exposure times. The results of immunological tests demonstrated that the exposure to 180 J/cm2 of N2 laser radiation induce adverse effect to cellular immune response. The results o

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Publication Date
Sat Jan 06 2018
Journal Name
International Journal Of Applied Pharmaceutics
PREPARATION, RELEASE, RHEOLOGY AND STABILITY OF PIROXICAM EMULGEL
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Objective: The purpose of this work was to develop and optimize the emulgel formulation of piroxicam with two types of gelling agent chitosan and xanthan gum. The release profiles of prepared formulas were investigated. In addition, the rheology and stability of the best formula were investigated.Methods: Emulsified piroxicam was prepared to use oleic acid, tween 80 and PG with a ratio (3:10:10). In xanthan based emulgel, the xanthan gum (1% and 1.5%) was spread as powder on emulsified piroxicam with stirring until emulgel was formed. In chitosan-based emgels, Chitosan gel was added to emulsified piroxicam and stirring until the Emulgel was constructed. Chitosan gels were prepared by incorporating different concentration, 2%, 3%, 6%

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Optimization of Oral Fast Dissolving Prochloperazine Maleate Tablets
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Prochloperazine maleate (PCM) is one of the most prescribed phenothiazine. The purpose of the present research was to develop fast dissolving tablets of PCM with β-cyclodextrin inclusion complex. Tablets prepared  by wet granulation with sublimation and by using  different superdisintegrants type [ low-hydroxypropylcellulose LH21 (L-HPC LH21), carboxymethylcellulose calcium (ECG505), crospovidone (CP)], and different type of subliming agents (urea and ammonium bicarbonate (AB)). Tablets evaluated for its % friability, disintegration time, wetting time, hardness, content uniformity, weight variation, in vitro dissolution studies. For further enhancement of disintegration and dissolution, PCM orodispersible tablet were formula

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Publication Date
Thu Oct 01 2026
Journal Name
Journal Of Baghdad College Of Dentistry
An Evaluation of Corrosion Pits in Esthetic Coated Stainless Steel Orthodontic Archwires in Dry and Wet Environment at Different Intervals (An In Vitro Study)
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Background: The demand for esthetic orthodontic appliances is increasing; so the esthetic orthodontic archwires were introduced. Among them, Teflon and Epoxy coated stainless steel archwires. The amount of force available from the archwire depends on the structural properties and susceptibility to corrosion. All metallic alloys are changed during immersion in artificial saliva, chlorhexidine mouthwash andtoothpaste, but their behaviors differ from one type to another. They corrode at different rates, which lead to decrease the amount of force applied to the teeth. This in vitro study was designed to evaluate the corrosion pits in stainless steel archwires coated with Teflon and with Epoxy in dry and after immersion in artificial saliva, chl

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