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Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel
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Background:

Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.

Objective:

This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.

Method:

Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.

Result:

The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p < 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one to be selected as the optimum formula.

Conclusion:

NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula that will be ready for further clinical study is NEIG 2.

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Publication Date
Sat Jan 24 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of in office bleaching on surface roughness and micro-hardness of newly developed composite materials (In vitro study)
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Background: Alterations in the microhardness and roughness are commonly used to analyze the possible negative effects of bleaching products on restorative materials. This in vitro study evaluated the effect of in-office bleaching (SDI pola office +) on the surface roughness and micro-hardness of four newly developed composite materials (Z350XT –nano-filled, Z250XT-nano-hybrid, Z250-mico-hybrid and Silorane-silorane based). Materials and methods: Eighty circular samples with A3 shading were prepared by using Teflon mold 2mm thickness and 10mm in diameter. 20 samples for each material, 10 samples for base line measurement (surface roughness by using portable profillometer, and micro-hardness by usingDigital Micro Vickers Hardness Test

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Preparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study
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Preparation and Identification of some new Pyrazolopyrin derivatives and their Polymerizations study

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Publication Date
Fri Apr 01 2016
Journal Name
Journal Of Engineering
Preparation and Study of morphological properties of ZnO nano Powder
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In this work, ZnO nanostructures for powder ZnO were synthesized by Hydrothermal Method. Size and shape of ZnO nanostructureas can be controlled by change ammonia concentration. In the preparation of ZnO nanostructure, zinc nitrate hexahydrate [Zn(NO3)2·6H2O] was used as a precursor. The structure and morphology of ZnO nanostructure have been characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), X-ray diffraction (XRD). The synthesized ZnO nanostructures have a hexagonal wurtzite structure. Also using Zeta potential and Particle Size Analyzers and size distribution of the ZnO powder

 

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Publication Date
Sun Dec 05 2010
Journal Name
Baghdad Science Journal
Propagation of Chickpea in vitro
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Apical meristems, lateral buds, anthers of immature flowers and immature embryos of chickpea ( Cicer arietinum L.) were cultured on MS media with different growth regulators and incubated for 6 weeks at 25-27?C with 16 hrs photoperiod for callus initiation. Results indicated that 1 and 0.1 mg/l of 2,4-D and BA were suitable for callus initiation when apical meristems and lateral buds were used. While 2 and 0.5 mg/l of both growth regulators were essential for immature embryos. It was noticed that using chickpea anthers of the MS medium must contain 1mg/l 2ip and 0.5 mg/l IAA. However, MS medium supplemented with 1-3 mg/l of BA and 2,4-D respectively was good for callus initiation from lateral buds, anther and immature embryos.

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Publication Date
Fri Jan 01 2016
Journal Name
International Journal Of Applied Pharmaceutics
Preparation of ferrous sulfate microcapsules as a sustained release dosage forms
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Publication Date
Mon Oct 01 2018
Journal Name
Iraqi Journal Of Physics
Preparation single layer of (MgO) as antireflection coating using PLD technique
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In this work preparation of antireflection coating with single layer of MgO using pulsed laser deposition (PLD) method which deposit on glass substrate with different thicknesses (90 and 100) nm annealed at temperature 500 K was done.
The optical and structural properties (X-ray diffraction) have been determined. The optical reflectance was computed with the aid of MATLAB over the visible and near infrared region. Results shows that the best result obtained for optical performance of AR'Cs at 700 shots with thickness 90 nm nanostructure single layer AR'Cs and low reflection at wavelength 550 nm.

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Publication Date
Fri May 01 2015
Journal Name
Journal Of Nuclear Medicine
Comparison of in vivo uptake of radioactive gold nanoparticles formulated using phytochemicals
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1267 Objectives Aim to evaluate 198Au nanoparticles (AuNP) biodistribution and uptake in a human prostate model for treatment. Many phytochemicals are known to have anti-tumor properties but have short half-lives in vivo. We hypothesized that using these phytochemicals to formulate and coat AuNP would inhibit enzyme cleavage and enhance their anti-tumor properties. Initial evaluations were performed in SCID mice bearing PC3 tumors. Methods : 198AuNP were formulated with the following gum Arabic, epigalocatechin gallate (EGCg) pomegranate extract and mangiferin extract. The resultant nanoparticles were evaluated in normal mice and in human prostate bearing SCID mice. The tumor bearing mice were injected intratumorally with 3-5 uCi of 198A

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Publication Date
Sun Dec 05 2010
Journal Name
Baghdad Science Journal
Effect of vincristine and vinblastine on mice spermatozoa in vitro
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The aim of this project was to study the in vitro effect of antineoplastic drugs (vincristine and vinblastine) on mice spermatozoa. Eighteen adult (age 8-9 weeks) male mice were divided into three groups equally. The animals in each group were slain by cervical dislocation, the testes were removed and two tails of epididymides isolated. Spermatozoa were obtained from the two tails of epididymides by mincing in 500 µl TCM-199.The first group non-treated (unadded) as a control group, second group added 10 µg/ml of vincristine to TCM-199 and the third group added 10 µg/ml of vinblastine to TCM-199. After 10 minutes from added of vincristine and vinblastin measured the following test: spermatozoa activity, percentage dead spermatozoa and mor

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Physiological and Immunological Assessment in Infertile Women Undergoing In-vitro Fertilization
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All the available reports on the issue of infertility confirmed the increase in this population problem worldwide. Although the accurate estimate of the number of infertile people is due to several reasons, including the discrepancy in the true definition of infertility (whether it extends for one, two or five years of failed pregnancy attempts), as well as the great discrepancy in the size of the selected population groups (large population sample size versus epidemiological studies) and defining the category that diagnosed included (individuals, women, or couples). The goal of today’s IVF program is to obtain high-quality embryos with high efficiency in development, which leads to an increase in live birth rates.

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Publication Date
Sun Dec 08 2019
Journal Name
Periodicals Of Engineering And Natural Sciences (pen)
Estimating total dissolved solids and total suspended solids in Mosul dam lake in situ and using remote sensing technique
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