Preferred Language
Articles
/
7xc3kpIBVTCNdQwCSrdB
Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel
...Show More Authors
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.

Scopus Crossref
View Publication
Publication Date
Fri May 01 2020
Journal Name
Systematic Reviews In Pharmacy
Methotrexate effect on obestatin, progranulin and kidney function in RA Iraqi males patients
...Show More Authors

Methotrxate (MTX) has become the standard of care and first-line therapy for patients who have RA and consider as a gold standard of treatment for RA. The role of MTX in the treatment of RA has now been well established. The use of MTX treatment of RA inhibits proliferation of the lymphocytes, reduces signs and symptoms this disease, reduces progression damage of the joints and improves quality of life outcome. Progranulin (PGRN) acts a role in autoimmune inflammatory, has important function in several processes including immune response. Present study has conducted to find the effect of MTX drugs as a therapeutic target for RA patients because of its ability to bind with tumor necrosis factor receptor (TNFR), with progranulin, obestatin an

... Show More
Scopus
Publication Date
Sun Oct 22 2023
Journal Name
مجلة الدراسات المستدامة
Strategies, Techniques and Activities Used by English Language Teachers in Employing Online Teaching
...Show More Authors

Publication Date
Fri Jul 21 2023
Journal Name
Journal Of Engineering
Cooling and Heating a Greenhouse in Baghdad by a Solar Assisted Desiccant System
...Show More Authors

Modeling the microclimate of a greenhouse located in Baghdad under its weather conditions to calculate the heating and cooling loads by computer simulation. Solar collectors with a V-corrugated absorber plate and an auxiliary heat source were used as a heating system. A rotary silica gel desiccant dehumidifier, a sensible heat exchanger, and an evaporative cooler were added to the collectors to form an open-cycle solar assisted desiccant cooling system. A dynamic model was adopted to predict the inside air and the soil surface temperatures of the greenhouse. These temperatures are used to predict the greenhouse heating and cooling loads through an energy balance method which takes into account the soil heat gain. This is not included in

... Show More
View Publication Preview PDF
Crossref (4)
Crossref
Publication Date
Fri Aug 19 2022
Journal Name
International Journal Of Health Sciences
Interleukin-32, interleukin-33 and acid phosphatase levels in patients with Helicobacter Pylori
...Show More Authors

The study was carried out to detection of H. pylori in (218) patients who attended two teaching hospitals in Baghdad. The diagnosis was done by Immunochromatography methods. Stools and blood samples were taken from each patient as well as other (30) healthy control matching in age. The study included measurement the Levels of Interleukin-32, Interleukin-33, and Acid phosphatase   in sera of patients and control .The result indicated  presence  of H pylori antigen in 115 cases 59 cases  of males and 51 of females , Also, the result indicated  increasing levels of IL-32 and IL-33 and Acid phosphatase  in patients sera  in comparison with healthy control.

View Publication
Crossref
Publication Date
Sun Jan 01 2017
Journal Name
Research Journal Of Pharmacy And Technology
Estimating the plain and negative tendonography techniques for evaluating injured tendon in rabbit
...Show More Authors

View Publication
Scopus (2)
Scopus Crossref
Publication Date
Thu Jun 01 2017
Journal Name
Applied Nursing Research
Examining perceived and actual diabetes knowledge among nurses working in a tertiary hospital
...Show More Authors

View Publication
Scopus (30)
Crossref (31)
Scopus Clarivate Crossref
Publication Date
Sun Mar 07 2010
Journal Name
Baghdad Science Journal
Free Fatty Acids and Biochemical Changes in Iraqi patients with Chronic Renal Failure
...Show More Authors

Chronic renal failure (CRF) is progressive irreversible destruction of kidney tissue by disease which, if not treated by dialysis or transplant, will result in patient's death. This study was carried out on 30 patients (17 male and 13 female) with chronic renal failure. The aim of this research was studied the changes in the level of total protein ,albumin, calcium ,ionized calcium, phosphorous , iron ,ALP, LDH ,CK and FFA in patients with CRF before and after hemodialysis .The obtained results have been compared with 30 healthy subjects as control group (18male and 12 female). The results showed that there was significant increase in the level of calcium ,ionized calcium, phosphorous ,iron ,ALP,LDH,CK and FFA ,while there was a signifi

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Jan 01 2013
Journal Name
International Journal Of Contemporary Mathematical Sciences
Equivalent between the Criterion and the Three Open Set's Conditions in Disk-Cyclicity
...Show More Authors

A vector in a separable infinite dimensional Hilbert space is called disk-cyclic for bounded operator if the orbit α : 0, α∈;|∝| 1is dense in. The useful tool used to discover codisk-cyclic operation is called the disk-cyclic Criterion. In this paper we will show that some equivalent conditions of the

View Publication
Crossref
Publication Date
Sat Oct 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Suggestive Framework for Applying Performance and Programs Budget in Iraqi Government Units Environment
...Show More Authors

Abstract

This research  aims to reform the Iraqi public budget through going into the challenges the budget faces in applying item-line budget in its preparation, implementation and control; which encourage extravagance and waste instead of rationalizing expenditures. This  is shown in the data analysis of Federal public budget laws in Iraq for the years from 2005 till 2013; there was a continuous increase in the aggregate public expenditures in the public budget for the years previously mentioned, as the public expenditures growth has reached into the percent 284.71% in 2013. In addition the public budget for these years (2005-2013) is being prepared with planned deficit without confirming that

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Jan 01 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Fabrication and Characterization CdO: In/Si Photovoltaic Solar Cell Prepard By Thermal Evaporation
...Show More Authors