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Abd-Elhady R.M.,National Organization for Drug Control and Research | Elsheikh A.M.,National Organization for Drug Control and Research | Khalifa A.E.,Ain Shams University
International Journal of Developmental Neuroscience | Year: 2013

Aluminum is the most widely used non-ferrous metal. However, recently it is reported to be a neurotoxic agent that could induce biochemical defects in brain by affecting levels of neurotransmitters and generating reactive oxygen species resulting in oxidative stress. This study aimed at evaluating neuroprotective effect of Ginkgo biloba extract. 22GBE: Ginkgo biloba extract. (GBE) (200. mg/kg for 28 days) in antagonizing aluminum-induced neurotoxicity through investigating certain parameters such as serum aluminum level, brain aluminum content, brain regional distribution of aluminum, brain oxidative stress biomarkers' content, and brain acetylcholinesterase. 33AchE: acetylcholinesterase. (AChE) activity. Passive avoidance paradigm was used to assess memory retrieval of rats. Rats' activities were studied using open field test. Results showed that administration of aluminum (10. mg/kg for 28 days) impaired rats' memory retrieval associated with marked elevation of aluminum brain content, serum aluminum level and AChE activity. In addition, aluminum treatment induced significant elevation in its brain content in all tested regions. GBE treatment attenuated neurotoxic effects of aluminum as evidenced by improving rats' performance in passive avoidance and lowering brain AChE activity. Moreover, marked elevation in brain content of oxidized glutathione. 44GSSG: oxidized glutathione. (GSSG) and malonedialdehyde. 55MDA: malonedialdehyde. (MDA) as well as depletion of reduced glutathione. 66GSH: reduced glutathione. (GSH) demonstrated following aluminum administration were reversed reaching normal levels after GBE treatment. Open field test, demonstrated no changes in latency period, number of ambulation, rearing, and grooming following aluminum or other treatments. Therefore, GBE may be a promising therapy ameliorating neurotoxicity of aluminum as an environmental toxic agent. © 2013 ISDN.


Ibrahim D.A.,National Organization for Drug Control and Research | Ismail N.S.M.,Ain Shams University
European Journal of Medicinal Chemistry | Year: 2011

The design and synthesis of a small library of 4-aminopyrido[2,3-d] pyrimidine derivatives is reported. The potential activity of these compounds as CDK2/Cyclin A, CDK4/Cyclin D, EGFR and anti-tumor was evaluated by cytotoxicity studies in A431a, SNU638b, HCT116 and inhibition of CDK2-Cyclin A, CDK4/Cyclin D and EGFR enzyme activity in vitro. The anti-proliferative and CDK2-Cyclin A inhibitory activity of compounds 4c and 11a was significantly more active than roscovotine with IC50 0.3 and 0.09 μM respectively. Molecular modeling study, including fitting to a 3D-pharmacophore model, docking into cyclin dependant kinase2 (CDK2) active site and binding energy calculations were carried out and these studies suggested the same binding orientation inside the CDK2 binding pocket for these analogs compared to ATP. © 2011 Elsevier Masson SAS. All rights reserved.


This work aimed to develop voriconazole in situ gelling ocular inserts loaded with niosomal suspension. Niosomes and mixed niosomes were prepared using span 40 and span 60 with pluronic L64 and pluronic F127. The entrapment efficiency percentages (EE%), mean vesicle size, polydispersity index (PI), zeta potential and in vitro drug release of these niosomes were evaluated. F3-mixed niosomes prepared with span 60 and pluronic L64 was selected, due to its highest EE; optimum vesicle size with smallest PdI and suitable release pattern of the drug (63% after 8 h). In situ ocular inserts were prepared using sodium carboxymethylcellulose (CMC Na) and sodium alginate (ALG) and characterised for surface morphology, surface pH, water uptake, mucoadhesion and in vitro release. ALG in situ ocular insert (S2) was selected for further in vivo evaluation of the ocular irritation and drug pharmacokinetics in the aqueous humour of rabbit's eyes. S2 in situ gelling ocular insert was non-irritant and showed significantly (p < 0.01) higher Cmax, delayed Tmax and increased bioavailability. © 2016 Taylor and Francis.


Ibrahim D.A.,National Organization for Drug Control and Research | El-Metwally A.M.,National Organization for Drug Control and Research
European Journal of Medicinal Chemistry | Year: 2010

Novel derivatives of 2,4,5,6-tetrasubstituted pyrimidine cyclin-dependent kinase (CDK2) inhibitors was designed and synthesized. We built a library of proposed pyrimidine derivatives and by using pharmacophore and docking techniques we made our selections. We modified the proposed compounds due to the interaction of docked structures with the protein to achieve the best fit. The newly synthesized compounds showed potent and selective CDK2 inhibitory activities and inhibited in-vitro cellular proliferation in cultured human tumor cells. The design, synthesis and biological evaluation of these 2,4,5,6-tetrasubstituted pyrimidine derivatives are reported. © 2009 Elsevier Masson SAS. All rights reserved.


Nesseem D.,National Organization for Drug Control and Research
International Journal of Cosmetic Science | Year: 2011

Synopsis Solid lipid nanoparticle (SLN) was regarded as new topical delivery systems for pharmaceutical and cosmetic active ingredients. The purpose of this study is to develop carrier systems for organic and inorganic sunscreens based on a matrix composed of carnauba wax and decyl oleate. Formulae (F1-F7) were prepared using butyl methoxydibenzoylmethane and octyl methoxycinnamate as organic components, and titanium dioxide (TiO2) was used as inorganic component. Both types of sunscreens were incorporated into SLN formulations using classical method of preparation. To evaluate the effect of the pigments on the nanoparticles, particle size was measured using Mastersizer particle size analyser. UV-protection abilities of formulations were investigated by the in vitro sun protection factor test (SPF). Further parameters determined were spreadability as well as viscosity. The rheological behaviour of the formulations was also carried out. From the plot of log of shear stress vs. log of shear rate, the slope of the plot representing flow index and ontology of the y-intercept indicating consistency index was calculated. The formulae showed a flow index of 0.2074-0.4005 indicating pseudoplastic flow behaviour. Significant increases in SPF values up to about 50 were reported after the encapsulation by using organic and inorganic filters in Canada wax and decyl oleate. So, SLN could be appropriate vehicles to carry organic and inorganic sunscreens. The rational combination of cinnamates, titanium dioxide and Zinc oxide has shown a synergistic effect to improve the SPF of cosmetic preparations. © 2010 The Author. Journal compilation.


Mabrouk M.I.,National Organization for Drug Control and Research
Journal of Applied Sciences Research | Year: 2012

Aqueous and ethanol extracts of fruits and leaves (1000 ppm) of six important medicinal plants species, Foeniculum vulgare (Apiaceae), Priminella anisum (Apiaceae), Carum carvi L. (Apiaceae), Majorana hortensis L. (Labiateae), Mentha longifolia (Labiateae) and Salvia officnalis (lamiaceae) has been tested individually and in combination for their antibacterial activity against total of 5 E. coli O157:H7 resistant isolates collected from human, cattle and food. Results showed higher antibacterial activity in combination of extracts of the medicinal plants studied. The aqueous extracts of Foeniculum vulgare and ethanolic extracts of Salvia officnalis showed 1.4 and 1.2 cm zone of inhibition (ZI), respectively against E. coli O157:H7 when tested individually. Whereas, the combination of aqueous extracts of Foeniculum vulgare + Priminella anisum+ Carum carvi L (1:1:1) showed 2.5 cm ZI against E. coli. Similarly, the highest antibacterial activity of 4.0 cm ZI was observed against E. coli O157:H7 collected from food in combination of aqueous extracts of plants. This study clearly demonstrates the synergistic activity of plant extracts against E. coli O157:H7.


El-Tantawy W.H.,National Organization for Drug Control and Research | Haleem E.N.A.A.,Al - Azhar University of Egypt
Molecular and Cellular Biochemistry | Year: 2014

Diabetes mellitus is the most common endocrine disorder that affects more than 285 million people worldwide. The purpose of this study was to investigate the effect of mesenchymal stem cells (MSCs) from the bone marrow of albino rats, on hyperglycemia, hyperlipidemia, and oxidative stress induced by intraperitoneal injection (i.p.) of alloxan at a dose of 150 mg/kg in rats. Injection of alloxan into rats resulted in a significant increase in serum glucose, total cholesterol, triglyceride, low density lipoprotein cholesterol, and sialic acid level and a significant decrease in serum insulin, high density lipoprotein-cholesterol, vitamin E, and liver glycogen as compared to their corresponding controls. Also, oxidative stress was noticed in pancreatic tissue as evidenced by a significant decrease in glutathione level, superoxide dismutase, glutathione-S-transferase activities, also a significant increase in malondialdehyde and nitric oxide levels when compared to control group. Treatment of diabetic rats with MSCs stem cells significantly prevented these alterations and attenuated alloxan-induced oxidative stress. In conclusion, rat bone marrow harbors cells that have the capacity to differentiate into functional insulin-producing cells capable of controlling hyperglycemia, hyperlipidemia, and oxidative stress in diabetic rats. This may be helpful in the prevention of diabetic complications associated with oxidative stress. © 2014 Springer Science+Business Media.


Herein, an electrochemical differential pulse voltammetric method was developed for the determination of moexipril hydrochloride based on the enhancement effect of sodium dodecyl sulfate. The oxidation process has been carried out in Britton-Robinson buffer. Moexipril hydrochloride exhibits a well-defined irreversible oxidation peak over the entire pH range (2-11). The peak current varied linearly over the range from 4.0 × 10-7 to 5.2 × 10-6 mol L-1. The limits of detection and quantification were 6.87 × 10-8 mol L-1 and 2.29 × 10-7 mol L-1, respectively. The recovery was found in the range from 99.65% to 100.76%. The relative standard deviation was found in the range from 0.429% to 0.845%. The proposed method possesses high sensitivity, accuracy and rapid response. Finally, this method was successfully used to determine moexipril hydrochloride in tablets. © 2009 Elsevier B.V. All rights reserved.


El-Houssini O.M.,National Organization for Drug Control and Research
Analytical Chemistry Insights | Year: 2013

Two simple, accurate and reproducible methods were developed and validated for the simultaneous determination of paracetamol (PARA) and pamabrom (PAMB) in pure form and in tablets. The first method was based on reserved-phase high-performance liquid chromatography, on a Thermo Hypersil ODS column using methanol:0.01 M sodium hexane sulfonate:formic acid (67.5:212.5:1 v/v/v) as the mobile phase. The flow rate was 2 mL/min and the column temperature was adjusted to 35 °C. Quantification was achieved with UV detection at 277 nm over concentration range of 100-600 and 4-24 μg/mL, with mean percentage recoveries were found to be 99.90 ± 0.586 and 99.26 ± 0.901 for PARA and PAMB, respectively. The second method was based on thin-layer chromatography separation of PARA and PAMB followed by densitometric measurement of the spots at 254 nm and 277 nm for PARA and PAMB respectively. Separation was carried out on aluminum sheet of silica gel 60F254 using dichloromethane:methanol:glacial acetic acid (7.5:1:0.5 v/v/v) as the mobile phase over concentration range of 1-10 and 0.32-3.20 μg per spot, with mean percentage recovery of 100.52 ± 1.332 and 99.71 ± 1.478 for PARA and PAMB, respectively. The methods retained their accuracy in presence of up to 50% of P-aminophenol and could be successfully applied in tablets. © the author(s), publisher and licensee Libertas Academica Ltd.


Nesseem D.I.,National Organization for Drug Control and Research
Drug Testing and Analysis | Year: 2011

The objective of the present work was (1) to develop an in situ gelling ophthalmic delivery system by combining pluronic F127 and pluronic F68, with sparfloxacin; and (2) to examine the influence of incorporating a mucoadhesive polysaccharide such as sodium hyaluronate on the healing property due to bacterial keratitis. The formulations (F1-F6) were sterilized by gamma irradiated using Co60. Ultraviolet (UV) and infrared (IR) spectra studies were performed on sterilized and non-sterilized formulae. The formulations were evaluated for rheological characteristics, in vitro release behavior, and efficacy against induced bacterial conjunctivitis in rats' eyes. Moreover, histopathological evaluations were also done. All the samples passed sterility tests, and no change in physical appearance of the formulae due to gamma radiation was observed. The IR spectra of the formulae before and after sterilization showed similar peaks which confirmed that no ingredient was affected by gamma radiation. The formulations showed a flow index of 0.116-0.493 indicating pseudoplastic flow behavior. The release behavior of all formulae was non-Fickian anomalous release. The different formulae used to overcome the pathological alterations, produced by bacteria infections varied among each other depending on the duration of treatment; however, the effectiveness of formulation was arranged as F5, F4 and F3, respectively. The developed formulations were therapeutically efficacious, and provided sustained release of the drug over a 24-hour period. A better improvement in artificially induced bacterial conjunctivitis in rats' cornea was observed with the developed formulae; thus it can be considered as a viable alternative to conventional eye drops. Copyright © 2010 John Wiley & Sons, Ltd.

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