Time filter

Source Type

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 | 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.

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.

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.

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.

Discover hidden collaborations