Vol. 34, November, 2010.


Amira Roushdy Khattab, *Mohamed Abou-Shoer, *Fathallah Mohamed Harraz, *Maged Gaber El-Ghazouly

Department of Pharmacognosy, Faculty of Pharmacy, Pharos University, Alexandria, Egypt and *Department of Pharmacognosy, Faculty of Pharmacy, Alexandria University, Alexandria.

Chamomile oil has always been characterized and standardized in many compendial and non-compendial monographs as configured by the specified critical values for few particular constituents such as the bisabolol oxides, (-)-α-bisabolol and chamazulene. However, tagging the oil quality by its content of a limited number of components oversimplifies not only the process of estimating the oil purity but also the process of assessing its potency, and hence; the wholeness-value of the material would not be treasured. In this study, an evaluation of the commercially available chamomile oil was conducted using two different chromatographic techniques (TLC and GC) and assisted by chemometrics while not being endured or bound by the former quality-curbing markers. An innovative tool for visualizing the oils compositional-quality has been developed via merging the analytical concept of HCA with DE-TLC and GC profiles which will be of value in discriminating between the various quality grades of the analyzed oil samples in a holistic rather than a reductionistic approach.




Awatf A. Farrag, Yousry A. Ammar*, Abd Allah G. El-Sehemi*, Samir Y. Abbas**, Nashwa A. Hassan and Aziza Kh. Samy

Chemistry Department, Faculty of Science for Girls at Khorma, Taif University, Makka, SaudiArabia.

*Chemistry Department, Faculty of Science, King Khaled University, Abha,

Saudi Arabia.

**National Research Centre, Dokki, Cairo, Egypt

Treatment of 2,3-dichloroquinoxalines (2a,b) with p-fluoroaniline and m-trifluoromethylaniline under different conditions was discussed. In ethanol afforded the monoamine derivatives 3a-d, while in DMF the corresponding diamines 5a-d were obtained. Interaction of the sulfonyl chlorides 6a,b with the same amines furnished the corresponding sulfonamides 7a-d. Thionation of compounds 7a,b with phosphorous pentasulfide produced the thiol derivatives 8a,b. Furthermore, interaction of 2,3-dichloroquinoxalin-6-sulfonyl chloride (9a,b) with p-fluoroaniline and m-trifluoromethylaniline gave the corresponding 2,3-dianilino-quinoxaline-6-(aryl)- sulfonamides (10a-d). Finally, 2-arylamino-3,6-dimethylqunoxalines (13a,b) were obtained upon treatment of the chloro derivative 12 with the requisite amines. The anticancer activity for the tested compounds showed that, compounds 5d, 8b, 13b, 7d and 3d were the most effective against the liver carcinoma cell line showing IC50 values0.3, 0.78, 1.14, 1.25 and 1.89µg/ml, respectively.



Faten K. Abd El-Hady, Mohamed H. Arif*, Abd El-Monem M.F. Eissa*, Kamel H. Shaker**, Ahmed G. Hegazi*** and Amal M. Ibrahim

Department of Chemistry of Natural Products, National Research Center, Egypt.

*Department of organic chemistry, Faculty of science, Benha Univercity.;

**Department of Chemistry of Natural Compounds, National Research Center, Egypt

***Department of Zoonosis, National Research Center, Giza, Egypt

Propolis is a resinous substance collected by honeybees from leaf buds and cracks in the bark of various plants .Three flavonoids were isolated; chrysin as major compound with two other minor compounds (Acacetin and chlorochrysin). The isolated compounds exhibited significant antioxidant activity against the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and superoxide anion radical generated from Xanthine-Xanthine oxidase system.



Maha F.M. Ali and Shahira F. El-Menshawe*

Department of Medical Applications of Laser, Pharmaceutical Technology Unit, National Institute of Laser Enhanced Sciences, Cairo University, Cairo, Egypt.

*Departement of Pharmaceutics and Industrial Pharmacy, Beni-Sueif University,

Beni Sueif, Egypt

Liposomes are carriers of photosensitizers used in photodynamic therapy. Preparation of flexible liposomes loaded with eosin (E) for ecrine glands targeting using intense pulsed light was evaluated as a novel approach to the problem of primary axillary hyperhidrosis (PAH). Various formulations regarding percentage of cholesterol (CHOL) and sodium deoxycholate (SDC) were prepared by film hydration method. Liposomes were characterized and the best formulation in 5% carboxymethylcellulose sodium hydrogel was evaluated for in vitro skin permeation using BALB/C mice. Clinical study was conducted on 20 patients with persistent bilateral PAH and the efficacy was measured by Hyperhidrosis disease severity scale (HDSS). Maximum loading of E was noted for liposomes composed of 50 % CHOL and 5% SDC. After gel application and laser sessions, 45% of patients were of grade 1, 50% were of grade 2 and only one patient improved one point of HDSS. Results supported that good release of E from vesicles form a concentration gradient to facilitate the penetration with the enhancing effect of the phospholipids. Deposition in ecrine gland was facilitated by the hydrophilic nature of E. Liposome size and phospholipids content were major factors in permeation and deposition.



Maha F.M. Ali

Department of Medical Applications of Laser, Pharmaceutical Technology Unit, National Institute of Laser Enhanced Sciences, Cairo University, Cairo, Egypt.

Light sensitive liposomes represent one of the advantages in the improvement of drug delivery. The objectives of this work are to prepare, study the physicochemical properties and the photostability of photosensitive liposomes embedded photoreceptor for drug delivery. Hypericin (HYP) is a hydrophobic photosensitizer was embedded in liposomal membrane as a photoreceptor. Liposomes from partially unsaturated egg yolk PC, cholesterol and HYP was prepared by simple film hydration method and loaded with oxytetracyclin (OTC) as a model drug. Photostability studies were carried out using UV-Visible spectrophotometry and following emission characteristics. The irradiated samples with 90 J/cm2 of 532 nM laser module had significant (p<0.001) higher and immediate drug release in vitro (20%) than the un-irradiated ones due to the effect of free radicals and singlet oxygen generated from photoactivated HYP in liposomal membrane despite of the increased photostability. The release mechanism for the prepared liposomes was best fitted with Higuichi's diffusion which changed in irradiated liposomes to zero order. The results were agreed with Fourier Transform-Infrared (FT-IR) spectroscopy which showed that post irradiation there was a brake down of hydrogen bonds between HYP and phospholipids functional groups in liposomal membrane and there was a decrease in phase transition temperatures as measured by Differential Scanning Calorimetry (DSC). As a conclusion, liposomes imbedded HYP as a photoreceptor is photostable pharmaceutical drug delivery system and laser irradiation photoactivate HYP to liberate free radicals that break down hydrogen bonds between HYP and phospholipids functional group and causes immediate drug release in vitro.



Mona H. Aboul-Einien, Nadia A. Soliman* and Ebtsam M. Abdou*


Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

*National Organization of Drug Control and Research (NODCAR), Cairo, Egypt.

Rabeprazole sodium is a proton pump inhibitor that is susceptible for acid degradation and undergoes hepatic metabolism. Development of sublingual tablets that deliver rabeprazole directly to the blood stream is presented in this work. Different formulations containing different types of super disintegrants were prepared and evaluated for their flow and compression properties. The selected formulations were compressed with 0.5% sodium lauryl sulphate as a permeation enhancer and the produced tablets were in- vitro evaluated for their main physical characteristics and were found to comply with USP pharmacopoeial specifications. The wetting time and disintegration time of the prepared tablets as well as dissolution profiles of the drug from them were assessed. The formulation that gave best results was that prepared using 5% crosspovidone and 0.5% sodium lauryl sulphate, it was selected for further investigation. Differential scanning calorimetry and infrared spectroscopy studies -carried out on the selected formulation- disproved any interaction between the drug and the used excipients. No significant changes in main tablet characteristics of the selected formulation were recorded after storage at 40ºC and 75% relative humidity for three months. The extent of absorption of rabeprazole from a selected sublingual tablet formulation, an enteric- coated commercially available tablet and an oral capsule was compared after single oral dose (10 mg) administration in rabbits. The tested sublingual tablet showed 1.3 and 1.4- fold increase in the average Cmax, 67 and 32- minutes decrease in the average Tmax when compared to the other treatments, respectively. The average AUC0-5 of rabeprazole from sublingual tablets increased by 33% and 39% in comparison to the other treatments, respectively. It could be concluded that formulation of rabeprazole as sublingual tablets succeeded in improving its biovailability.




Al-Sayeda H. Abdel-Aziz, Hadir M. Meir and Mona R. Al-Shathly

Zoology Department, Science Collage, King Abdullaziz University, Jeddah, KSA.

To evaluate the efficiency of neoadjuvant chemotherapy with docetaxel /epirubicin combination fifteen female patients with LABC were treated at KAAH & OC-Jeddah-KSA from 2003-2004. Each patient received 4 cycles of NAC once per three weeks, consisting of epirubicin (EPI) 90 mg/m2 followed by docetaxel (DOC) 75 mg/m2. A lumpectomy or modified radical mastectomy was performed, then 4 cycles of adjuvant chemotherapy once per three weeks, and the treatment ended with radiotherapy. Post-treatment clinical assessment revealed that 27% of patients showed a clinically complete response. A partial clinical response was observed in 60% of patients, with reduction in tumor size and axillary nodes. Histological and ultrastructural examination on pre-treatment tumor biopsy and post-treatment remaining tumor tissue reveald complete disappearance of some tumor cells, and persistence of small masses with remarkable vacuolar degeneration and necrosis, where multinucleated giant cells were detected in other specimens, increases in heterochromatin aggregation, dilation of outer nuclear membranes and formation of intranuclear inclusions of cytoplasmic organelles and helioid bodies. This study suggests that the regimen of DOC & EPI combination as NAC may be efficient for treatment of locally advanced breast cancer.



Sherif K. Abu-Elyazid, Gina S. El Feky* and Fathy I. Abd Allah**

Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern sciences and Arts, 6th October, Egypt.

*Researcher of Pharmaceutical Technology, National Research Center, Cairo, Egypt.

**Department of Pharmaceutics, Faculty of Pharmacy, El Asher University, 10th of Ramadan, Egypt

The anti-diabetic drug, Repaglinide was incorporated into a microemulsion and niosomal drug delivery systems in order to overcome the drawbacks associated with its conventional oral formula. In the microemulsion based formulation Triacetin was selected as the oil phase, whereas, Cremophor® RH40 and n-butanol were used as the surfactant and co-surfactant, respectively. Pseudoternary phase diagrams were constructed in order to obtain the concentration range of the oil, surfactant and co-surfactant using three different surfactant/cosurfactant S/CoS weight ratios. The prepared microemulsion showed spherical particles with mean diameter of 40.60 ± 13.04 nm, viscosity of 58.94 ± 0.02 (mPa.S), refractive index (RI) of 1.43 ± 0.02 and pH 5.32 ± 1.1. However, the release of Repaglinide from the microemulsion formulations showed a zero order pattern. Repaglinide was also encapsulated in different niosomal formulations. The prepared niosomal formulations using span 60 and cholesterol showed an entrapment efficiency of 99.3 ± 5.2 % and vesicle size diameter of approximately 109 ± 6.2 nm. Moreover, the release profile of Repaglinide from the niosomal formulations followed Higuchi model. The release of the drug from the selected prepared delivery systems showed controlled and sustained profile when compared to the commercial tablet.


Seham S. El-Hawary, Abd El- Rahman O. EL-Shabrawy, Shahira M. Ezzat

And Fatema A. EL-Shibany*

Pharmacognosy Department, Faculty of Pharmacy, Cairo University,

Kasr El Ainy Street, Cairo, Egypt.

* Pharmacognosy Department, Faculty of Pharmacy, Garyounis University,

Bengazi, Libya.

A detailed macro- and micromorphological study of stems and leaves of Ajuga iva (L.) schreb, Marrubium vulgare (L.), Rosmarinus Officinalis (L.) and Thymus capitatus (L.) Hoffmann's. et link, (family Labiatae or Lamiaceae) grown in Libya as well as the diagnostic characters of their poweders were studied.




Amal S. Abu El- Enin, Afaf A. Ramadan and Amal K. Hussein*

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy,        

Al-Azhar University, Nasr City, Cairo, Egypt

*Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy,        

Minia University, Egypt

The aim of this work was to formulate once-daily sustained-release matrix tablets of isoxsuprine hydrochloride, a peripheral vasodilator used fordirect relaxation of vascular and uterine smooth muscles. The short half life of the drug, its short duration of action in addition to the side effect arising from repeated administration of market tablet (immediate release) made it suitable candidate for sustained release formulations.Therefore, sustained release tablets of isoxsuprine hydrochloride were prepared to increase the patient compliance by decreasing frequency of drug administration and the severity of adverse side effects. Sixteen formulations were prepared by the wet granulation method (F1-F16). Ethanolic solutions of ethyl cellulose (EC), Eudragit RL-100 (ERL), Eudragit RS-100 (ERS), and polyvinylpyrrolidone (PVP) were used as granulating agents along with hydrophilic matrix materials like hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (Na CMC), and sodium alginate. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, and in vitro release studies. All the tablet formulations showed acceptable pharmacotechnical properties and complied with specifications for tested parameters. The results of dissolution studies indicated that formulation F16 (drug-to-HPMC, 1:4; EC 10% w/v as granulating agent), could extend the drug release up to 24 hours and showed zero-order drug release, so it was selected for a comparative bioavailability study.


Ola M. Mousa, Mohamed A. Mahmoud*, Abd-El-Fattah H. Belal*, Magdy G. Abdel ELFadeel** and Mohamed M. Elmazar***

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Egypt.

*Plant Production Department, Faculty of Environmental Agricultural Sciences, Suez Canal University.

**Biochemistry Department of Food Scienecs, Faculty of Environmental Agricultural Sciences, Suez Canal University.

***Pharmacology Department, Faculty of Pharmacy, Ahram Canadian University (ACU).

The growth response of Salvadora persica L. in vitro via micropropagation using nodal cutting explants was investigated. The effect of kinetin, indole acetic acid and type of nutrient medium on the growth of nodal cutting cultured in vitro after 8 weeks in starting stage was studied. The influence of kinetin, indole acetic acid treatments and their combination on the Murashige and Skoog (MS) basal medium full strength was determined in the multiplication stage. The highest rooting percentage was obtained on MS medium supplemented with 2.0 mg/l IAA without addition of active charcoal. Preliminary phytochemical screening identifies the presence of carbohydrates and/or glycosides, free flavonoids, sterols and/or triterpenes, alkaloids as well as tannins more strongly in the shoot samples propagated from tissue culture technique indicating their occurrence in such samples with higher amounts. The UV and the visible spectra were recorded spectrophotometrically for the tested extractsprepared from both the wild and tissue culture propagated plant of S. persica L. The UV/visible spectra of the ethanol 95% extracts of both the wild and tissue culture propagated plant were similar. The intensities of the absorption bands were higher with the extracts prepared from the plantpropagated by tissue culture technique. The extracts of the propagated plant exhibited a broad spectrum antimicrobial activity against the tested microorganisms, meanwhile the extracts of the wild plant showed less activity.




Hamed H.M Abou-Seada, Khalid A.M. Attia, Monir A.A. Amin

and Ragab A.M. Said

Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University,

Cairo, Egypt

Four simple, sensitive, accurate, and precise methods were developed for determination of cefixime (CFX) in raw materials as will as in pharmaceutical preparation. The first method is HPLC stability – indicating method, where the intact drug (CFX), internal standard (cefadroxil) and CFX degradate were separated using a Scharlua neucleosil C18 column (25 cm x 4.6 mm I.D, 5μm particle size) using acetonitrile - 0.007 M phosphoric acid (16.5: 83.5 v/v) as mobile phase at flow rate 1.2 ml min-1 and UV detection at 270 nm, where a good linearity was obtained in the range of 0.5 – 16 µg ml-1. The second method depended on measurement of the difference absorbance (ΔA) of the drug in the presence of its degradate between 0.1M HCl and 0.1M NaOH solutions at 279 nm. Beer’s law was obeyed in the range of 5 – 40 µg ml-1. The third method is based on the reaction of drug with tetrazolium red in presence of KOH solution and measuring the produced red color at 484 nm. Linear relationship between absorbance and concentrations was obtained in the range of 10 – 70 µg ml-1. The fourth method is the measurement of the blue color produced from heating CFX with ammonium molybdate solution in H2SO4 medium at 699 nm. Good linearity was exhibited in the range of 5 – 30 µg ml-1. The percent recoveries ± RSD% of these methods were 100.64 ± 0.59, 100.69 + 0.69, 100.65 ± 1.01 and 100.63 ± 0.85 % respectively. The obtained results were compared with those of the reported method and no significant difference was observed regarding accuracy and precision.



Ashrf S. Darwish and Fatma E. Agha*

Biochemistry Department, Animal Health Research Institute, Dokki

*Department of Forensic Medicine and Toxicology, Faculty of Medicine for Girls, Al-Azhar University, Cairo, Egypt

Albendazole compounds are among the less toxic drugs currently used for parasitic control in human and veterinary medicine. Nevertheless exposure to albendazole during organogenesis and early developmental period is especially harmful. So the current study was carried out to investigate the suppressing effect of folic acid on maternal and embryo-fetal toxicity induced by albendazole in albino rats. Eighty mature female albino rats were divided into eightgroups, 10 animals in each group. First group was orally administered aqueous solution daily by gavage (-ve control group), while second, third and fourth groups were orally administered freshly aqueous suspension solutions of albendazole by gavage at a dose of 5, 10 or 20 mg/kg b.wt. Respectively daily from 6-15 of gestation days.Fifth group was administered folic acid at a dose of 2 mg /kg admixed with diet 15 days prior to the experiment and continues from the onset of gestation till the termination of the experiment (+ve control group). However, sixth, seventh and eighth groups were administered folic acid (pretreated) plus albendazole with the same doses and durations which are mentioned before.Resorption, placental and fetal characteristics data were recorded; in addition to fetal visceral and skeletal malformation.The results of the rat teratology studies showed that high dose of albendazole were embryotoxic and that lower doses caused impairment of fetal development.Dosage of 20 mg/kg albendazole evoked 100% resorption, while at 10 mg/kg induced a significant increase in resorption rate compared to controls. Dead and deformed small fetuses with remain of placenta were recorded at dose level of 5mg/kg. Fetal body weight of albendazole treated rats was significantly decreased than untreated rats. The most frequently observed internal soft tissue malformations were dilated third ventricle of brain & brain hydrocephaly, hypertrophy of heart, hypoplasia of lungs and dilated renal pelvis. The skeletal anomalies were skull abnormalities (in the form of incomplete ossification of skull and large open fontanel), retarded development of the sternum, incomplete ossification of pelvic bone, absence of caudal and coccogial vertebrae, absence of some metacarpal and metatarsal bone and absence of digits. Folic acid supplementation was extremely effective in reducing the occurrence of early resorption induced with the high dose levels and has a valid response in decrease incidence and severity of visceral and skeletal anomalies of the lower doses of albendazole.



Yasser I. Kandil, Mohammed M. El-Zahabi, Ossama A. Mansour, Shawkey S. Ali, Magdy M. Saber*, Samia Shouman* and Sayed A. El-Behery**

Biochemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University,

Cairo, Egypt.

*National Cancer Institute (NCI), Kasr Eleiny Hospital, Cairo University,

Cairo, Egypt.

**National Institute of Urology and Nephrology (NIUN), Elmatarya, Cairo, Egypt.

Introduction: Prostate cancer (PCa) is the second most frequent malignancy diagnosed in adult men. Androgens are considered the primary growth factors for prostate normal and cancer cells. However, other non-androgenic growth factors are involved in the growth regulation of PCa cells. Insulin-like Growth Factor (IGF-1) modulates cell growth and survival, and is thought to be important in tumor development. The association between IGF-1 and PCa risk is well established. However, there is no evidence that the measurement of IGF-1 enhances the specificity of PCa detection beyond that achievable by serum PSA levels. Objective: The aim of this work was to examine the biochemical relationship between serum IGF-1 and prostatic enlargement (eithermalignant or benign). Also, to determine if measuring serum IGF-1 level can improve the detection of PCa. Subjects and Methods: A consecutive series of 27 men with newly diagnosed untreated PCa, 30 men with newly diagnosed untreated Benign Prostatic Hyperplasia (BPH), and 24 healthy men controls were recruited. The diagnosis of PCa and BPH was made by transrectal ultrasound (TRUS) guided prostate biopsies followed by histopathological investigation. Serum total and free PSA and IGF-1 levels were measured by using chemiluminescence’s technique. Serum levels of IGF-1, total and free PSA were compared between cases and controls. Results: Serum IGF-1 levels were significantly higher in both PCa (231 ± 7.62 ng/ml, mean ± SEM, p < 0.001) and BPH patients (215 ± 9.20 ng/ml, p < 0.01) than in controls (176 ± 5.60 ng/ml). The median of both free and total PSA was significantly higher in both PCa and BPH patients as compared to control group (p < 0.001). Only total PSA was significantly higher in PCa than BPH patients (p < 0.05). The area under the curve (AUC) for total PSA, free PSA, and IGF-1 were 0.89, 0.81, and 0.72, respectively. Conclusions: The present results suggest that serum IGF-1 levels provide no useful information in the diagnosis of PCa or BPH. In addition, the measurement of IGF-1 does not enhance the specificity of PCa detection beyond that achievable by serum PSA alone, but rather that IGF-1 may be predictive of later cancer development.



Mohammed M. El-Zahabi, Ossama A. Mansour,Shawkey S. Ali, *Ashraf I. Amin, Mostafa M. El Shafaey and Ahmed I. Abul-Soud

Biochemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University,
Cairo, Egypt.
*National Institute of Diabetes and Endocrinology, Cairo, Egypt.

Metabolic syndrome (MetS) refers to the clustering of various metabolic and cardiovascular risk factors including dysglycemia, dyslipidemia, hypertension, and obesity. Recent evidence suggests a strong relationship between MetS and the development of chronic kidney disease (CKD). Insulin resistance (IR) and compensatory hyperinsulinemia with its multiple deleterious effects is central to MetS and is thought to contribute to renal injury. In addition, endothelial dysfunction, renal lipotoxicity, and inflammatory adipocytokines derived from visceral adipose tissue are thought to further contribute to renal injury in MetS. Objectives: To explore the significance of the MetS in the development of CKD, we examined the relation of metabolic disorders to renal function in diabetic and MetS subjects. Methods: Eighty subjects (40 male and 40 female their mean of age were 43 years) were employed in this study. Thirty patients with MetS and thirty diabetic patients were identified. Twenty age- and sex-matched subjects who did not have any of the criteria for MetS were used as controls. Results: Plasma vascular endothelial growth factor (VEGF) was significantly higher in MetS and diabetes mellitus (DM) groups. Also serum uric acid, urea, cystatin C, beta 2 microglobulin (β2M), urinary albumin and albumin creatinine ratio (ACR) were significantly higher in MetS group than control group. While serum triacylglycerols (TAG), creatinine, C reactive protein (CRP), were significantly higher in MetS group when compared to DM and control groups. On the other hand creatinine clearance was significantly lower in MetS and DM group than control groups. Also serum high density lipoprotein cholesterol (HDL-C) and estimated glomerular filtration rate (eGFR) were significantly lower in MetS group when compared to DM and control groups. While serum albumin, serum totals protein levels were significantly lower in MetS than controls in male groups. Conclusions: These results indicated that IR, endothelial dysfunction and inflammation might be important risk factors in the development of CKD. There was a steeper decrease in kidney function in patients with MetS, suggesting limited renal reserve. Aggressive screening and management may be warranted in patients with MetS to protect kidney function.

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