Al-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301PREPARATION AND CHARACTERIZATION OF PLGA NANOPARTICLES1171248810.21608/ajps.2015.12488ENDinaHelalFaculty of Pharmacy, Department of Pharmaceutics and Industrial Pharmacy, Ain Shams University, Cairo, EgyptJournal Article20180904Nanoparticles were prepared by emulsion solvent evaporation method, using methylene chloride (DCM) as the organic solvent and poly vinyl alcohol (PVA) as the surfactant. Different formulation conditions such as surfactant concentration, drug amount, homogenization time, aqueous phase volume were investigated for drug entrapment efficiency, drug loading and particle size. It was found that PVA concentration less than 1% was unable to form a stable emulsion, increasing drug amount more than 30 mg didn't lead to any significant difference in drug entrapment efficiency or particle size, homogenization for 2 minutes led to particles having larger size and higher entrapment efficiency than those obtained after 3 minutes homogenization, increasing the aqueous phase volume from 40 ml to 80 ml led to a significant increase in entrapment efficiency and a significant decrease in particle size.https://ajps.journals.ekb.eg/article_12488_168925a2a463146c316c9b3ac13f6dcb.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301THE PROKINETIC EFFECT OF ITOPRIDE, A COMPARATIVE STUDY WITH METOCLOPRAMIDE18301248910.21608/ajps.2015.12489ENElsayedKamelDepartment of Clinical Pharmacology, Faculty of Medicine, Zagazig UniversityJournal Article20180904The motor function of GIT can be modulated by prokinetics or myorelaxant drugs depending on the nature of the disorder. There is a frequent need for facilitation of gastric emptying in treatment of functional dyspepsia. Among prokinetic drugs used there are compounds belonging to cholinergic and adrenolytic classes. In addition, drugs having affinity for serotonin, motilin and opioid receptors, also participate in alleviating delayed gastric emptying. Itopride is a prokinetic that acts via blocking D<sub>2 </sub>receptors in addition to inhibition of choline esterase. Metoclopramide prokinetic effect on the other hand is mediated through D<sub>2 </sub>receptor blockade. This study was designed to investigate the effect of the two prokinetic drugs (itopride and metoclopramide) on the motility of different parts of GIT.
The results of the present work demonstrated that both itopride and metoclopramide produced significant increments in the amplitude of contraction of fundus stomach of rats, pylorus, jejunum and colon of rabbit in a concentration – dependent manner, It was also proved that itopride is more potent as a prokinetic on these parts of GIT which is evident by the low ED50 of itopride compared to that of metoclopramide. In conclusion, itopride is preferred as a prokinetic than metoclopramide because it has higher potency in addition to acceleration of upper and lower GIT motility.https://ajps.journals.ekb.eg/article_12489_5be47c8b2667b333cd1f9aac2ab7fb43.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301CYTOTOXICITY OF SORAFENIB IN HUMAN HEPATOCELLULAR CARCINOMA CELLS31401249010.21608/ajps.2015.12490ENMaiAbd El-MageedFaculty of Pharmacy, Pharmacology and Toxicology Department, The British University in Egypt (BUE), Cairo, EgyptJournal Article20180904Hepatocellular carcinoma (HCC) is the predominant type of primary liver malignancy with high rates of mortality worldwide. Most HCC tumors are inherently resistant to chemotherapy and despite the tremendous advances in cancer chemotherapy, their treatment remains quite challenging.
Sorafenib, a multikinase inhibitor, has recently been approved for the treatment of advanced HCC. The present study aimed to further explore the potential cytotoxic activities of sorafenib in HepG2 cells as well as the possible underlying mechanisms. Thus, HepG2 cells were treated with different concentrations of sorafenib. The concentration that inhibited the growth of the cells by 50% was calculated from the fitted survival curves. The effect of sorafenib on cell cycle, apoptosis and proliferation was investigated. Sorafenib- induced cytotoxicity in HepG2 cells. This could be partially attributed to increased apoptosis by augmenting the level of active caspase-3. Moreover, sorafenib induced cell cycle arrest and had anti-proliferative effects by decreasing the level of p-Akt.https://ajps.journals.ekb.eg/article_12490_454050afc53399654a4ffcdf1be963c5.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301ROLE OF OXIDATIVE STRESS IN TRAUMATIC BRAIN INJURY41521249110.21608/ajps.2015.12491ENAmiraEl-gazarPharmacology & Toxicology Department, Faculty of Pharmacy, October 6 UniversityJournal Article20180904Traumatic brain injury (TBI) is a worldwide health problem with oxidative stress recognized as a major pathogenetic factor, and leading cause of disability and death in young adults. The present experimental work was designed to study the role of oxidative stress in TBI. Mice were randomly classified into two groups (Sham group and TBI group, n=18 each). Mice were anaesthetized with chloralhydrate (400mg/kg), after 24 hour of the surgery, the animals were killed by cervical dislocation, and brains were rapidly isolated and homogenized in saline, sham animals were subjected to same conditions without TBI. Traumatic brain injury group exhibited significant increment in lactate dehydrogenase (LDH), malondialdehyde (MDA) and prostaglandin E2 (PGE-2) contents as compared to sham group. Also, TBI group showed decrease in total antioxidant capacity (TAC) and systolic blood flow (SBF). TBI group showed focal gliosis detected in the cerebral cortex, associated with neuronal degeneration and diffuse gliosis in the striatum of the cerebrum. Based on our results, we concluded that, increasing oxidative stress plays an important role in TBI and decreasing it will offer neuroprotection to mice against TBIhttps://ajps.journals.ekb.eg/article_12491_186688fc23efeef417d5192097a98668.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301EFFECT OF AROMATASE INHIBITOR THERAPY ON PREDICTED ADULT HEIGHT IN PREPUBERTAL BOYS WITH IDIOPATHIC SHORT STATURE53731249210.21608/ajps.2015.12492ENThamarMahmoudDepartment of Clinical Pharmacy, Faculty of Pharmacy, MISR UniversityJournal Article20180904To investigate the effect of blocking estrogen biosynthesis with anastrozole, a potent aromatase inhibitor (AI) on growth and consequently predicted adult height (PAH) in boys with high estrogen level. Also, the effects of aromatase inhibition on gonadotropin secretion in boys during prepubertal phase.https://ajps.journals.ekb.eg/article_12492_8249b81b9cc5d3b74f366ebb20002858.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301EFFICACY AND SAFETY OUTCOMES OF RIVAROXABAN IN ACUTE DEEP VENOUS THROMBOSIS PATIENTS74821249310.21608/ajps.2015.12493ENNevenSarhanTeaching Assistant in Clinical Pharmacy department, Faculty of Pharmacy, Misr International UniversityJournal Article20180904<strong>Background</strong>
Rivaroxaban is the first oral anticoagulant drug that is a direct inhibitor of activated factor X (FXa) of clotting which may provide a simple, fixed-dose regimen for treating acute deep-vein thrombosis (DVT) without the need for laboratory monitoring.
<strong>Method</strong>
An opened label randomized parallel group clinical trial compared subcutaneous enoxaparin 1 mg/ kg once daily for 5 days followed by oral rivaroxaban 20 mg once daily with subcutaneous enoxaparin 1 mg/ kg once daily followed by a vitamin K antagonist (warfarin) for 2 month of treatment. The primary efficacy outcome for both was recurrent venous thromboembolism (VTE). The principal safety outcome was major bleeding or clinically relevant non major bleeding.
<strong>Results</strong>
Out of the 20 patients in the rivaroxaban group, 5 patients (25%) developed bleeding events while in the standard therapy group 8 out of 20 patients, 40 % developed bleeding events. Moreover, 10 patients in the rivaroxaban group (50%) developed adverse drug reactions versus 14 patients (70%) in the standard therapy group. However, none of the patients in both groups developed recurrent VTE neither DVT nor pulmonary embolism (PE).https://ajps.journals.ekb.eg/article_12493_d49acc767557cec7dc9d843a12eac40a.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301CARDIOPROTECTIVE EFFECT OF CILOSTAZOL VERSUS CLOPIDOGREL IN EXPERIMENTALLYINDUCED MYOCARDIAL INFARCTION IN MALE ALBINO RATS831071249410.21608/ajps.2015.12494ENEl SayedKamelDepartment of Clinical Pharmacology, Faculty of Medicine Zagazig UniversityJournal Article20180904Antiplatelet agents remain the cornerstone treatment in patients with ischemic heart diseases, as they decrease the mortality as well as the recurrence of cardiovascular complications. This study aimed to assess and compare the possible cardioprotective effect of cilostazol, clopidogrel and their combination in experimentally induced myocardial ischemia/reperfusion (MI/R) in rats.In this study ninety-six rats were divided into six equal groups (each of 16 rats): group 1, control normal received the vehicle; group 2, sham-operated and received the vehicle; group 3 (MI/R-treated) where myocardial infarction was induced by left coronary artery ligation (LCAL) for 30 min, followed by 2 h. reperfusion; group 4 received cilostazol (20 mg/kg, p.o.); group 5 received clopidogrel (30 mg/kg, p.o.); group 6 received combination of both drugs in the same doses. In all treated groups (groups 4, 5 & 6), drugs were administered for 3days, then they were exposed to MI/R. Results of the present study revealed that MI/R injury induced a significant decrease in mean arterial blood pressure (MABP), increase in heart rate (HR), elevation in T-wave voltage along with increased infarct size, plasma cardiac troponin I (cTnI) level and tumor necrosis factor alpha (TNF-α) and heart content ofmalondialdehyde (MDA), consequently with reduction in heart tissue glutathione peroxidase (GPx) activity. Cilostazol, clopidogrel or their coadministration exerted cardioprotective effect manifested by significant reductions in the T-wave voltage, infarct size and cTnI level via enhancement of antioxidant capacity and prevention of inflammatory and oxidative stress cascades. Additionally, cilostazol increased the HDL and decreased the LDL levels. It could be concluded that cilostazol is an effective cardioprotective agentin treatment of myocardial infarction particularly when used as an adjuvant to clopidogrel.https://ajps.journals.ekb.eg/article_12494_8294c8505f9ce6d9eb7cb8463a69ef5e.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301THE EFFECT OF SELENIUM SUPPLEMENTATION ON LUNG FUNCTIONS IN PATIENTS WITH IDIOPATHIC PULMONARY FIBROSIS1081161249510.21608/ajps.2015.12495ENNadaHazemTeaching Assistant, Clinical Pharmacy and Pharmacy Practice Department, Misr International University, EgyptJournal Article20180904Idiopathic pulmonary fibrosis (IPF) is a common aggressive form of the idiopathic interstitial pneumonias of unknown cause. It is chronic, progressive, irreversible, fibrosing and lethal lung disease with a poor prognosis. The cardinal symptom of IPF is dyspnea; however, other pulmonary and extra-pulmonary symptoms are often present. The study aims to implement a novel pharmaceutical approach by administration of selenium accompanied with prednisone in an attempt to improve clinical outcome of IPF patients to decrease other medications toxicities and improve patients’ quality of life. This study was conducted at Kasr El-Ainy Chest Hospitals, from April 2012 to March 2014.The work included forty clinically and radiologically diagnosed cases of IPF and twenty healthy controls, they were subdivided into Group I: twenty IPF patients received; N-acetyl cysteine (NAC) 600 mg/3 times (for 3 months).Group II: twenty IPF patients received: Selenium 200 mcg/day (for 3 months). All cases subjected to medical history, clinical examination, plain X-ray chest, and High resolution computed tomography (HRCT), 6-minute walk test, and spirometry. All patients signed informed consents. The comparison of Selenium group with NAC revealed a significant increase in both of forced vital capacity (FVC) and Forced expiratory volume in the first second (FEV1) (p= 0.008, 0.016, respectively), using a Mann-Whitney test. There was no remarkable adverse drug reactions observed in both groups, and no serious drug interactions. This study showed that selenium supplementation in IPF patients’ significantly improved pulmonary functions, which reflect an antioxidant capacity. In addition patients’ clinical presentation shown as significant decrease of coughing and dyspnea on exertion.https://ajps.journals.ekb.eg/article_12495_f950cea6ca66e9b54bae7f8837a3fef7.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301PROFILES OF LIPASE AND PROTEASE ENZYMATIC ACTIVITIES AND ANTIMICROBIAL RESISTANCE OF SOME BACTERIAL ISOLATES RECOVERED FROM BLOOD SAMPLES1171331249610.21608/ajps.2015.12496ENAmiraAbdelbasetDrug Radiation Research Department, National Center for Radiation Research and TechnologyJournal Article20180904Bloodstream infection (BSI) continues to be a life threatening condition. The host response to such infection varies from clinical signs. In this study, blood samples were collected from immonocompromised patients having leukemia and immunocompetent patients during onset of fever. blood samples were collected at fever onset to predict gram negative bacteremia and study the relation between virulence factors represented as lipase and protease enzymes production in gram negative bacteremia in comparison to antibacterial resistance profiles. Twenty four (24) feverish in-patients were enrolled in the study. Blood samples were collected and cultured on blood culture media for isolation of gram negative organisms and identified by API 20E technique then antimicrobial susceptibility tests and enzymatic activity of lipase and protease were performed.Gram negative bacteria isolated from blood samples showed high resistance against most of the antibacterial agents used. Even in presence of protease and lipase activity as virulence factors.We concluded that continuous monitoring of antimicrobial resistance is required among in-patients to decrease the risk of bacteremia and resistance.https://ajps.journals.ekb.eg/article_12496_41e194caa825743092f3f2e794973d68.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301BIOADHESIVE BUCCAL DISCS OF FLUVASTATIN SODIUM1341511249910.21608/ajps.2015.12499ENNadaAssaediDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptJournal Article20180904Fluvastatin sodium (FVS) is a cholesterol lowering agent (HMG-CoA reductase inhibitor) which undergoes extensive hepatic first pass metabolism causing an absolute bioavailability of ~30%. The aim of this work was to formulate a buccoadhesive disc of FVS to be applied to the buccal mucosa, releasing the drug in a unidirectional manner, in order to improve the bioavailability of the drug and lower the dose-dependent side effects. The bioadhesive discs were prepared by direct compression method using several polymers such as: guar gum, sodium alginate, sodium carboxymethyl cellulose, carbopol 934P, and hydroxypropylmethyl cellulose. Impermeable ethyl cellulose was applied as the backing layer. Different permeation enhancers such as bile salts, surfactants, fatty acids, chitosan, dimethyl sulfoxide, and polyethylene glycol 6000 (PEG 6000) were tested to improve the permeability of buccal mucosal membranes. The optimized formulation contained FVS, guar gum, PEG 6000, and sodium deoxycholate (permeation enhancer, 4%). It showed a drug release of 95.4% in 80 min, drug permeation through chicken pouch membrane (flux (J<sub>ss</sub>) = 3.74 mg cm<sup>-2</sup> h<sup>-1</sup>), ex vivo bioadhesion strength of 2.543 g, along with satisfactory bioadhesion time of 4.87 h. Physicochemical characteristics of the buccal discs such as drug content uniformity, disc thickness, disc hardness, surface pH, and swelling index were also evaluated.https://ajps.journals.ekb.eg/article_12499_b02c8cff454f3012ab47c12c3e09ffab.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301DOES VITAMIN D CONCENTRATION IS CORRELATED TO CHRONIC HEPATITIS C TREATMENT FAILURE: A CASE CONTROL STUDY1521631250110.21608/ajps.2015.12501ENAhmedAbdelsalamMisr International University, Department of Biochemistry, Faculty of PharmacyJournal Article20180904Egypt has the highest prevalence rate of Hepatitis C virus (HCV) in the world, where, chronic hepatits C (CHC) is considered a major health problem. The standard treatment of CHC is combination therapy of pegylated interferon and ribavirin. Successful treatment and sustained virological response (SVR) are only achieved in 30% of patients. Major adverse effects and high cost of the treatment makes predicting the treatment output is an important approach. The aim of this study to find an association between Vitamin D concentration with achieving SVR. <strong>Patients and methods</strong>: In this study; 250 patients were selected and divided into 3 groups (100 CHC patients who achieved SVR, 100 CHC patients who did not achieve SVR, and 50 patients as control). Blood samples were collected to measure vitamin D concentration and routine liver function tests. <strong>Results</strong>: Vitamin D concentration was found significantly higher in the responders more than non responders. <strong>Conclusion</strong>: Vitamin D concentration is valid predector to the response of CHC patients to combination of pegylated interferon and ribvirin thrapyhttps://ajps.journals.ekb.eg/article_12501_60249cb79e3f44e3f26e6599494b2ad9.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME NEW 1,2,4-TRIAZINO[6,1-B]QUINAZOLINE DERIVATIVES.1641751250410.21608/ajps.2015.12504ENMervatEl-EnanyPharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.Journal Article20180904In this study, novel 3-substituted 1,2,4-triazino[6,1-b]quinazolines 4a-e, 8-substituted-1H-[1,2,4]triazino[6,1-b]quinazoline-2,4,10(3H)-triones 8a&b and 2-substituted 1,2,4-triazino[6,1-b]quinazolines 9a-d, 10 & 11 were synthesized from 3-amino-6-bromo-2-ethoxycarbonylquinazolin-4(3H)-one<strong> (2b) </strong>and3-amino-2-aminocarbonylquinazolin-4(3H)-one 7a&b. Some of the newly synthesized compounds were tested for their antimicrobial activity and analgesic activity.
Depending on the obtained results, the newly synthesized compounds possess significant analgesic activity and mild antimicrobial activity.https://ajps.journals.ekb.eg/article_12504_8c1806abeb6ffc55e780bdc16f4d7d88.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301HEPATOPROTECTIVE EFFECT OF FORSKOLIN IN CARBON TETRACHLORIDE-INDUCED MODEL OF ACUTE LIVER INJURY1761841250710.21608/ajps.2015.12507ENNermeenEl-AgroudyDepartment of pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptJournal Article20180904Liver disease is one of the most common causes of death in the world. Nowadays, research studies have been focused on the development of new drugs for treatment of liver damage. Some natural products from medicinal plants have been found as potent agents for protection against liver injury induced by chemicals. Thus, it is interesting to find more effective natural products for protection against liver injury. Accordingly, the present study was designed to assess the hepatoprotective potential of a diterpenoid forskolin, isolated from the Indian plant Coleus forskohlii, at different doses in rat model with acute liver injury induced by carbon tetrachloride (CCl<sub>4</sub>) at a dose of 1ml/kg intraperitoneally as a mixture with corn oil. Forkolin was administered in doses of 5,10,20,40 mg/kg intraperitoneally for 7 days. Its protective effect was assessed via liver function tests and histopathological liver sections. Significant reduction in the hepatic enzymes levels was found in animals treated with forskolin at a dose of 10mg/kg as well as restoration of hepatocellular architecture. Therefore, treatment with forskolin showed preventive effect against CCl<sub>4</sub>-induced liver damage.https://ajps.journals.ekb.eg/article_12507_88568594f77e13364a2fcbe2f1f5bee9.pdfAl-Azhar University, Faculty of PharmacyAl-Azhar Journal of Pharmaceutical Sciences1110-164451120150301EVALUATION OF SAFETY AND EFFICACY OF CAUDAL ADMINISTRATION OF BUPIVACAINE/ DEXMEDETOMIDINE VERSUS BUPIVACAINE/FENTANYL IN PEDIATRIC UNILATERAL HERNIA REPAIR1851971250910.21608/ajps.2015.12509ENReemSleem,Department of Clinical Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, EgyptJournal Article20180904Background& Aim: Effective postoperative analgesia is important from the patient’s perspective and can also improve clinical outcomes. This study aimed to compare the effect of caudal bupivacaine plus fentanyl versus caudal bupivacaine plus dexmedetomidine on the recovery of anesthesia, postoperative analgesia required, hemodynamic stability& neurological complications in pediatric unilateral hernia repair patients.
Patients & Methods: 50 (ASA) grade I patients, aged 2-4 years with uncomplicated unilateral inguinal hernias treated as day cases were randomly allocated into either; Group I (BF), received Bupivacaine 0.25 % 1 ml\ kg, and fentanyl 1 μg\ kg, or Group 2 (BD), received Bupivacaine 0.25 % 1 ml\ kg, and dexmedetomidine 1 μg\ kg.
Patients were evaluated in terms of pain and sedation using FLACC scale and Ramsay Sedation Scale, respectively. Haemodynamic stability and Neurological complications were assessed during the postoperative period and one day postoperatively.https://ajps.journals.ekb.eg/article_12509_b6aab481348a49acf1e68192e0fa0425.pdf