Vol. 43, November, 2013.

1/43 FORMULATION AND EVALUATION OF NEW KETOCONAZOLE SOLID DISPERSION MUCOADHESIVE VAGINAL TABLETS

Ghada H. Elosaily

Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.

In the present investigation mucoadhesive vaginal tablets of ketoconazole were formulated to prolongtheantimycotic action. Matrix tablets of ketoconazole were formulated using some mucoadhesive polymers namely HPMC K15M, HPC, HEC, Na alginate, NaCMC and xanthan gum. Solubility and in-vitro dissolution of ketoconazole was increased by preparing solid dispersion using some polymers namely poloxamer-407, mannitol and PEG-6000 in different ratios. These solid dispersions were analysed for the solubility and In-vitro dissolution profile. Solid dispersion of drug with poloxamer-407in the ratio 1:5 had shown enhanced solubility with improved dissolution rate. Further FTIR and DSC studies were carried out. Solid dispersion prepared with poloxamer-407 shows the presence of amorphous form confirmed by the characterization study. So the study shows that the dissolution rate and solubility of ketoconazole can be enhanced to considerable extent by solid dispersion technique with poloxamer-407. The mucoadhesive vaginal tablets of ketoconazole were prepared using ketoconazole-poloxamer-407 solid dispersion and the mucoadhesive polymers. The performances of these mucoadhesiveformulations were evaluated by the swelling behavior, the mucoadhesive strength and in-vitro dissolution. Anti-fungal activity of the selected mucoadhesive vaginal formulations of ketoconazole was determined.

2/43 SILDENAFIL DRUG ATTENUATES CISPLATIN-INDUCED NEPHROTOXICITY IN MALE ALBINO RATS

Abdel Moneim A. Ali, Ehab T. Mohamed* and Ahmed A. Elkady*

Department of Pathology, Faculty of Veterinary Medicine, ZagazigUniversity, Egypt

*Health Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA)

The aim of this study was focused on investigating the possible protective effect of sildenafil against cisplatin induced nephrotoxicity in male albino rats. Twenty four albino rats were divided into four equal groups as follows: control group; animals received orally distilled water, cisplatin group; animals received a single dose of cisplatin at a dose of 7 mg/kg body weight via intraperitoneally injection, sildenafil group; animals received sildenafil at a dose of 0.4 mg/kg/day via oral tube for 7 days and sildenafil and cisplatin group; animals received sildenafil at a dose of 0.4 mg/kg/day via oral tube for 7 consecutive days then injected intraperitoneally with cisplatin at a dose of 7 mg/kg via body weight. The obtained results revealed that the administration of cisplatin induced a marked increase in serum creatinine and blood urea nitrogen as well as the activity of urinary N-acetyl-b-glucosaminidase (NAG). Moreover, cisplatin induced an increase in the concentration of Malondialdehyde(MDA) and depletion in the activity of kidney catalase (CAT), Glutathione S transferases (GST), glutathione peroxidase (GPx) and reduced glutathione (GSH). Pathological examination of the kidneys confirmed the occurrence of renal damage. On the other hand, sildenafil was found to abolish cisplatin nephrotoxicity. In conclusion, our results indicate that sildenafil is a highly protective agent against kidney damage caused by cisplatin via maintenance of the oxidant–anti-oxidant status. Furthermore, sildenafil shows nephroprotective effects and might be useful in improving the therapeutic index of cisplatin.

3/43 BIOCHEMICAL STUDIES ON THE EFFECT OF GAMMA RADIATION ON RICE MOTH CORCYRA CEPHALONICA (STAINT) (LEPIDOPTERA:PYRALIDAE)

Doaa S. Farghaly, Asmaa Z. El Sharkawy, Nahed A. El-Halfawy*, Salwa A. Rizk* and Naglaa F. Bader

Zoology Deparment, Faculty of science, Al-Azhar University and *National Center for Radiation Research and Technology, Atomic EnergyAuthority.

The changes in total proteins,lipids and carbohydrates of 6th instar larvaeof Corcyra cephalonica (Staint) resulted from combination of irradiated males and normal females, combination of irradiated females and normal males and combination of irradiated males and irradiated females were studied. The total protein, lipids and carbohydrate levels decreased gradually as the dose of gamma radiation increased. Also,changes in amylase and invertase activities in the larvae resulted from the previous combinations showed that the activity of haemolymph amylase and invertase of F1 progeny 6th instar larvae decreased gradually as the dose of gamma radiation increase.

4/34 PROPHYLACTIC AND IMMUNO-MODULATIVE EFFECT OF GANODERMA LUCIDUM AGAINST THIOACETAMIDE -INDUCED HEPATOTOXICITY IN MALE ALBINO RATS

Nora E. Mohamed Shaheen

Zoology Department, Faculty for Women (Art, Science & Education),

Ain Shams University

Metabolism of many drugs and toxins is done in the liver. In this process some materials cause severe liver injury. In this regard this study aimed to assess the protective role of ganoderma lucidum (G.L.) on liver toxicity of male albino rats induced by thioacetamide (TA). Fiftyadult male rats were allocated into five groups: Group (I) served as a control group. Group (II); received distilled water (1 ml/kg b.w.) and treated with TA in a dose of 300 mg / kg b.w. intraperitoneally (i.p.) thrice a 4th week. Group III:pre-treated with G.L. in a dose of 100 mg orally in 1 ml distilled water daily for 4 weeks and treated with normal saline (1 ml/kg b.w.) thrice a 4th week. Group IV:pre-treated with G.L.(100 mg/kg b.w.) orally for 4 weeks and treated with TA (300 mg/kg b.w.) thrice a 4th week. Group V:pre-treated with G.L. (200 mg/kg b.w.) for 4 weeks and treated with TA (300 mg/kg b.w.) thrice a 4th week. The results indicated that exposure of TA caused significantly elevated of serum activities of aspartate and alanine aminotransferases (AST & ALT), gamma glutamate transferase (GGT) and alpha fetoprotein (AFP) indicating liver dysfunction. In addition, serum total cholesterol, triglycerides, tumor necrosis factor (TNF-α) and interleukien-12 (IL-12) levels showed highly significant increases, while, marked decrease in the interlukien-10 (IL-10) was observed. Hepatic Malondialdehyde (MDA) concentration and peroxidase activity were markedly increased reflecting increased lipid peroxidation, whereas, reduced glutathione (GSH) and superoxide dismutase (SOD) contents were significantly decreased. On the other hand, G.L. plus TA dose-dependently inhibited activities of AST, ALT, GGT and AFP in serum. On the other hand, the administration of G.L. plus TA exhibited significant reduction of lipid profile, peroxidase and lipid peroxidation while GSH content and SOD activity were elevated significantly that reflecting improving hepatotoxicity. In conclusion, the results obtained clearly indicated the role of thioacetamide on immuno and oxidative stress in induction toxicity and suggested hepatoprotective effect of ganoderma lucidum against toxicity of thioacetamide compound.

5/43 EFFECT OF BEE VENOM ON TUMOR MARKERS IN RATS INOCULATED WITH BREAST CANCER CELL LINE (MCF7)

Samir A.M. Zaahkouk, Mahmoud M. Elkasass, Diaa F. Ibrahim and Basem E. Elarabi

Department of Zoology, Fac. Science, Al-Azhar University, Cairo, Egypt.

This work was designed to evaluate the protective role of bee venom against cancer induced disease compared with adriamycin as chemotherapy by using white rats injected with breast cancer cell line (Mcf7) and incubated for one month. Method: This study using 70 virgin female Sprague Dawley Rats weighting 120±5 gram at the beginning of experiment. Rats were divided into seven equal groups: Except negative control rats, all groups inoculated with breast cancer cell line Mcf7 and incubated for one month, then treated by bee venom and Adriamycin. Results: Tumor markers CA15.3, CEA showed elevation in breast cancer cell line injected group. However bee venom groups showed improvement in the concentration of tumor marker CA15.3 and CEA. Conclusion:Bee Venom has anti-cancer activity on breast cancer but high dose effect on liver function test. The best dose for treatment of breast cancer in this study (1/4 LD50 of bee venom+Adriamycin)

6/43 TRANSFER KINETICS OF TEMOPORFIN BETWEEN UNILAMELLAR DONOR VESICLES AS A DRUG DELIVERY SYSTEM AND UNILAMELLAR ACCEPTOR VESICLES AS A CELLULAR MEMBRANE MODEL: INFLUENCE OF DONOR: ACCEPTOR LIPID RATIO AND THE DRUG: LIPID RATIO IN DONOR LIPOSOMES

Hossam Hefesha, Hany M. Ibrahim and Hatem R. Ismail

Department of   Pharmaceutics and industrial pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

Optimal drug delivery depends on understanding the release kinetics of the drug molecules from the host liposomes during the journey to the target site and at the target site. Unilamellar vesicles have been used as model of cell membrane in studies aimed to defining the mechanism and the effect of certain parameters on the transfer kinetics of poorly water-soluble drug namely temoporfin. To better mimic in vivo situation, cholesterol has been added to all vesicles. The main purpose of this study was the investigation of transfer kinetics of the drug by investigating the influence of lipid ratio between temoporfin-loaded liposomes (donor): liposomes used as cell membrane model (acceptor) and the drug:lipid ratio in temoporfin-loaded liposomes (donor). After incubation of temoporfin-loaded liposomes with liposomes used as cell membrane model, donor and acceptor liposomes were separated via ion exchange chromatography. Liposome stability and temoporfin transfer kinetics profile were determined with the help of a non-exchangeable 3H-lipid label and 14C-labeled temoporfin. The obtained results indicate that the transfer proceeds through the aqueous phase and suggest as approximation a first order kinetics at low lipid concentration. While at high lipid concentration, diffusion and collision mechanism take place through aqueous phase. Regarding the drug:lipid ratio, the concentration of the drug in the liposomal membrane has an impact on transfer rates. It is clear that at high membrane drug concentration, self-quenching of the drug influences on the release kinetics.

7/43 EFFECT OF ANTIHYPERTENSIVE DRUGS ATENOLOL AND CAPTOPRIL ON CARBOHYDRATE METABOLISM IN NORMAL AND DIABETIC RATS.

Omnia E. Ismael and Haytham A. Ali*

Biochemistry Department, Faculty of Pharmacy, Egypthian Russian University, Bader, Egypt.

*Biochemistry Department, Faculty of Vet. Med.-Zagazig University. Egypt.

Diabetes mellitus is a metabolic disorder of multiple etiologies characterized by chronic hyperglycemia with disturbances in carbohydrate, fat and protein metabolism resulting from defects in insulin secretion, action or both. Hypertension is a global problem all over the world, with a high increase in the level of mortality. So this work was designed aiming to study the effect of two different antihypertensive drugs on carbohydrate metabolism either in normal or diabetic status, these two drugs are beta blockers. Atenolol is an example and Captopril as another example and both are most common and widely used drugs. Ninety male albino rats were divided into 2 main groups: The first group is the normal group which is subdivided equally into control group, Atenolol treated group at a dose of 0.1mg/kg dissolved in 0.067 ml of distilled water and Captopril treated group in a dose of 0.1mg/kg dissolved in 0.067 ml of distilled water. The second group is the diabetic group which is subdivided in the same way. All sex groups provide their dose orally. The rats were scarified after 2 and 4 weeks. Serum glucose, serum insulin, hepatic glucokinase, succinate dehydrogenase, aldolase, pyruvate kinase, glycogen synthetase and glycogen phosphorylase activity and hepatic glycogen concentration have been verified. Results showed that, there were increases in the levels of plasma glucose, aldolase & pyruvate kinase with decrease the levels of insulin, glucokinase, SDH and liver glycogen amounts and enzymes in the groups treated with Atenolol when compared with other groups, at the same time there were a decrease in the plasma glucose level in the group treated with Captopril with increase in the serum insulin level with increase in the level of mitochondrial enzyme Sorbitol dehydrogenase (SDH) and liver glycogen especially in the diabetic groups that refers to improvement in the carbohydrate metabolism especially aerobic pathway. And so Captopril was found to improve carbohydrate metabolism in the diabetic and normal rat so it is preferred as a drug of choice over Atenolol especially in diabetic patients.

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