Open Access Short Research Article

In vitro Antioxidant Activity of Porana paniculata and Ipomoea quamoclit-Two Ethnomedicinally Important Plants of Convolvulaceae Family

A. Sanjeeva Kumar, J. Raveendra Reddy, V. Rama Mohan Gupta

Journal of Pharmaceutical Research International, Page 286-293
DOI: 10.9734/BJPR/2015/12226

Aims: Present study deals with the in vitro antioxidant activity of Porana paniculata and Ipomoea quamoclit whole plants belongs to Convolvulaceae family.
Study Design: The present study was designed for in vitro evaluation of antioxidant activity of two ethnomedicinally important plants of Convolvulaceae family.
Place and Duration of Study: Division of Pharmacognosy, Raghavendra Institute of Pharmaceutical Education and Research, Krishnam Reddy Palli cross, Chiyyedu, Anantapuramu-515721, Andhra Pradesh, India, between June 2013 and July 2013.
Methodology: Plant materials were procured, shade dried and made into powder. The extraction was carried out by maceration using water and ethanol as solvent and then total flavonoid and total phenol content was determined by standard methods. In vitro antioxidant activity was performed by DPPH assay, superoxide anion scavenging activity assay, nitric oxide scavenging activity assay, hydrogen peroxide scavenging assay and metal chelating activity. Percentage inhibition of free radical formation and IC50 values were calculated.
Results: Total flavonoids were found to be 59.86 and 49.26 for HAPP and HAIQ mg/ml of standard compound quercetin and total phenols was found to be 33.34 and 39.32 mg/g of gallic acid. In DPPH method, the half inhibition concentration [IC50] of HAPP, HAIQ and ascorbic acid were 71.68, 49.63 and 32.46 μg/ml respectively. In Superoxide anion scavenging activity assay, the half inhibition concentration [IC50] of HAPP, HAIQ and standard compound BHA was found to be 54.61, 69.34 and 93.46 μg/ml respectively. In nitric oxide scavenging activity assay both the extracts HAPP and HAIQ moderately inhibited nitric oxide in dose dependent manner with the IC50 being 83.49 and 89.47 μg/ml and standard compound ascorbic acid was 78.93 μg/ml respectively. The IC50 of HAPP, HAIQ and gallic acid were found 25.65, 46.39 and 24.29 μg/ml respectively in hydrogen peroxide scavenging method and in metal chelating method, HAPP and HAIQ indicated that they have chelating activity with an IC50 of 49.27 and 65.41 μg/ml and alpha tocopherol was 32.48 μg/ml.
Conclusion: From the above findings it can be concluded that Porana paniculata and Ipomoea quamoclit extracts exhibited antioxidant activity.

Open Access Original Research Article

A New Approach for the Treatment of Diabetes and Nicotine Induced Cataract by Modulating Specific Ion-Channels Function in Rat Lens

Vijay R. Chidrawar, Krishnachaitanya Gudlawar, Sushma Mondi, Uma Maheshwararao Vattikutti

Journal of Pharmaceutical Research International, Page 228-240
DOI: 10.9734/BJPR/2015/14002

Aim: Cataract is an eye disease characterized by a cloudiness of the normally transparent crystalline lens. Diabetes and smoking are the known risk factors for cataract development. It is well known fact that inorganic ions like Na+, K+, Ca++ and Cl- play an important role for the maintenance of lens hydration and transmittance. Nicotine aggravates cataract formation in diabetic patients by disturbing the ionic balance in the lens, generation of free radicals and disturbing normal lens physiology by generation of free radicals. Based upon these observations we have screened few drugs like Lidocaine, Nifedipine and Phenylglycine against Streptozotocin (STZ) + Nicotine induced cataract.
Methodology: Diabetes was induced by administration of combination of STZ (single dose of 52 mg/kg i.p.) and nicotine (0.3 mg/kg s.c) for 22 consecutive days and simultaneously treated with ophthalmic preparation of test drug i.e. Lidocaine, Nifedipine and Phenylglycine at 1% and 2% to the right and left eye respectively. On 23rd day of the study, various parameters like measurement of various ions (Na+, K+, Ca++ and Cl-), anti-oxidants (ascorbic acid, sulfhydral group, glutathione) and fructose content in rat lens were studied. We have also investigated the level of ascorbic acid in serum and monitored the blood glucose level at regular interval throughout the experiment.
Results: Accumulation of fructose in the lens cause malfunctioning of Na+-K+- ATPase pump which leads to accumulation of Na+ ions inside the membrane that causes to accretion of water and osmotic swelling of the lens. By the treatment with lidocaine (1% and 2%) eye drop significantly (P<0.001) reduced the Na+ content in both the eyes compared to disease control group.
Conclusion: In our study lidocaine has offered best protection against cataract. Phenylglycine has also shown protection but not as good as lidocaine, at the same time Nifedipine has not shown any protection.

Open Access Original Research Article

Effect of Root and Leaf Extracts of Tetracarpidium conophorum on Liver Enzyme Levels in Alloxan Induced Diabetic Rats

Ogbonna Onyemaechi John, Udia Pius Monday, Ikechi Winifred Nneka, Ogbeihe Geraldine Ogom, Omoregha Charles Uwaifiokun, Nnaemeka Louis Benedict

Journal of Pharmaceutical Research International, Page 241-248
DOI: 10.9734/BJPR/2015/13407

Aim: Tetracarpidium conophorum is a climbing shrub grown principally for its leaf, root, fruit and nut in Southern Nigeria and Western Cameroon. This study was conducted to assess the liver function status in alloxan- induced diabetic rats treated with methanol extracts of leaf and root of Tetracarpidium conophorum.
Methodology: The leaf and root extracts of Tetracarpidium conophorum were obtained using Soxhlet extractor and diabetes was induced by intraperitoneal injection of alloxan (100mg/kg). Plasma levels of glucose, alkaline phosphatase (ALP), alanine aminotransferase (ALT) and aspartate aminotransferase (AST) were estimated using standard diagnostic kits and procedures.
Results: The results from this study show significant (P<0.001) elevation of ALP, AST and ALT levels in alloxan- induced diabetic rats. Oral administration of leaf and root extracts of Tetracarpidium conophorum for 14 days significantly (P<0.001) lowered diabetic induced serum liver enzyme levels.
Conclusion: The present results indicate that the leaf and root extracts of Tetracarpidium conophorum possess potent antidiabetic and hepatoprotective activities and could be exploited in the development of antidiabetic and hepatoprotective drugs.

Open Access Original Research Article

Effect of Ethyl Acetate Extracts from Peel of Citrus decumana and Citrus aurantifolia on Aspirin Induced Gastric Ulcer in Mice

E. C. Egwim, R. U. Hamzah, Aberuagba Adepeju

Journal of Pharmaceutical Research International, Page 249-259
DOI: 10.9734/BJPR/2015/6674

Aims: The present study is aimed at investigating the antiulcer activity of ethyl acetate extract of Citrus decumana (grapefruit) and Citrus aurantifolia (lime) peels.
Study Design: Animals were divided into six groups of six animals each as follows;
• Group EtCD: Ulcer was induced and treated with Citrus decumana peel extract.
• Group EtCA: Ulcer was induced and treated with Citrus aurantifolia.
• Group EtCD + EtCA: Ulcer was induced and treated with Citrus decumana + Citrus aurantifolia.
• Group Ranitidine: Ulcer was induced and treated with Ranitidine.
• Group Ulcer: Ulcer was induced but not treated.
• Group Normal: Ulcer was not induced.
Place and Duration of Study: Department of Biochemistry, Federal University of Technology, P.M.B 65, Minna Niger State, Nigeria.
Methodology: Ethyl acetate extracts of dried peel powder of Citrus decumana and Citrus aurantifolia were obtained using reflux. Phytochemical screening was done on the extracts to determine their chemical constituents. Ulcer was induced in six groups of mice by oral administration of aspirin. The mice were treated by oral administration of ethyl acetate extract of Citrus decumana and Citrus aurantifolia. The antiulcerogenic activity was evaluated in aspirin induced ulcerogenic mice models at a dose of 400 mg/kg. Ulcerative indexes as well as oxidative stress markers like thiobarbituric acid reactive species (TBARS), Superoxide dismutase (SOD) and Catalase activity (CAT) in the plasma and gastric tissue were measured in all groups to study the possible involvement of antioxidants with gastro protection.
Results: Pretreatment of animals with ethylacetate extracts of Citrus decumana and Citrus aurantifolia peel showed a significant decrease in ulcerative index and TBARS Level in both plasma and gastric tissues compared to the control. Although all the treatment groups showed a significant increase in SOD and CAT concentration in plasma and gastric tissue, Citrus decumana extract showed a more significant increase in the concentration of SOD when compared to all other groups.
Conclusion: This study indicates that Citrus decumana and Citrus aurantifolia peel may be used as a natural therapeutic agent in the treatment of ulcers.

Open Access Original Research Article

In vitro and in vivo Studies of Repaglinide Fast Dissolving Tablet Utilizing Solid Dispersion Techniques

Dalia Abdel-Rhman Attia

Journal of Pharmaceutical Research International, Page 260-279
DOI: 10.9734/BJPR/2015/14739

Repaglinide according to the biopharmaceutics classification system is considered as class II drug, which suffers from low aqueous solubility and hence, low bioavailability. The current study concerned with improvement of the aqueous solubility and dissolution rate of repaglinide by using solid dispersion techniques with different polymers. Moreover, fast-dissolving tablets of repaglinide solid dispersion with superdisintegrant were formulated to enhance the repaglinide bioavailability. In the present study, solid dispersion formulae of repaglinide were prepared by utilizing different polymers namely polyethylene glycol 6000, mannitol and urea in various drug: polymer ratio (1:1, 1:3, 1:5, 1:10) by using melting and solvent evaporation methods. The solubility of repaglinide in different carriers was estimated, and solid dispersions were prepared and characterized. The drug release profile was carried out in phosphate buffer 6.8 using USP type I dissolution apparatus. From the above studies, it was found that the fusion method shows the better enhancement of dissolution in comparison to the solvent evaporation method. Among carriers used and based on the in vitro release study, the faster drug release appeared from solid dispersion prepared with urea in ratio 1:10. The increase in dissolution rate of repaglinide was confirmed by X-ray diffraction spectral studies of its solid dispersion which showed a significant decrease in drug crystallinity. The absence of interactions between drug and polymer was confirmed by differential scanning calorimetry and Fourier transform infrared spectroscopy studies. In addition, formula repaglinide solid dispersion FU10 was selected to develop a fast dissolving tablet that disintegrates rapidly and releases the maximum amount of repaglinide using Ac-Di-Sol as superdisintegrant. The prepared batches of tablets were tested for mechanical strength properties (hardness and friability), weight variation, disintegration, drug content and in vitro dissolution studies. Furthermore, pharmacokinetic studies with the selected fast dissolving tablet of repaglinide in solid dispersion were conducted on human volunteers. The fast dissolving tablet is a promising formulation for repaglinide that results in higher solubility, a rapid onset of action, and enhanced systemic bioavailability. 

Open Access Original Research Article

Use of Xanthan Gum in the Formulation of Diethylcarbamazine for Targeted Drug Delivery

Clement Jackson, Martins Emeje, Sabinus Ofoefule

Journal of Pharmaceutical Research International, Page 280-285
DOI: 10.9734/BJPR/2015/14412

Matrix tablets were prepared using xanthan gum (XG) and Diethylcarbamazine was used as model drug. The controlled release of the drug by the polymer matrices in the upper gastrointestinal tract (GIT) was assessed through release studies carried out in the presence and absence of rat caecal content. Desired release profile was noted with Diethylcarbamazine batch with Xanthan gum 30% and 40% (XG3 and XG4.). Presence of Xanthan gum in relatively higher concentration in the tablets delayed the initial release of drug from the matrices due to swelling and consequent exposure to effect of polysaccharidases in the colon. XG3 and XG4 released the drug by zero order kinetics through non fickian mechanism. Drug release in dissolution medium with rat cecal content was significantly (P<0.05) different from the control (without rat cecal content) for the optimized formulations of Diethylcarbamazine tablets. 

Open Access Review Article

TNF-α Inhibitor Treatment for Crohn’s Disease: Comparative Review of Post Therapy Malignancy between Infliximab and Adalimumab

Danil Hammoudi, Adekunle Sanyaolu, Nirav Nagarsheth, Jason Kimbel, Amos Abioye

Journal of Pharmaceutical Research International, Page 217-227
DOI: 10.9734/BJPR/2015/12381

The association between chronic inflammatory disease and cancer has been well established through years of research. In corollary, progressive resistance to chimeric monoclonal antibodies has been reported in literature. The purpose of this investigation was to establish the overall trend of the chimeric monoclonal antibody (Infliximab) failure compared with human monoclonal antibody (Adalimumab). It was opined that this failure may result in subclinical yet cancer-inducing inflammation that could be measurable in patient populations undergoing the therapy by examining cancer prevalence. An overall trend of increased incidence of new malignancy in patient populations on Infliximab compared with Adalimumab was confirmed from the literature reviewed. There was also a significant trend of developing Gastrointestinal (GI) related cancer in patients on Infliximab, which corresponds with the majority of the progression process in Crohn’s disease. It was opined that future observations in clinical practice will lead to the phasing out of Infliximab as a front-line monoclonal antibody in the treatment of Crohn’s disease in favor of less immunogenic monoclonal antibodies. In conclusion an increased incidence of both general and GI malignancies has been widely reported in patient populations undergoing Infliximab therapy than with Adalimumab.