Open Access Original Research Article

Signal Detection and Clarification of Peripheral Neuropathy and Guillain-Barré Syndrome Associated with Exposure to Systemic Fluoroquinolones

Ayad K. Ali

Journal of Pharmaceutical Research International, Page 407-417
DOI: 10.9734/BJPR/2014/6954

Aims: Peripheral neuropathy (PN) is an identified risk of systemic antibacterial therapy with fluoroquinolones. The risk and its severity, including the development of Guillain-Barré syndrome (GBS) between individual agents is uncertain. This study examines the association between fluoroquinolones and PN and GBS in cases spontaneously reported to the FDA Adverse Event Reporting System (FAERS).
Study Design: Retrospective pharmacovigilance analysis.
Place and Duration of Study: Cases submitted to FAERS between 1997 and 2012.
Methodology: The MedDRA Preferred Term was used to define PN and GBS. Individual fluoroquinolones were identified by generic names and route of administration. Empirical Bayes Geometric Mean (EBGM) with 95% confidence interval (EB05-EB95) was calculated as disproportionality measure. Safety signals with EB05>2 was considered a significant disproportional increase in event reporting of at least twice times higher than expected.
Results: There were 539 PN reports out of 46,257 adverse event reports submitted for fluoroquinolones. 9% of PN reports were for GBS. Significant disproportionality of PN (EBGM 2.70; EB05-EB95 2.51-2.90) and GBS (EBGM 3.22; EB05-EB95 2.55-4.02) was identified for fluoroquinolones. Signals of PN were detected for ciprofloxacin (EBGM 3.24; EB05-EB95 2.87-3.66) and levofloxacin (EBGM 3.36; EB05-EB95 3.02-3.72). A GBS signal was detected for ciprofloxacin (EBGM 4.15; EB05-EB95 2.94-5.74). GBS and PN respectively ranked 6th and 8th among reported neurological events.
Conclusion: This study reemphasizes the link between fluoroquinolones and PN, and shows potential association with more severe forms of nerve damage, e.g. GBS. Unless the benefit of fluoroquinolone therapy outweighs PN risk, treatment with alternative antibacterial agents is recommended.

Open Access Original Research Article

UV Spectrophotometric Method for the Simultaneous Determination of Desloratidine and Pseudoephedrine HCl in Combined Dosage Form

K. Hussain Raviteja, Mahesh Nasare, V. V. L. N. Prasad, Prakash V. Diwan

Journal of Pharmaceutical Research International, Page 418-428
DOI: 10.9734/BJPR/2014/5615

Aims: UV Spectrophotometric Method for the Simultaneous Determination of Desloratidine and Pseudoephedrine HCl in combined Dosage form.
Study Design: A simple, rapid and specific UV spectroscopic method with good sensitivity was developed and validated for the simultaneous determination of Desloratidine and Pseudoephedrine HCl in bulk and pharmaceutical dosage form.
Place and Duration of Study: Department of pharmaceutical Analysis & Quality Assurance, School of Pharmacy, Anurag Group of Institutions, Venkatapur, R.R Dist, Andhra Pradesh, India during February 2013 and April 2013.
Methodology: Vierodt’s (Simultaneous equation) method was performed for Estimation of Desloratidine and Pseudoephedrine HCl in Pharmaceutical dosage form.
Results: In Ethanol the λmax of Desloratidine and Pseudoephedrine HCl was fixed as 240 and 258 nm respectively using a Shimadzu UV-Visible spectrophotometer. In this proposed method both drugs obeyed linearity within the concentration range of 5-30 μg/ml and 80-800 μg/ml for Desloratidine and Pseudoephedrine HCl respectively. The low RSD values indicate good precision and high recovery values indicate accuracy of the proposed method. The proposed method has been applied to the determination of drugs in commercial formulations. Assay results were in good agreement with label claim. The method was validated as per ICH guidliness.
Conclusion: The developed method was simple, accurate, precise, specific, sensitive and reproducible which can be efficiently and easily applied to pharmaceutical dosage forms

Open Access Original Research Article

Effects of Momordica charantia on Serum Lipid Profile, Serum Protein Levels and Selected Markers of Cardiovascular Damage in Diabetic Rats

Omobola A. Komolafe, David A. Ofusori, Olarinde S. Adewole, Julius B. Fakunle

Journal of Pharmaceutical Research International, Page 429-442
DOI: 10.9734/BJPR/2014/5320

Aims: To investigate the effects of M. charantia on serum lipid profile, serum protein concentration and selected markers of cardiovascular damage in streptozotocin-induced diabetic Wistar rats.
Study design: Forty healthy adult Wistar rats of both sexes were randomly assigned into five groups A, B, C, D and E of eight rats each.
Place and Duration of Study: Department of Anatomy and Cell Biology, Obafemi Awolowo University, Nigeria, between January 2010 and March 2012.
Methodology: At the expiration of the research, the animals were sacrificed and blood samples were collected for biochemical analysis. Serum lipid profile, total protein and serum albumin, serum Creatine Kinase, Lactate Dehydrogenase and Glucose-6-Phosphate Dehydrogenase activities were determined using Randox assay kits. The levels of Serum globulin and albumin/globulin ratio were calculated. Serum nitric Oxide and Prostaglandin E2 levels were determined using assay kits.
Results: The result showed a significant reduction (p<0.05) in the blood glucose levels in group D when compared with groups A, B, C and E. There was an increase in triglyceride (p<0.05), total cholesterol (p>0.05), low density lipoprotein (p>0.05) and very low density lipoprotein cholesterol (p<0.05) were increased in group B when compared with group D. The serum levels was presented a non significant reduction in total protein (p>0.05), albumin (p>0.05), globulin (p>0.05) and albumin/globulin ratio (p>0.05) when group B was compared with group D. Lactate dehydrogenase (F=0.18, p>0.05) and creatinine kinase (F=1.96, p>0.05) were increased (p>0.05) while the nitric oxide (F=2.21, p<0.05), PGE2 (F=1.25, p<0.05) and G6PDH (F=2.92, p<0.05) were reduced (p<0.05) in group B when compared with A, C, D and E.
Conclusion: The presents study thus suggests that M. charantia could serve as a useful antidiabetic agent.

Open Access Original Research Article

In vitro Cytotoxic Activity of Hydro Ethanolic Extract of Delonix regia (Bojer ex. Hook.) Flowers on Cancer Cell Lines

Madan R. Pusapati, Tejaswi Jonnalagadda, Phani K. Kola, Ankamma C. Yarlagadda, Girijasankar Guntuku

Journal of Pharmaceutical Research International, Page 443-452
DOI: 10.9734/BJPR/2014/5746

Aims: To evaluate the In vitro cytotoxic effects of the hydro ethanolic extract (HEE) of the Delonix regia flowers against different cell lines.
Methodology: The dried Delonix regia flowers are subjected to soxhlet extraction by using 70% ethanol. The dried extract was used to determine the qualitative preliminary phytochemical analysis, total phenolic and flavonoid content. The cytotoxic property of the extract was determined by using MTT assay against breast cancer (MCF-7), cervix (HeLa), brain and colon cancer cells. Tamoxifen is used as a standard for all the cell lines.
Results: Qualitative phytochemical tests of extract HEE showed the presence of sugars, flavonoid, tannins, phenolic compounds, steroids and saponins. The percentage of phenolic and flavonoid content was determined as 31.42 mg/g, 29.22 mg/g respectively. The cytotoxic activity of the extract showed, IC50 concentrations (μg/ml) against MCF-7 (breast), carcinoma of cervix HeLa cells, carcinoma of the brain, and carcinoma of colon cells against tamoxifen are 141.6 ± 0.08, 223.7 ± 2.16, 173.9 ± 0.7, 168.33 ± 0.04 respectively.
Conclusions: The experimental data clearly demonstrate the hydro ethanolic extract (HEE) showed cytotoxic properties against human cancer cells.

Open Access Original Research Article

Preparation and Characterization of Polymeric Mucoadhesive Film for Buccal Administration

Ramy B. Gales, Hassan M. Ghonaim, Ahmed R. Gardouh, Mamdouh M. Ghorab, Sabry S. Badawy

Journal of Pharmaceutical Research International, Page 453-476
DOI: 10.9734/BJPR/2014/5399

Objectives: Buccal films consist mainly of polymer that has a good mucoadhesive profile and plasticizer. A lot of polymers and plasticizers can be used to configure the mucoadhesive films as hydroxyethyl cellulose and glycerin respectively.
Material and Methods: Films prepared by dispersing the polymer, mixing it with plasticizer and pouring it in Petri dishes to be dried and cut finally. Physicochemical tests were used to evaluate the films. These tests are organoleptic evaluation and polymer and plasticizer selection, determination of rheological properties of polymers, film thickness, and determination of moisture content, determination of moisture uptake and evaluation of mechanical properties.
Results and Conclusions: It was found that films prepared from polyvinyl alcohol 2% (w/w) especially with the addition of propylene glycol 20% from the weight of the polymer have excellent characteristics. This formula has promising organoleptic and mechanical properties and its solution is Non-Newtonian pseudoplastic. Moreover, this formula is very thin and has moderate percent of moisture content and moisture uptake. Also, it has high elongation with moderate tensile strength. As a result, it is better to prepare the film by these ingredients to obtain an ideal mucoadhesive formula.

Open Access Original Research Article

Exploration of the Angiogenic Potential of Honey

R. M. Munshi, S. S. Bhalerao, S. A. Kalekar, T. A. Patil

Journal of Pharmaceutical Research International, Page 477-489
DOI: 10.9734/BJPR/2014/6930

Aims: The present study was conducted to confirm the angiogenic potential of honey using Chick Chorioallantoic Membrane (CAM), an in ovo model and to study its effect on Vascular Endothelial Growth Factor (VEGF) expression in the CAM tissue. Attempts were also made to identify the probable active constituents present in honey that contributed to its angiogenic potential.
Methodology: Honey was evaluated over concentrations ranging from 0.015 to 25% v/v and the extent of angiogenesis was quantified using stereomicroscopy. VEGF expression at transcript level was determined by RT-PCR. Erythropoietin and Heparin were used as positive and negative controls respectively. Four known constituents of honey viz., Glucose, Proline, Vitamin C and Hydrogen peroxide were tested by biochemical methods.

Results: New blood formation was seen at all the concentrations tested, however the pro-angiogenic effect was greater at lower concentrations. These results were significantly greater than that seen with erythropoietin, the positive control. VEGF mRNA expression in CAM tissue also demonstrated similar findings. Among the constituents tested, Vitamin C and Hydrogen peroxide were observed to be associated with the angiogenic effect of honey.
Conclusion: The study thus confirms the pro-angiogenic potential of honey at low concentrations. This effect is probably due to the presence of Hydrogen peroxide and Vitamin C and is mediated via alteration in VEGF expression.

Open Access Original Research Article

Formulation and Characterization of Nystatin-loaded Nanostructured Lipid Carriers for Topical Delivery against Cutaneous Candidiasis

Rawia M. Khalil, A. Abd-Elbary, Mahfouz A. Kassem, Mohamed S. El Ridy, Mona M. Abou Samra, Ghada E. A. Awad, Soheir S. Mansy

Journal of Pharmaceutical Research International, Page 490-512
DOI: 10.9734/BJPR/2014/7055

Aims: The objective of the current study was to formulate nystatin (Nyst) into nanostructured lipid carriers (NLCs) to enhance its antifungal activity.
Place and Duration of Study: Department of pharmaceutical technology, national research centre, Egypt, between mars 2011 to april 2013
Methodology: Nyst loaded NLCs (NYST-NLCs) were prepared by the hot homogenization and ultrasonication method followed by evaluation of its topical effect on the cutaneous candidiasis. The prepared Nyst-NLCs were characterized for entrapment efficiency, particle size, zeta potential, morphology (transmission electron microscopy), thermal characterisation (differential scanning calorimetry) and in vitro drug release. The study design involves the investigation of the effect of three independent variables namely liquid lipid type (Miglyol 812 and Squalene), liquid lipid concentration (30 and 50%) and Nyst concentration (0.125 and 0.25%). A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans.
Results: NLC dispersions were spherical in shape with particle size ranging from 68.06±6.56 to 141.8±3.33 nm. The entrapment efficiencies ranged from 45.50±2.34 to 92.73±0.33% with zeta potential ranging from -26.2 to -39.2 mV. The stability studies done for 6 months indicated that Nyst-NLCs were stable for more than 6 monthes.the microbiological studies showed A least number of colonies forming units (cfu/ml) were recorded for the selected Nyst-NLCs compared to the drug solution and the Nystatin® cream present in the market.
Conclusion: It can be fulfilled from this work that NLCs represent promising carrier for topical delivery of Nyst offering good physical stability, high entrapment efficiency and controlled drug release. Nyst-NLCs are a good candidate for cutaneous treatment of fungal infection.

Open Access Original Research Article

Antibacterial Screening of Some Synthesized Palmitoyl Amino Acids and Their Aromatic Analogues

Haruna Baba, Cyril O. Usifoh, Adebola Onanuga

Journal of Pharmaceutical Research International, Page 513-519
DOI: 10.9734/BJPR/2014/6063

Aims: The aims of the research were to synthesize, characterize some palmitoyl amino acids and their aromatic analogues and to screen the synthesized compounds for possible antibacterial activity
Study Design: Synthesis, characterization and antibacterial screening of palmitoyl amino acids and their aromatic analogues.
Place and Duration of Study: Department of Pharmaceutical and Medicinal Chemistry/ Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmacy, Niger Delta University, Wilberforce Island, between September 2012 and January 2013.
Methodology: Palmitoylchloride was condensed with the respective amino acids (glycine, β-alanine, γ-amino butyric acid) to form the corresponding palmitoyl amino acids. The opening of the isatoic anhydride ring with the three amino acids and subsequent condensation with palmitoyl chloride led to the formation of the amino acid benzamides. The antibacterial screening was carried out using agar well diffusion method.
Results: All the synthesized compounds were obtained in good yield and high purity; they were unequivocally characterized by the combination IR, 1H NMR, 13C NMR and MS. The compounds were however found to possess no antibacterial activity against the tested microorganisms
Conclusion: This work has shown that both the straight chain and aromatic analogues of saturated long chain lipid amides are inactive against the tested strains of microorganism.

Open Access Original Research Article

Dose Response of Viola odorata on Meiotic and Mitotic Chromosomes of Vicia faba

Monika Asthana, Avnish Kumar

Journal of Pharmaceutical Research International, Page 520-530
DOI: 10.9734/BJPR/2014/5998

Aims: Viola odorata is a medicinally important plant. It contains bioactive principle viz violin and probably methyl salicylic ester.The present study was designed to analyze the effect of different doses of this medicinal plant extract on meiotic and mitotic chromosomes of Vicia faba.
Study Design: In this study, different concentrations (5, 10, 20, 30, 40, & 50 %) of Viola odorata extract were applied for 4, 8, 12 and 24h on Vicia faba plant. Effect of these concentrations was studied on the meiotic and mitotic chromosomes. Gesticulate negative activity of herbal medicine was observed under the effect of different concentrations of the extract.
Place and Duration of Study: The extract of Viola odorata was prepared in the laboratory. Study was performed from January, 2011 to December, 2012.
Methodology: Flower bud treatment method was applied for meiotic analysis and seed soaked & root tip treatment methods were used for mitotic analysis. Mitotic and meiotic chromosome indicated various abnormalities against different doses. Cytotoxicity was inferred when the Mitotic index (dividing cells/1000 scored) of treated cells was significantly different (P<0.05) from control.
Results: The percent of their abnormalities increase with increasing dose (5-50%) and time (4-24 hours) dependent. Low dose treatment of buds caused increase in mitotic index. Treated roots were found negatively affected with no exception and found more harmful and effective compared to seed soaked treatment. Stickiness was more frequent than other abnormalities.
Conclusion: Vicia faba chromosome analysis is indicative of clastogenic action of Viola odorata. Thus, results of the present study suggest the doses of Viola odorata extract to verify the toxic properties before using for treatment.

Open Access Original Research Article

Wound Healing Activity of Ethanol Leaf Extract of Erythrina senegalensis

E. E. Ilodigwe, B. E. Okonkwo, C. A. Agbata, D. L. Ajaghaku, P. M. Eze

Journal of Pharmaceutical Research International, Page 531-540
DOI: 10.9734/BJPR/2014/7260

Aim: This study investigates the wound healing activity of ethanol leaf extract of Erythrina senegalensis using excision wound model on albino rats.
Methodology: Several herbal extract formulations were prepared with Petroleum Jelly ointment base. Cicatrin® powder (neomycin-bacitracin) was used as the positive control. The various ointment formulations were applied topically on the wounds daily for 21 days. Daily wound contraction and epithelialisation times were recorded for each group. The antibacterial activity of the extract was also evaluated against some bacteria species implicated in wound infections. The following test organisms were used: Staphylococcus aureus, Pseudomonas aeruginosa, klebsiella pneumoniae and Escherichia coli.
Results: The Phytochemical analysis revealed that alkaloids were abundant in the extract. The herbal ointment at various concentrations showed significant (P<.05) increase in percentage wound contraction on day 9 – 21 compared with the control group that received only the ointment base. The contraction produced by 40% w/w of the extract was similar to that of Cicatrin® powder on day 6 – 21. The results also revealed significant (P<.05) reduction in epithelialisation time exhibited by the extract treated animals compared to those of the control group. The result of antimicrobial studies showed that the extract inhibited the test organisms at concentrations ranging from 200 to 12.5 mg/mL. The Minimum Inhibitory Concentrations (MICs) of the extract on the test isolates was recorded at 25mg/mL for both S. aureus and E. coli and 6.25mg/ml for K. pneumoniae. P. aeruginosa showed no susceptibility to both the extract and the control drug at the concentrations evaluated.
Conclusion: The marked reduction of wound size and epithelialisation time by the extract is an indication of its wound healing potentials. Also, the antibacterial activity of this plant against bacterial species implicated in wound infections may contribute to the enhanced wound healing activity.