Open Access Original Research Article

Batch Equilibrium, Kinetics and Thermodynamics Study of Sulfamethoxazole Antibiotics Onto Azolla filiculoides as a Novel Biosorbent

Davoud Balarak, Ferdos Kord Mostafapour

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/28521

Azolla filiculoides (AF) were used as adsorbent for the sorption of Sulfamethoxazole (SMZ) from aqueous solution. Also adsorption Isotherms, kinetics and thermodynamics were studied. Experiments were conducted by varying parameters such as contact time, agitation speed, initial SMZ concentration and temperature. Adsorption isotherms models including Langmuir, Freundlich and Temkin were tested. It was inferred that the Langmuir models (with very high R2 values) were most suited to describe the sorption of SMZ in aqueous solutions. The experimental data were fitted into the following kinetic models: Pseudo-first-order, pseudo-second-order, and the intraparticle diffusion model. It was observed that the pseudo-second-order kinetic model described the adsorption process better than other kinetic models. Thermodynamic parameters including the Standard free energy changes (△G), standard enthalpy change (△H), and standard entropy change (△S) were calculated. This parameters indicated that the adsorption of SMZ onto AF biomass was feasible, spontaneous and endothermic. This study revealed that AF biomass is a good adsorbent for the elimination of Sulfamethoxazole antibiotics from aqueous solution.

Open Access Original Research Article

Synthesis and Investigation of Mutagenic and Genotoxic Effects of Some 2-hydroxy-1,4- Naphthoquinone Derivatives by Ames and Comet Assay

Recep Liman, Ibrahim Hakkı Ciğerci, Oğuzhan Alagöz

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28651

In this study, mutagenic and genotoxic effects of novel 2-hydroxy-1,4-naphthoquinone (1) derivatives, 2-phenyl-2-(2-thiophenyl)-2,3-dihydronaphtho[2,3-b]furan-4,9-dione (3) and 2-hydroxy-3-[(E and Z)-2-phenyl-2-(2-thiophenyl)ethenyl]naphthalene-1,4-dione (4) were investigated by using bacterial reverse mutation assay in Salmonella typhimurium TA98 and TA100 strains with or without metabolic activation system (S9 mix) and comet assay in haploid Saccharomyces cerevisiae BY4741 (MATa his3Δ1 leu2Δ0 met15Δ0 ura3Δ0), respectively. Derivatives, 3 and 4 were dissolved in dimethyl sulfoxide (DMSO) for all test systems. Five non-cytotoxic concentrations of the derivatives were tested in two parallel independent experiments in Ames test. Ames test did not show mutagenicity of test compounds. Two different concentrations (50 µg/m L and 100 µg/mL) of 3 and 4 were applied to S. cerevisiae cells. It was found that test materials did not show genotoxic effect. While all of the 4 and 100 mM of concentration 3 showed protective effect, all of the 1 and 50 mM of 3 did not show a protective effect against the DNA damage generated by H2O2.

Open Access Original Research Article

Memory Enhancing Activity of Dendrobium macraei Lindl. in Swiss Albino Mice

Esha Vatsa Vatsa, Kundan Singh Bora

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/BJPR/2016/28090

Background: Memory is not a single process, but rather a series of interactive processes beginning when we are exposed to new information, which is registered by the brain, encoded, and in the right conditions, stored for later retrieval. Short and long term memory loss may result from deteriorating cerebral mechanisms due to different causes having impact on the quality of life. Memory enhancers can improve thinking, memory, and alertness in people with Alzheimer’s disease or dementia that affect the mind or memory.

Objective: In the present study, an attempt has been made to highlight the importance of the plant Dendrobium macraei Lindl. (family- Orchidaceae) in the field of traditional medicines which is traditionally used as memory enhancer.

Methods: The present study comprises in vivo memory enhancing activity evaluation in mice using various memory models such as elevated plus maze model and Morris water maze model. Piracetam was used as standard drug. Effects of various extract viz. petroleum ether, chloroform, ethyl acetate, methanol and aqueous extract of D. macraei were evaluated for memory enhancing activity.

Results and Conclusion: Amongst all extracts tested, only ethyl acetate and methanol extract of D. macraei showed significant short term and long term memory enhancing activity using elevated plus maze model and Morris water maze model in mice respectively. Ethyl acetate extract (200 mg/kg, p.o.) showed marked significant (P<0.05) effect as compared to methanol extract (200 mg/kg, p.o.) in both the models. Therefore, it would be worthwhile to explore the potential of this plant in the management of dementia.

Open Access Original Research Article

Rumex usambarensis (Dammer) Leaf and Stem Extract Effect on Body Weight and Lipid Profile: A Study in Albino Rats

Nattabi Hilda, Nkwangu David, Ogwang Patrick Engeu

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/BJPR/2016/27409

Aims: The aim of the study was to determine the effect of Rumex usambarensis plant extract on body weight and lipid profile of fattened albino rats.

Study Design: This was an in-vivo experimental study in laboratory animal model.

Place and Duration: The study was conducted at the Faculty of Medicine, Mbarara University of Science and Technology, Uganda, from January to May 2015.

Methodology: Rumex usambarensis stems and leaves were collected from Kabale district in western Uganda during rainy season for the study while one whole plant was brought to the university for authentication by a university botanist. The fresh stems and leaves weighing 8.1 kg were blended in 1.045L of distilled water and filtered through a muslin cloth before evaporating in an oven set at 55°C to a constant weight of dry mass. A portion of the dry mass was screened for presence of phytochemicals groups while the remaining portion was dissolved in distilled water and administered to fattened wistar albino rats at the doses of 125 mg/kg, 250 mg/kg and 500 mg/kg corresponding to group 1, 2 and 3 respectively daily by gavage for 21 days. The Control group received equivalent volume of distilled water by gavage daily. Mean body weights at baseline and at day 21 were statistically compared using ANOVA followed by sidak statistical test at p=0.05. Lipid profiles obtained on day 21 were also compared using the same statistical tests.

Results: Rumex usambarensis extract significantly reduced body weight of fattened rats from baseline at all the doses tested i.e 338.7±141.4 Vs 323.4±135, p=0.03, for 125 mg/kg dose, 335.9±140.1 Vs 322.7±134.6, p=0.03 for 250mg/kg dose, 339.1±141.5 Vs 324.7±135.6, p=0.03 for 500 mg/kg dose while the control group had no significant change in body weight i.e 338.7±141.3 Vs 338.3±141.1, p=0.35.The extract groups at lower dose levels had significantly higher High Density Lipoprotein level i.e. 29.1±4.8 for 125 mg/kg dose (p= 0.002) and 29.1±6.8 for 250 mg/kg dose 4 (p=0.03) compared to 21.4±5 for the control group and 25.1±6.5 for the 500 mg/kg group.

Conclusion: Rumex umsambarensis extract decreased weight of fattened animals and may be useful in reduction of body weight in overweight and obese persons.

Open Access Original Research Article

Pharmacoeconomic Analysis of Direct Activity Antiviral Drugs Used for Treatment of Genotype 1 Chronic Hepatitis C

N. Z. Musina, A. G. Savilova, O. M. Korzinov

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/27144

Aims: Hepatitis C is one of the most important global health care problems. The goal of this study was to perform a pharmacoeconomic analysis of therapeutic schemes used in treatment of patients with genotype 1 chronic HCV by using direct-acting antiviral agents in combination with pegylated interferons and ribavirin.

Study Design: In the current study comparison of therapeutic schemes used in treatment of patients with genotype 1 chronic HCV by using direct-acting antiviral agents in combination with pegylated interferons and ribavirin was made.

Place and Duration of Study: Moscow Institute of Physics and Technology (State University), Department of Biological and Medical Physics, Laboratory of government programs and development projects in life sciences (April 2015 - November 2015).

Methodology: In the current study Markov decision process model was built in order to assess long-term costs and efficacy of preparations under study. Comparison of therapeutic schemes for chronic HCV infection treatment was performed with the use of cost-effectiveness and cost-utility analysis. In costs-effectiveness analysis, therapeutic schemes for CHC treatment that include telaprevir, boceprevir and simeprevir, life years gained (LYG) and quality adjusted life years (QALY) served as a criterion of benefit in costs-effectiveness and cost-utility analysis respectively.

Results: Pharmacoeconomic analysis of treatment of chronic hepatitis C viral infection showed that the best combination of costs and effectiveness was observed in combined treatment with the use of pegylated interferon, ribavirin and boceprevir in treatment-naïve patients as well as patients with unsuccessful treatment experience.

Conclusion: Our results showed that combined therapy with the use of boceprevir is the most pharmacoeconomically justified in comparison with telaprevir and simeprevir-based treatment.

Open Access Original Research Article

Evaluation of Novel Solid Lipid Microparticles Drug Delivery Systems for Oral Delivery of a Herbal Antidiabetic Extract

Mumuni A. Momoh, Musiliu O. Adedokun, Jameelu Muazu

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/8168

Aim: The aim of the present study was to prepare and evaluate a novel multiparticulate pharmaceutical formulation of Vernonia amygdalina extract suitable for oral administration.

Study Design: Solid lipid microparticles (SLMs) of Vernonia amygdalina aqueous extract and evaluate in vivo

Place and Duration of Study: Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria Nsukka, between October 2011-2013.

Methods: Phospholipon® 90H and Homolipid (HLP) from Capra hircus were used to prepare solid lipid microparticles (SLMs) of Vernonia amygdalina (VA). The SLMs were characterization based on size, morphology, stability and encapsulation efficiency (EE%). In vitro release was performed in phosphate buffer while the antidiabetic properties of the SLMs were evaluated in alloxan- induced diabetic rats.

Results: There was a dose dependent increase in EE% irrespective of the type of matrixing agents used. Generally, the batches containing 400 mg VA (A1-A3) had higher EE (79.24, 81.42 and 89.16%) than those containing 200 mg VA (B1-B3; 72.19, 73.09 and 84.21%). The ratio of Phospholipon® 90H and Homolipid determined the EE% of the formulation. The formulations are stable, the particle size range 38.1 µm to 81.1. The release of VA in phosphate buffer varied widely with the lipid contents. Moreover, significant antidiabetic (p<0.05) properties were observed in all the VA-loaded SLM formulations.

Conclusion: The SLMs-based formulations would likely offer a more effective means of delivering Vernonia amygdalina, a natural extract with good antidiabetic activities as compared to the traditional way of taking the extract orally.

Open Access Original Research Article

In vivo Anti-trypanosomal Evaluation and Phytochemical Analysis of Methanol Extract of Nauclea latifolia

C. E. Ugwu, I. O. Ezeh, N. C. Obitte, S. A. Chime, C. O. Agubata

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/27249

Aim: Trypanosomiasis is a pathological condition that requires serious attention. The dried root of Nauclea latifolia was investigated to determine the anti-trypanosomal activity on groups of Wistar rats.

Methods: A 1000 mg/kg body weight of methanol extract was administered for 7 consecutive days by intraperitoneal route (ip) to Group II while Group I received a 3.5 mg/kg of Samorinil® through the same route. The phytochemical constituents were also determined. Parasitaemia level, body weight, temperature and packed cell volume (PCV) were monitored and determined before and after the commencement of the experiment.

Results: The packed cell volume (PCV) increased significantly (P = .05) in Group I and II post infection from an average of 35.0 ± 0.68 to 38.05 ± 0.32% when compared to the infected - untreated group (Group III) with a PCV value of 30.0 ± 1.11%. The methanol extract at a concentration of 1000 mg/kg of the plant reduced the parasitaemia level from 7.8 to 2.53 trypanosomes per ml at the end of the experiment. In Group I, the positive group, that received commercial drug (diminazene diaceturate (Samorinil®) was aparasitic before the end of the experiment. There was significant weight improvement (p =.05) in the entire Group (I and II) from  ̶  22 ± 0.01 to 4.4 ± 0.30 g and   ̶  2.4 ± 0.20 to 4.1 ± 0.04 g respectively except the Group III that was untreated with  ̶  2.4 ± 0.34 to  ̶  6.6 ± 0.18 g that kept depreciating postinfection. First death was recorded in Group III on 12-day post-infection. Temperature of G III continued to increase slowly as the parasitaemia level increased from 35.22 to 42 .36°C which significantly varied (p =.05) from the rectal temperature of GI and II from 35.85°C and 35.17 to 35.53°C and 34.40°C.

Conclusion: The experiment showed that a 1000 mg/kg methanol extract of Nauclea latifolia exhibited promising trypanocidal activity against T. brucei.