Open Access Original Research Article

Prime Risk Factors to Act as Biomarkers for the Diagnosis of Myocardial Infarction

Manish Kr Verma, Pradeep Kumar, Anand Narayan Singh, Preeti Sharma, Suman Kumar, Desh Deepak Singh, Poonam Verma, Rachna Sharma

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/jpri/2021/v33i24B31435

Aims: This study was done to find out retrospective case-control with respect to myocardial infarction diagnosis on the basis of biochemical markers and lipid profile characteristics.

Design and Setting: This study was conducted at the Department of Biochemistry and sample collection at LPS Institute of Cardiology & Cardiac Surgery Department, Kanpur.

Methods: The total number of subjects participated in this study (n=178), of either sex (with age>65years) were included in this study from the case collected from Outpatient Department (OPD) and Indoor Patient Department (IPD) and control from patients attendant, which consisted of two subject groups: The group I: myocardial infarction (cases) n= 89 and Group II: Healthy Subjects (controls) n= 89. Laboratory methodology was performed to determine the prime important risk factors such as body mass index (BMI), blood pressure and lipid profile characteristics associated with myocardial infarction. Risk factors were analyzed by Chi-square and Pearson correlation, receiver operating characteristic (ROC) curve method considered significant when the critical, P <0.01level was set up, for a 95% confidence interval.

Results: Total number of (n=178) participants (males=65; mean age of 65 years, females=24, mean age of 58 years) at 95% CI were considered in this study, out of these, 89 individuals were expected to have risk of myocardial infarction (especially observed in case groups), and remaining 89 individuals were considered as control groups, all were included as, study subjects.

Conclusion: The current study concludes the importance of myocardial infarction in presence of prognostic inflammatory markers: higher IL-6 and plasma fibrinogen level, instead of high-sensitivity C-reactive protein, incase and control groups.

Open Access Original Research Article

Phytonutrients and Antimicrobial Activities of Methanolic Extract from Hafr Al-Batin Truffles

Ghassab M. Al-Mazaideh, Farhan K. Al-Swailmi

Journal of Pharmaceutical Research International, Page 13-21
DOI: 10.9734/jpri/2021/v33i24B31437

The desert truffle is a wild mushroom, also referred to as Kamah or Fagaa. Kamah is a rich source of polysaccharides that have medicinal, antitumoral, antibacterial, and immune-stimulant effects. Studies of hypogeous fungi, especially desert truffles, have recently entered traditional studies of epigeous higher Basidiomycetes. Based on the tasty desert truffle Kamah obtained from Hafr Al-Batin Governorate, Saudi Arabia, as a source of potential antimicrobial agents with both the aim of obtaining novel agents toward bacteria and Fungi of clinical significance. We specifically tested the antibacterial and antifungal efficacy of methanol extracts of Kamah against the Gram-negative bacterial pathogens reference strains E. coli ATCC® 8739, P. Aeruginosa ATCC®9027, S. aureus ATCC®6538, Enterococci NCTC®775 and opportunistic fungus C. albicans ATCC®1231.The extract had MIC (minimum inhibitory concentrations) varying from 100 g/ml to 500 g/ml against the pathogens examined. The LC-QTOF-MS (liquid chromatography coupled to quadrupole time of flight mass spectrometry) phytoconstituents assay chromatogram indicated that the methanol extracts of Kamah comprises 264 with retention periods varying from 1.04 to 18.86, which were categorized as unsaturated and saturated natural ingredients sch as aromatic compounds, carboxylic acids, oxygenated hydrocarbons, fatty acids, amino acids, and vitamins).The main compounds were discovered to be 21 with peak areas larger than 2X10-5 and retention periods varying from 2.3 to 9.13.The main known substances with the maximum peaks were adenosine (11.724), phenylalanine (7.711), phenprobamate (7.711), and 5-hydroxytryptophan (5.711). Such preliminary findings, we assume, are encouraging in terms of obtaining a beneficial antibiotic substitute to battle antibiotic-resistant pathogens especially eye infections.

Open Access Original Research Article

Population Awareness and Attitude towards First Aid in Burn in Makkah Al-Mukarramah, Saudi Arabia – A Cross Sectional Study

Arwa Fairaq

Journal of Pharmaceutical Research International, Page 22-29
DOI: 10.9734/jpri/2021/v33i24B31438

Background: Worldwide, an estimated 180, 000 deaths per year are caused by burns. Majority occur in low- and middle-income countries. Inadequate awareness of burn first aid has been reported in both developed and developing countries. In Saudi Arabia, studies reported inadequate level of knowledge of general population of first aid in burns emergencies including communities of Al-Madinah Al-Munawwarah, Jeddah, Riyadh, Majmaah and Hail.

Objective: we aim to assess the general knowledge and attitude regrading burn first aid among Makkah Al-Mukarramah population. Thus, the results of this study could help to understand the need of community to more implantation of Health Awareness Campaigns to help burn injuries managements.

Methods: A cross-sectional study was performed using an online survey. A total of 1390 participants completed the questionnaire from 15 February to 15 March 2019.

Results: Around 51.4% believed that washing burned area with cold water is the immediate first aid in 1st degree burns, 38.3% and 61.7% believed that going to the nearest emergency department is the immediate first aid in 2nd and 3rd degree burns, respectively. Around 46.7% agreed to remove the clothes stuck to the burned skin in case of burns , 34.5% applied traditional home remedy including toothpaste, honey, tomato paste or egg.

Conclusion: we found that population of western region have fair knowledge and attitude towards first aid in burns. However, traditional home remedy practice still present. Health Awareness Campaigns still needed to improve community attitude towards burn injuries managements furthermore.

Open Access Original Research Article

Formulation and Optimization of Zaltoprofen Loaded Ethosomal Gel by using 23 Full Factorial Designs

K. Anju, Sneh Priya, D. S. Sandeep, Prashant Nayak, Pankaj Kumar, Abhishek Kumar, Cynthia Lizzie Lobo, S. P. Krithi

Journal of Pharmaceutical Research International, Page 30-44
DOI: 10.9734/jpri/2021/v33i24B31439

Aim:The objective of the present study is to design and characterize the ethosomal gel containing Zaltoprofen for sustained drug delivery and also to reduce the side effects. Zaltoprofen was chosen here as the drug candidate because of its short half-life and increased dosing frequency.

Methods: The ethosomes containing Zaltoprofen was prepared by using cold method. A 23 full factorial design containing 10 experimental trails was used in order to obtain an optimized formulation. The prepared ethosomes were characterized by Scanning Electron Microscopy, PDI, zeta potential, vesicle size, and percentage entrapment efficiency. Optimized ethosomal formulation was incorporated in 1% carbopol gel to deliver the drug through topical route. Invitro drug permeation studies of ethosomal gel (EGL) and conventional gel (CGL) was conducted and flux and permeability coefficient were calculated.

Results:The vesicle size, zeta potential, and % entrapment efficiency of optimized formulation were found to be 124.33 nm, -45.2 mV and 70.03%, respectively. The surface of the vesicles was found to be spherical and smooth. The in vitro drug release studies of the ethosomal gel formulation showed sustained drug delivery when compared with the conventional gel containing the pure drug. In vitro permeability studies show that the flux of ethosomal gel was 2.5 fold higher than conventional gel, which may be the attribution of ethanol and flexible nature of ethosomes.

Conclusion: It was concluded that the ethosomal gel could be a better choice for the topical delivery of Zaltoprofenwith improved bioavailability for its anti-inflammatory activity.

Open Access Original Research Article

Formulation and Evaluation of Eudragit Rl100 Polymeric Drug Loaded Microsponge for Ophthalmic Use

Rajashri B. Ambikar, Ashok V. Bhosale

Journal of Pharmaceutical Research International, Page 45-51
DOI: 10.9734/jpri/2021/v33i24B31440

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles.

Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM.

Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%.  Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure.

Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

Open Access Original Research Article

A New Heterocyclic 1H-perimidine synthesized 2-(2,3-dihydro-1H-périmidin-2yl-)-6-methoxyphenol: Evaluation of Acute Toxicity in Wistar Rat

Tuo Nanou Tiéba, Pacôme Kouadio N’Go, Ballo Daouda, Kangah Niameke Jean Baptiste, Kodjo Charles Guillaume, Yapo Ossey Bernard, Ziao Nahossé

Journal of Pharmaceutical Research International, Page 52-60
DOI: 10.9734/jpri/2021/v33i24B31441

Background and Aim: The 1H-perimidne, as novel source carbene ligand, is well known for its anti-fungal, anti-microbial or anti-tumor activities. Here, we aimed to study the acute toxicity in Wistar rat of 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol, a new heterocyclic 1H- perimidine synthetized in our laboratory.      

Materials and Methods: Five groups of males Wistar rats were intraperitoneally injected with 7 mg/kg, 40 mg/kg, 90 mg/kg, 130 mg/kg and 150 mg/kg dissolved in dimethyl sulfoxide (DMSO), and followed during 14 days. We noted any clinical signs of acute toxicity as body weight loss, salivation, tremor, convulsion among others, as well as food consumption and water intake level.

Results: The DL50 of the new 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol was estimated to 65 mg/kg. The No Observed Adverse Effect Level (NOAEL) dose was 7 mg/kg because it did not caused mortality, clinical signs of acute toxicity, and not affected feed and water intake behavior. However, significant abnormalities as inflammation and necrosis were observed at doses-effects dependent in liver, when compared to NOAEL dose and vehicle.

Conclusion: The new heterocyclic 2-(2,3-dihydro-1H-perimidin-2-yl)-6-methoxyphenol is considered as high toxicity grade product. From NOAEL dose, subsequent biological, toxicological, pharmacological and neurobehavioral studies are needed before using for clinical trials.

Open Access Original Research Article

Antibacterial Activity of Ananas comosus Fruit Extract against Clinically Isolated Bacteria from Urinary Tract Infected Patients

Anbu Jeba Sunilson John Samuel, Anita Gnana Kumari Anpumoni Vimala, Dhanuprabha Dakshanamurthy

Journal of Pharmaceutical Research International, Page 61-70
DOI: 10.9734/jpri/2021/v33i24B31442

Aim: To evaluate the antibacterial activity of Ananas comosus (A. comosus) fruit extract against clinically isolated bacteria from urinary tract infected patients.

Study Design: Experimental study.

Place and Duration of Study: Research Lab, Department of Siddha Medicine, Tamil University, Thanjavur, India and Microbiology lab, School of Pharmacy, KPJ Healthcare University College, Malaysia, between February 2019 and January 2020.

Methodology: In the present study the ethanol and aqueous extracts of A. comosus were analysed for the phytoconstituents and the activity of the plant extract was compared with a standard antibiotic which is used for a wide range of Urinary Tract infection which is Ciprofloxacin (250 mg/mL) using cup plate method.

Results: The ethanolic extract of A. comosus showed a great level of bacterial inhibition (27.3 mm) against Bacillus cereus as compared with standard (22.3 mm).Whereas the antimicrobial activity was moderate against Klebsiella organism and very less against Staphylococcus. Standard exhibits a huge difference in the zone of inhibition which is (34 mm) and ethanol extract (23 mm) against Enterococcus. While the aqueous extracts do not show any effect on the microorganism.

Conclusion: The ethanol extract A. comosus exhibited broad-spectrum activity against tested isolates compared to aqueous extract. A. comosus has broad inhibitory activities to pathogenic microorganisms and promising to act as potential antibacterial agents from natural plant sources.

Open Access Original Research Article

Evaluation of Anti-quorum Sensing Potential of Saraca asoca (Family Caesalpiniaceae) against Chromobacterium violaceum and Pseudomonas aeruginosa PA01

B. S. Paliya, J. Mathew, B. N. Singh

Journal of Pharmaceutical Research International, Page 71-82
DOI: 10.9734/jpri/2021/v33i24B31443

Aim: The present study was performed to evaluate the anti-quorum sensing (QS) potential of traditional medicinal herb Saracaasoca (family Caesalpiniaceae) stem bark extract against Chromobacterium violaceum and Pseudomonas aeruginosa PA01.

Study Design: First, the test sample (bark extract) was screened for anti-QS activity. Then systematic in-vitro and biochemical tests were performed to evaluate the effect of the test sample on the QS mediated virulence factors.

Place and Duration of Study: All the experimental works were performed in Lab 311, pharmacology division, CSIR-NBRI Lucknow from June 2019 to October 2019.

Methodology: The samples of Saraca asoca stem bark were washed, dried and extracted using 70% methanol. The minimum inhibitory concentration (MIC) of the prepared Sarca asoca bark extract was determined using the Alamar blue assay, and the anti-QS activity was screened using standard agar overlay method against CV 12472 at subinhibitory concentrations 100, 200 and 300 µg (< MIC value). SAE effect on biofilms formation was assessed by growing biofilms on glass slides in a static culture of PA01. Anti-virulence effect of SAE on the production of QS-regulated virulence factors such as Pyocyanin, proteases, elastases, rhamnolipid and alginate in Pseudomonas aeruginosa was determined using the supernatant of a 24 hours old broth culture of PA01 supplemented with SAE. Using the agar plate technique, the swimming and swarming motility assays were conducted on 0.3% and 0.5% agar plates respectively. One-way ANOVA was used to analyze the data, presented as mean ± SD (standard deviation) of three independent experiments.

Results: Preliminary screening results showed significant QS inhibition against CV 12472 in an agar overlay disk diffusion assay in a concentration-dependent manner. Data from the biofilm assay showed loose, distorted, irregular PA01 biofilm formation at 200 µg (48%) and 300 µg (65%). SAE caused a significant drop in virulence factor production, with maximum reduction in pyocyanin (58%), proteases (67%), elastases (52%), rhamnolipid (53%), and alginate (44%) observed at 300 µg concentration. At SAE sub-lethal concentrations (200 and 300 µg), both the swimming and swarming motility of PA01 were significantly inhibited.

Conclusions: The present study demonstrates the broad-spectrum anti-QS potential of SAE, reported for the first time, suggesting that SAE could be considered as an alternative herbal source to develop antimicrobial agents which can be either solitary or synergistically with conventional antimicrobial drugs.

Open Access Original Research Article

Screening of Common Potential Inhibitors against Periodontitis and Alzheimer's Disease

Mahvish Khan, Saif Khan, Mohtashim Lohani, Hazza A. Alhobeira, Shadab Mirza, Shafiul Haque

Journal of Pharmaceutical Research International, Page 83-91
DOI: 10.9734/jpri/2021/v33i24B31444

Introduction: As the amyloid precursor protein performs a remarkable part in chronic periodontitis and the progression of Alzheimer's disease growth, discoveryof novelactive inhibitors of this protein can be of great standing in the treatment of periodontitis. Chronic periodontitis is one of the causative factors and metabolic stressor for diabetes control. In chronic periodontitis and Alzheimer's disease, some molecules have been proposed to inhibit proteins in past.

Methods: This study was planned to find present potent inhibitors,A library of KDM compounds was obtained from Chem Div Database. Here, all complexes with goodglide score were short listed for analysis of protein-ligand interaction. Calculations were carried out to estimate the interaction of the ligands selected in complex with the beta amyloid protein.

Results: Five top hits were found considering Curcuminas reference. Five small molecules have been proposed as possible inhibitors of this protein. Here in this study, we have focused on small molecule lead inhibitors for identification of Chronic Periodontitis and Alzheimer's disease.

Open Access Review Article

Coronavirus Disease 2019 (COVID-19): Review on Transmission, Clinical Presentations, Treatments and Vaccines

Syed Arman Rabbani, Shrestha Sharma, Supriya Mishra, Asiya Mahtab

Journal of Pharmaceutical Research International, Page 92-114
DOI: 10.9734/jpri/2021/v33i24B31445

Coronavirus disease 2019 (COVID-19) has become one of the most prevalent and significant global health concerns since its origin in Wuhan, China in the December 2019. As on 05th April, this disease has affected over 131 million people and has resulted in more than 2.85 million deaths worldwide till date. The disease is transmitted from the infected patients to the people in close contact through respiratory droplets. There are a number of factors which affect the transmission of this disease. The clinical presentation of COVID-19 can range from asymptomatic infections to critical disease leading to respiratory failure, septic shock and multiple organ failure. The disease essentially affects the respiratory system but other organ systems may also be involved. Currently, the therapeutic management of the disease is based on the severity of the infection and employs various strategies like monoclonal antibodies, corticosteroids, antivirals, stem cell therapy and immunomodulators. Scientists and researchers all around the world have raced against the time and developed a number of vaccines for COVID-19.  At present, there are many COVID-19 vaccines, which have been authorized or approved for use by the regulators of the different countries. This article reviews the current published data on the COVID-19 transmission, clinical presentations, treatments and vaccines.