Open Access Original Research Article

Survey on Antimicrobial Resistance: Reason behind the Misuse of Antibiotics in Bangladesh

Md. Najem Uddin, Md. Hafizur Rahman, Md. Mehedi Hasan, Md. Nazmul Islam, Md. Bokhtear Sarkar, Md. Rafiul Islam, S. M. Abdul Barik, Md. Nazmul Sardar

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/JPRI/2017/36672

Aims: It is a base line survey to find the reason behind the misuse of antibiotic in Bangladesh.

Study Design: Questionnaires were supplied to corresponded persons to collect information from patient, doctors & pharmacy shop from seven region of Bangladesh. The data was analyzed by using simple descriptive statistics to generate frequencies, percentage & proportions.

Place and Duration of Study: The survey was carried out throughout Bangladesh from May 2016 to August 2016.

Methodology: Information of 2250 patients, 760 doctors & 1450 chemist shop form 7 regions of Bangladesh were collected from May 2016 to August 2016 using questionnaires consisting descriptive question, true false, multiple choice and a comment part by direct interview method. Wherever it was relevant, the Chi-square test was used to determine any significance difference.

Results:  We found majority of people (70%) are not so concern about the antibiotic resistance and it’s after effect due to lack of proper knowledge.  we found majority of people (70%) are not so concern about the antibiotic resistance and its after effect due to lack of proper knowledge. 18% people are known with the term antimicrobial resistance but do not have proper knowledge about resistance and the rest of the people (12%) has proper knowledge about antibiotic dosage and antimicrobial resistance. Majority of people are known with the some antibiotics like Azythromycin & Ciprofloxacin which are taken by them without prescription for reducing fever, severe pain and wound without considering the dosage completion.

Conclusion: Antibiotics should only be used when needed as prescribed by health professionals. The prescriber should closely adhere to the five rights of drug administration: the right patient, the right drug, the right dose, the right route, and the right time.

Open Access Original Research Article

Phytochemical Screening Antioxidant and Alpha-glucosidase Inhibitory Activities of Fagopyrum tataricum L. Extract

Muhammad Wajid, Muhammad Uzair, Bashir Ahmad Chaudhary

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/JPRI/2017/36067

Objective: The objective of this work was the screening of different phytoconstituents and invitro antioxidant potential and α-glucosidase inhibitory activity of aerial parts of Fagopyrum tataricum.

Methods: Preliminary phytochemical screening was performed by using standard protocols. The antioxidant activity was determined by using spectroscopic method against 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and α-glucosidase inhibition assay.         

Results: The plant extract also shows potent antioxidant and α-glucosidase inhibitory potential against the tested methods.

Conclusion: From the results it seen that this plant exhibits significant antioxidant and α-glucosidase inhibitory potential.

Open Access Original Research Article

Solubility Enhancement of a BCS Class II Drug Using Granulated Fumed Silica as an Adsorbent

Sawani D. Talekar, Rutesh H. Dave

Journal of Pharmaceutical Research International, Page 1-15
DOI: 10.9734/JPRI/2017/36872

Aim: The aim of this study was to improve solubility and dissolution characteristics of Ibuprofen using granulated fumed silica (Aeroperl®300) as a carrier.

Methods: Ibuprofen-silica complex was prepared by solvent evaporation technique using ethanol as the solvent. Formulation I and II consisted of polymers hydroxypropyl methylcellulose (HPMC E5) and Polyvinyl Pyrrolidone (PVP K-30) respectively. Each formulation was prepared using 1:1:1 and 1:1:2 ratio of drug, polymer and silica. Dried powder obtained was characterized using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and Polarized Light Microscopy (PLM). In-vitro dissolution studies were carried out using three different media including Phosphate buffer (pH 6.8), 0.1N Hydrochloric Acid (pH 1.2) and de-ionized water.

Results: Drug loading up to 30% w/w was successfully achieved with 1:1:1 ratio formulations. Physical characterization data confirmed change of crystalline Ibuprofen into amorphous form after processing. Maximum solubility increment of 33-37% was achieved in Phosphate buffer with formulations II A and II B within the first 5 minutes of dissolution as compared to the control (pure drug).

Conclusion: Enhancement in drug solubility and subsequent dissolution rate can be attributed to adsorption of amorphous drug molecules onto porous silica that readily desorb on contact with dissolution media. High porosity and huge surface area of silica makes it a potential candidate for improving delivery of poorly soluble drugs.

Open Access Original Research Article

Cell-specific Reduction in Viability of Two Breast Cancer Cell Lines after Exposure to Gold Nanoparticles

Olivia G. Waszczuk, Jennifer R. Schroeder

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/JPRI/2017/36154

Aims: Nanoparticle composites are a recent research hotspot, with the potential to be drug-delivery vehicles for more efficient treatment of malignant cancerous tumors. However, as this is a relatively new field, the safety of these nanoparticles is of concern. In this study, we assess whether two preparations of gold nanoparticles, HPN1 and HGN2, affect cell viability using a metabolic assay.

Study Design: We treated two breast cancer cell lines, MCF-7 and MDA-MB-231, with two different nanoparticle preparations for five days. Following treatment, we assessed changes in cellular metabolic activity using an MTT assay.

Methodology: HPN1 are 32 nm diameter colloidal gold nanoparticles, which reflect a purple hue, while HGN2 are 10 nm diameter and reflect a yellow-orange color. We plated MDA-MB-231 or MCF-7 cells into a 6-well plate at 60% confluence. After 24 hours, we treated cells with fresh media containing 5-10% of HPN1 or HGN2 nanoparticles or PBS control. After 120 hours, we assessed the metabolic activity of live cells using a standard MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay, performed in triplicate. Univariate analysis of variance (ANOVA) was performed using SPSS, with P=0.05 indicating significant variation from the controls.

Results: Interestingly, we show little change in cell activity after exposure of human MDA-MB-231 breast cancer cells to fresh and aged nanoparticles for five days; however, MCF-7 breast cancer cells responded to the two nanoparticles differently. After nanoparticles had been stored for several months, treatment with HPN1 led to a loss of viability; in contrast, HGN2 increased proliferation. 

Conclusion: We must be cautious moving forward in the development of new chemotherapeutic techniques, since acute tests may not be indicative of the true toxicity of these compounds.

Open Access Original Research Article

A Novel Acyl-CoA: Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitor, GSK2973980A, Inhibits Postprandial Triglycerides and Reduces Body Weight in a Rodent Diet-induced Obesity Model

Sanjay Kumar, Vijaya G. Tirunagaru, Jennifer Ariazi, Amit Awasthi, Venkatesh Babu Jayaraman, Premkumar Arumugam, Mahesh Yanamandra, Sayan Mitra, Sudhir Tiwari, Raghuram S. Tangirala, Thilo Werner, Douglas Thomson, Giovanna Bergamini, Mui Cheung

Journal of Pharmaceutical Research International, Page 1-15
DOI: 10.9734/JPRI/2017/36835

Background and Aim: Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) is a key enzyme catalyzing the final step of triglyceride (TG) synthesis and is implicated in fat absorption and disposition. However, development of several DGAT1 inhibitors has been hampered due to unacceptable gastrointestinal (GI) tolerability observed in clinical trials. Our aim is to develop a novel, potent and selective DGAT1 inhibitor that reduces plasma TG levels and body weight with acceptable GI tolerability in a rodent model of obesity.

Study Design: In vitro enzyme and cellular assays as well as in vivo experimental studies in mice and rat examining the effect of drugs on triglycerides, fecal fat, body weight and food intake.

Place and Duration of Study: Virtual proof of concept, GSK USA & Cellzome, GSK Germany and Collaborative research, GVK, India between 2011-2017.

Methodology: A radiometric assay of TG formation evaluated DGAT activity and a thermal shift assay determined target specificity. Fasted mice received an oral corn oil bolus to model hypertriglyceridemia. Intralipid administration in fasted rats was used to evaluate triglyceride clearance. Mice were fed a high fat diet to induce obesity.

Results: Herein, we describe GSK2973980A as a novel, potent and selective DGAT1 inhibitor that reduced plasma TG levels in postprandial lipid excursion and impaired clearance studies in rodents and reduced body weight and food intake in obese mice.  Interestingly, robust plasma TG reduction was accompanied by varying degrees of fecal lipid excretion. Alternate dosing via the subcutaneous route maintained a significant effect on plasma TG reduction with no altered fecal lipid excretion, suggesting GI tolerability may be modulated by limiting local GI exposure of DGAT1 inhibitors.

Conclusion: Our data suggest that the impaired TG clearance model in the rat can be used to identify DGAT1 inhibitors with potentially better GI tolerability.