Search results for: lipid lowering drug

Authors: Larissa M. Vargas, Julia M. Sacchi, Renata O. Pereira, Lucas S. Asano, Iara C. Araújo, Patricia Fiorino, Vera Farah

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The aim of this study was to evaluate the occurrence of subclinical organ injuries induced by high-fat diet. Male wistar rats (n=5/group) were divided in control diet group (CD), commercial rat chow, and hyperlipidic diet (30% lipids) group (HD) administrated during 8 weeks, starting after weaning. All the procedures followed the rules of the Committee of Research and Ethics of the Mackenzie University (CEUA Nº 077/03/2011). At the end of protocol the animals were euthanized by anesthesia overload and the left kidney was removed. Intrarenal lipid deposition was evaluated by histological analyses with oilred. Kidney slices were stained with picrosirius red to evaluate the area of the Bowman's capsule (AB) and space (SB), and glomerular tuft area (GT). The renal expression of sterol regulatory element–binding protein (SREBP-2) was performed by Western Blotting. Creatinine concentration (serum and urine) and lipid profile were determined by colorimetric kit (Labtest). At the end of the protocol there was no differences in body weight between the groups, however the HD showed a marked increase in lipid deposits, glomeruli and tubules, and biochemical analysis for cholesterol and triglycerides. Moreover, in the kidney, the high-fat diet induced a reduction in the AB (13%), GT (18%) and SB (17%) associated with a reduction in glomerular filtration rate (creatinine clearance). The renal SRBP2 expression was increased in HD group. These data suggests that consumption of high-fat diet starting in childhood is associated with subclinical renal damage and function.

Keywords: high-fat diet, kidney, intrarenal lipid deposition, SRBP2

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Authors: Ifeanyichukwu Edeh, Tim Overton, Steve Bowra

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Currently biodiesel is produced from plant oils or animal’s fats by a liquid-phase catalysed transesterification process at low temperature. Although biodiesel is renewable and to a large extent sustainable, inherent properties such as poor cold flow, low oxidation stability, low cetane value restrict application to blends with fossil fuels. An alternative to biodiesel is renewable diesel produced by catalytic hydrotreating of oils and fats and is considered a drop in fuel because its properties are similar to petroleum diesel. In addition to developing alternative productions routes there is continued interest in reducing the cost of the feed stock, waste cooking oils and fats are increasingly used as the feedstocks due to low cost. However, use of oils and fat are highly adulterated resulting in high free fatty acid content which turn impacts on the efficiency of FAME production. Therefore, in light of the need to develop, alternative lipid feed stocks and related efficient catalysis the present study investigates the potential of producing renewable diesel from the lipids-extracted from activated sludge, a waste water treatment by-product, through catalytic hydrothermal decarboxylation. The microbial lipids were first extracted from the activated sludge using the Folch et al method before hydrothermal decarboxylation reactions were carried out using palladium (Pd/C) and platinum (Pt/C) on activated carbon as the catalysts in a batch reactor. The impact of three temperatures 290, 300, 330 °C and residence time between 30 min and 4hrs was assessed. At the end of the reaction, the products were recovered using organic solvents and characterized using gas chromatography (GC). The principle products of the reaction were pentadecane and heptadecane. The highest yields of pentadecane and heptadecane from lipid-extract were 23.23% and 15.21%, respectively. These yields were obtained at 290 °C and residence time 1h using Pt/C. To the best of our knowledge, the current work is the first investigation on the hydrothermal decarboxylation of lipid-extract from activated sludge.

Keywords: activated sludge, lipid, hydrothermal decarboxylation, renewable diesel

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Authors: Sahil Kumar, Rajaram Ghadge, Ramesh Bhujade

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Historically, lipid extraction from dried algal biomass remained a focus area of the algal research. It has been realized over the past few years that the lipid-centric approach and conversion technologies that require dry algal biomass have several challenges. Algal culture in cultivation systems contains more than 99% water, with algal concentrations of just a few hundred milligrams per liter ( < 0.05 wt%), which makes harvesting and drying energy intensive. Drying the algal biomass followed by extraction also entails the loss of water and nutrients. In view of these challenges, focus has shifted toward developing processes that will enable oil production from wet algal biomass without drying. Hydrothermal liquefaction (HTL), an emerging technology, is a thermo-chemical conversion process that converts wet biomass to oil and gas using water as a solvent at high temperature and high pressure. HTL processes wet algal slurry containing more than 80% water and significantly reduces the adverse cost impact owing to drying the algal biomass. HTL, being inherently feedstock agnostic, i.e., can convert carbohydrates and proteins also to fuels and recovers water and nutrients. It is most effective with low-lipid (10--30%) algal biomass, and bio-crude yield is two to four times higher than the lipid content in the feedstock. In the early 2010s, research remained focused on increasing the oil yield by optimizing the process conditions of HTL. However, various techno-economic studies showed that simply converting algal biomass to only oil does not make economic sense, particularly in view of low crude oil prices. Making the best use of every component of algae is a key for economic viability of algal to oil process. On investigation of HTL reactions at the molecular level, it has been observed that sequential HTL has the potential to recover value-added products along with biocrude and improve the overall economics of the process. This potential of sequential HTL makes it a most promising technology for converting wet waste to wealth. In this presentation, we will share our experience on the techno-economic and engineering aspects of sequential HTL for conversion of algal biomass to algal bio-oil and co-products.

Keywords: algae, biomass, lipid, protein

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Authors: Abhishek Kumar Sah, Preeti K. Suresh

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Effective drug delivery to the eye is a massive challenge, due to complicated physiological ocular barriers, rapid washout by tear and nasolachrymal drainage. Thus, most of the conventional ophthalmic formulations face the problem of low ocular bioavailability. Ophthalmic drug therapy can be improved by enhancing the precorneal drug retention along with improved drug penetration. The aim of the present investigation was to develop and evaluate a biodegradable polymer poly (D, L-lactide-co-glycolide) (PLGA) coated nanoparticulate carrier of loteprednol etabonate. PLGA nanoparticles were prepared by modified emulsification/solvent diffusion method using high-speed homogenizer followed by sonication. The nanoparticles were characterized for various parameters such as particle size, zeta potential, polydispersity index, X-ray powder diffraction (XRD), Transmission electron microscopy (TEM), in vitro drug release profile and stability. The prepared nanocarriers displayed mean particle size in the range of 271.7 to 424.4 nm, with zeta potential less than –10 mV. In vitro release in simulated tear fluid (STF) nanocarrier showed an extended release profile of loteprednol etabonate. TEM confirmed the spherical morphology and smooth surface of the particles. All the prepared formulations were found to be stable at varying temperatures.

Keywords: drug delivery, ocular delivery, polymeric nanoparticles, loteprednol etabonate

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Authors: Jolanta Pulit-Prociak, Olga Dlugosz, Marcin Banach

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The toxicity of bare zinc oxide nanoparticles used as drug carriers may be the result of releasing zinc ions. Thus, zinc oxide nanoparticles modified with galactose were obtained. The process of their formation was conducted in the microwave field. The physicochemical properties of the obtained products were studied. The size and electrokinetic potential were defined by using dynamic light scattering technique. The crystalline properties were assessed by X-ray diffractometry. In order to confirm the formation of the desired products, Fourier-transform infrared spectroscopy was used. The releasing of zinc ions from the prepared products when comparing to the bare oxide was analyzed. It was found out that modification of zinc oxide nanoparticles with galactose limits the releasing of zinc ions which are responsible for the toxic effect of the whole carrier-drug conjugate.

Keywords: nanomaterials, zinc oxide, drug delivery system, toxicity

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Authors: Rajesh Chandra, Uttam K. Ghosh

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This study demonstrates microalgal bio-diesel generation from a cheap, abundant, non-edible fruit pulp of Cassia fistula L. The Cassia fistula L. fruit pulp aqueous extract (CFAE) was utilized as a growth medium for cultivation of microalga Chlorella minutissima (C. minutissima). This microalga accumulated a high amount of lipids when cultivated with CFAE as a source of nutrition in comparison to BG-11 medium. Different concentrations (10, 20, 30, 40 and 50%) of CFAE diluted with distilled water were used to cultivate microalga. Effects of light intensity and photoperiod were also observed on biomass and lipid yield of microalga. Light intensity of 8000 lux with a photoperiod of 18 h resulted in maximum biomass and lipid yield of 1.28 ± 0.03 and 0.3968 ± 0.05 g/L, respectively when cultivated with 40% CFAE. Fatty acid methyl ester (FAME) profile of bio-diesel obtained shown the presence of myristic acid (C14:0), palmitic acid (C16:0), palmitoleic acid (C16:1), stearic acid (C18:0), linoleic acid (C18:2), linolenic acid (C18:3), arachidic acid (C20:0), and gondoic acid (C20:1), as major fatty acids. These facts reflect that the fruit pulp of Cassia fistula L. can be used for cultivation of C. minutissima.

Keywords: biomass, bio-diesel, Cassia fistula L., C. minutissima, GC-MS, lipid

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Authors: Meltem Koray, Arda Ozgon, Duygu Ofluoglu, Mehmet Yaltirik

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Oral ulcerations can be seen as a side effect of different drugs. These ulcers usually appear within a few weeks following drug treatment. In most of cases, these ulcers resist to conventional treatments, such as anesthetics, antiseptics, anti-inflammatory agents, cauterization, topical tetracycline and corticosteroid treatment. The diagnosis is usually difficult, especially in patients receiving multiple drug therapies. Hyaluronan or hyaluronic acid (HA) is a biomaterial that has been introduced as an alternative approach to enhance wound healing and also used for oral ulcer treatment. The aim of this report is to present the treatment of drug-induced oral ulceration on maxillary mucosa with HA gel. 60-year-old male patient was referred to Department of Oral and Maxillofacial Surgery complaining of oral ulcerations during few weeks. He had received chemotherapy and radiotherapy in 2014 with the diagnosis of nasopharyngeal carcinoma, and he has accompanying systemic diseases such as; cardiological, neurological diseases and gout. He is medicated with Escitalopram (Cipralex® 20mg), Quetiapine (Seroquel® 100mg), Mirtazapine (Zestat® 15mg), Acetylsalicylic acid (Coraspin® 100mg), Ramipril-hydrochlorothiazide (Delix® 2.5mg), Theophylline anhydrous (Teokap Sr® 200mg), Colchicine (Colchicum Dispert® 0.5mg), Spironolactone (Aldactone® 100mg), Levothyroxine sodium (Levotiron® 50mg). He had painful oral ulceration on the right side of maxillary mucosa. The diagnosis was 'drug-induced oral ulceration' and HA oral gel (Aftamed® Oral gel) was prescribed 3 times a day for 2 weeks. Complete healing was achieved within 3 weeks without any side effect and discomfort. We suggest that HA oral gel is a potentially useful local drug which can be an alternative for management of drug-induced oral ulcerations.

Keywords: drug-induced, hyaluronic acid, oral ulceration, maxillary mucosa

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Authors: Mustafa M. Donma, Orkide Donma

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The examination of both serum lipid fractions and body’s lipid composition are quite informative during the evaluation of obesity stages. Within this context, alterations in lipid parameters are commonly observed. The variations in the fat distribution of the body are also noteworthy. Total cholesterol (TC), triglycerides (TRG), low density lipoprotein-cholesterol (LDL-C), high density lipoprotein-cholesterol (HDL-C) are considered as the basic lipid fractions. Fat deposited in trunk and extremities may give considerable amount of information and different messages during discrete health states. Ratios are also derived from distinct fat distribution in these areas. Trunk-to-leg fat ratio (TLFR) and trunk-to-appendicular fat ratio (TAFR) are the most recently introduced ratios. In this study, lipid fractions and TLFR, as well as TAFR, were evaluated, and the distinctions among healthy, obese (OB), and morbid obese (MO) groups were investigated. Three groups [normal body mass index (N-BMI), OB, MO] were constituted from a population aged 6 to 18 years. Ages and sexes of the groups were matched. The study protocol was approved by the Non-interventional Ethics Committee of Tekirdag Namik Kemal University. Written informed consent forms were obtained from the parents of the participants. Anthropometric measurements (height, weight, waist circumference, hip circumference, head circumference, neck circumference) were obtained and recorded during the physical examination. Body mass index values were calculated. Total, trunk, leg, and arm fat mass values were obtained by TANITA Bioelectrical Impedance Analysis. These values were used to calculate TLFR and TAFR. Systolic (SBP) and diastolic blood pressures (DBP) were measured. Routine biochemical tests including TC, TRG, LDL-C, HDL-C, and insulin were performed. Data were evaluated using SPSS software. p value smaller than 0.05 was accepted as statistically significant. There was no difference among the age values and gender ratios of the groups. Any statistically significant difference was not observed in terms of DBP, TLFR as well as serum lipid fractions. Higher SBP values were measured both in OB and MO children than those with N-BMI. TAFR showed a significant difference between N-BMI and OB groups. Statistically significant increases were detected between insulin values of N-BMI group and OB as well as MO groups. There were bivariate correlations between LDL and TLFR (r=0.396; p=0.037) as well as TAFR values (r=0.413; p=0.029) in MO group. When adjusted for SBP and DBP, partial correlations were calculated as (r=0.421; p=0.032) and (r=0.438; p=0.025) for LDL-TLFR as well as LDL-TAFR, respectively. Much stronger partial correlations were obtained for the same couples (r=0.475; p=0.019 and r=0.473; p=0.020, respectively) upon controlling for TRG and HDL-C. Much stronger partial correlations observed in MO children emphasize the potential transition from morbid obesity to metabolic syndrome. These findings have concluded that LDL-C may be suggested as a discriminating parameter between OB and MO children.

Keywords: children, lipid parameters, obesity, trunk-to-leg fat ratio, trunk-to-appendicular fat ratio

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Authors: Nagasamy Venkatesh Dhandapani

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This work aims at investigating the use of β-Cyclodextrin as a cross linker, in an attempt to formulate nanosponges containing ketoconazole. The nanosponges were prepared by cross-linking method. The excipients used in this study did not alter the physicochemical properties of a drug as revealed by FTIR spectroscopy. Studies on various formulation variables revealed that all the variables are inter-related with the formulation. The ideal batch among the formulation was selected based on the higher entrapment efficiency and drug loading. The in vitro release studies of ketoconazole nanosponges in hydrogel exhibited a sustained release over a period of 24 hours. Mathematical analysis of drug release from the formulation followed non-Fickian diffusion obeying first order kinetics. The anti-fungal activity of the formulation exhibited better zone of inhibition when compared to pure drug (ketoconazole) against Tinea corporis.

Keywords: nanosponges, beta-cyclodextrin, ketoconazole, tinea corporis

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Authors: Venkatalakshmi Ranganathan, Ong Hsin Ju, Tan Yinn Ming, Lim Kien Sin, Wong Man Ting, Venkata Srikanth Meka

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The mucoadhesive buccal tablet is an oral drug delivery system which attached to the buccal surface for direct drug absorption into the systemic circulation and the unidirectional drug release is ensured by formulating a hydrophobic backing layer. The objective of present study was to formulate mucoadhesive atenolol bilayer buccal tablets by using sodium alginate, hydroxyethyl cellulose, and xanthan gum as mucoadhesive polymer and the technique applied was direct compression method. Ethyl cellulose was used as backing layer of the tablet. FTIR and DSC analysis were carried out to identify the drug polymer interactions. The prepared tablets were evaluated for physicochemical parameters, ex vivo mucoadhesion time and in-vitro drug release. The formulated tablets showed the average surface pH 6-7 which is favourable for oral mucosa. The formulation containing sodium alginate showed more than 90 % of drug release at the end of the 7 hours in vitro dissolution studies. The formulation containing xanthan gum showed more than 8 hours of mucoadhesion time and all formulation exhibited non fickian release kinetics. The present study indicates enormous potential of erodible mucoadhesive buccal tablet containing atenolol for systemic delivery with an added advantage of circumventing the hepatic first pass metabolism.

Keywords: atenolol, mucoadhesion, in vitro drug release, direct compression, ethyl cellulose

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Authors: Farzad Khajavi, Farzaneh Jalilfar, Faranak Jafari, Leila Shokrani

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Formulation of gliclazide in the form of extended-release tablet in 30 and 60 mg dosage forms was performed using hypromellose (HPMC K4M) as a retarding agent. Drug-release profiles were investigated in comparison with references Diamicron MR 30 and 60 mg tablets. The effect of size of powder particles, the amount of hypromellose in formulation, hardness of tablets, and also the effect of halving the tablets were investigated on drug release profile. A mathematical model which describes hypromellose behavior in initial times of drug release was proposed for the estimation of hypromellose content in modified-release gliclazide 60 mg tablet. This model is based on erosion of hypromellose in dissolution media. The model is applicable to describe release profiles of insoluble drugs. Therefore, by using dissolved amount of drug in initial times of dissolution and the model, the amount of hypromellose in formulation can be predictable. The model was used to predict the HPMC K4M content in modified-release gliclazide 30 mg and extended-release quetiapine 200 mg tablets.

Keywords: Gliclazide, hypromellose, drug release, modified-release tablet, mathematical model

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Authors: Ian Walmsley

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The aim of this paper is to explore the influence of time and temporality on the experience of coming off heroin in prison. The presentation draws on qualitative data collected during a small-scale pilot study of the role of self-care in the process of coming off drugs in prison. Time and temporality emerged as a key theme in the interview transcripts. Drug dependent prisoners experience of time in prison has not been recognized in the research literature. Instead, the literature on prison time typically views prisoners as a homogenous group or tends to focus on the influence of aging and gender on prison time. Furthermore, there is a tendency in the literature on prison drug treatment and recovery to conceptualize drug dependent prisoners as passive recipients of prison healthcare, rather than active agents. In building on these gaps, this paper argues that drug dependent prisoners experience multiple temporalities which involve an interaction between the body-times of the drug dependent prisoner and the economy of time in prison. One consequence of this interaction is the feeling that they are doing, at this point in their prison sentence, double prison time. The second part of the argument is that time and temporality were a means through which they governed their withdrawing bodies. In addition, this paper will comment on the challenges of prison research in England.

Keywords: heroin withdrawal, time and temporality, prison, body

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Authors: Muhammad Saad Shoaib Khan, Rasbin Basnet, Qingyao Shu

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Phospholipids are one of the major classes of lipid comprising 10% of total grain lipid in rice. Phospholipids are the main phosphorus containing lipid in the rice endosperm, contributing to rice palatability and seed storage property. However, in the rice grain, the majority of phosphorus occur in the form of phytic acid and are highly abundant in the bran. Phytic acid, also known as hexaphosphorylated inositol (IP6), are strong chelating agents which reduces the bioavailability of essential dietary nutrients and are therefore less desirable by rice breeders. We used the CRISPR/Cas9 system to generate mutants of a phospholipase D gene (PLDα1), which is responsible for the degradation of phospholipids into phosphatidic acid (PA). In the mutants, we found a significant reduction in the concentration of phytic acid in the grain as compared to the wild-type. The biochemical analysis of the PLDα1 mutants showed that the decrease in production of phosphatidic acid is due to reduced accumulation of CDP-diacylglycerolderived phosphatidylinositol (PI), ultimately leading to lower accumulation of phytic acid in mutants. These results showed that loss of function of PLD in rice leads to lower production of phytic acid, suggesting the potential application of Ospldα1 in breeding rice with less phytic acid.

Keywords: CRISPR/Cas9, phospholipase D, phytic acid, rice

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Authors: Ernest Moles, Patricia Urbán, María Belén Jiménez-Díaz, Sara Viera-Morilla, Iñigo Angulo-Barturen, Maria Antònia Busquets, Xavier Fernàndez-Busquets

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Bearing in mind the absence of an effective vaccine against malaria and its severe clinical manifestations causing nearly half a million deaths every year, this disease represents nowadays a major threat to life. Besides, the basic rationale followed by currently marketed antimalarial approaches is based on the administration of drugs on their own, promoting the emergence of drug-resistant parasites owing to the limitation in delivering drug payloads into the parasitized erythrocyte high enough to kill the intracellular pathogen while minimizing the risk of causing toxic side effects to the patient. Such dichotomy has been successfully addressed through the specific delivery of immunoliposome (iLP)-encapsulated antimalarials to Plasmodium falciparum-infected red blood cells (pRBCs). Unfortunately, this strategy has not progressed towards clinical applications, whereas in vitro assays rarely reach drug efficacy improvements above 10-fold. Here, we show that encapsulation efficiencies reaching >96% can be achieved for the weakly basic drugs chloroquine (CQ) and primaquine using the pH gradient active loading method in liposomes composed of neutrally charged, saturated phospholipids. Targeting antibodies are best conjugated through their primary amino groups, adjusting chemical crosslinker concentration to retain significant antigen recognition. Antigens from non-parasitized RBCs have also been considered as targets for the intracellular delivery of drugs not affecting the erythrocytic metabolism. Using this strategy, we have obtained unprecedented nanocarrier targeting to early intraerythrocytic stages of the malaria parasite for which there is a lack of specific extracellular molecular tags. Polyethylene glycol-coated liposomes conjugated with monoclonal antibodies specific for the erythrocyte surface protein glycophorin A (anti-GPA iLP) were capable of targeting 100% RBCs and pRBCs at the low concentration of 0.5 μM total lipid in the culture, with >95% of added iLPs retained into the cells. When exposed for only 15 min to P. falciparum in vitro cultures synchronized at early stages, free CQ had no significant effect over parasite viability up to 200 nM drug, whereas iLP-encapsulated 50 nM CQ completely arrested its growth. Furthermore, when assayed in vivo in P. falciparum-infected humanized mice, anti-GPA iLPs cleared the pathogen below detectable levels at a CQ dose of 0.5 mg/kg. In comparison, free CQ administered at 1.75 mg/kg was, at most, 40-fold less efficient. Our data suggest that this significant improvement in drug antimalarial efficacy is in part due to a prophylactic effect of CQ found by the pathogen in its host cell right at the very moment of invasion.

Keywords: immunoliposomal nanoparticles, malaria, prophylactic-therapeutic polyvalent activity, targeted drug delivery

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Authors: Marcelus U. Ajonina, Deodata B. Ngonga, Kenric B. Ware, Carine K. Nfor

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Background: Lack of knowledge of rational use of antimalarial drugs among dispensers is a serious problem, especially in areas of intense transmission, thus increasing the risk of resistance and adverse drug reactions. This study was aimed at assessing the knowledge of malaria as well as perception and dispensing practices of antimalarials among vendors in Buea community. Methods: A community-based cross-sectional survey of a random sample of 140 drug vendors living within the Buea community was conducted between March and June 2017. A questionnaire was designed to obtain information from drug vendors on the general knowledge of malaria as well as dispensing practices. Data were analyzed using SPSS Statistics 20.0 and were considered significant at p ≤ 0.05. Results: Knowledge of malaria symptoms, transmission, and prevention was reasonable among 55.8% (77) of the respondents. Only 33.6% (47) of the respondents could attribute the cause of malaria to protozoan of genus Plasmodium species. Of the 140 vendors, 115 (82.7%) prescribe antimalarial drugs. The knowledge of the national protocol was malaria case management among dispensers was 35.0%. Vendors in hospital/community pharmacies were 2.4 times (OR = 3.14, 95% CI: 4.14 - 8.74, p < 0.001) more knowledgeable about malaria treatment protocol than those of in drugstores. The prevalence of self-prescription of antimalarials was 39.3%. Self-prescription was significantly higher in drugstores than hospital/community pharmacies (p=0.004). In all, 56 (40.6%) of vendors showed good practices regarding antimalarial drug dispensing with the majority (51.7%) from community pharmacies (OR=2.27,95% CI: 1.13-4.56). Conclusion: Findings reveal moderate knowledge of malaria but poor prescription and dispensing practices of antimalarial drugs among vendors, thus indicating a need for routine monitoring and evaluation to prevent the emergence of resistant strains to current efficacious antimalarials.

Keywords: antimalarials, drug retail outlets, dispensing, drug resistance, prescription

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Authors: Varsha Chorsiya, Pooja Aneja, Dhananjay Kaushik, Abhinav Yadav

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Intoduction: Women’s Health Initiatives (WHI) focuses on defining the risks and benefits of strategies that could potentially reduce the incidence of obesity, heart disease, breast cancer and colorectal cancer, and fractures in menopause women. The utility of the present research work determines to find the role of Hormone Replacement Therapy (HRT) in changing the different component of body composition during perimenopause period. Methods: A comparative cross-sectional study included 30 subjects, aged between 40 and 50 years which were assigned into 2 groups i.e. 15 subjects in HRT (Group A) and 15 subjects in non-HRT (Group B). The subjects were taken from the hospitals and clinics of Faridabad undergoing HRT in supervision of the consultant gynecologist. The informed consents were signed before including the participants in the study. The body composition and lipid profile were evaluated for all the subjects. Result and Discussion: The BMI, body density, percent body fats and fat mass in both groups showed statistically significant differences i.e. p < 0.05. Our study did not reveal any statistically significant difference between non-HRT and HRT for lipid profile composition of HDL, LDL, VLDL, ratio, triglycerides and total cholesterol although these indicators (LDL, VLDL, ratio, triglycerides and total cholesterol) showed difference clinically with a higher mean values for non-HRT as compared to HRT group. The mean value for HDL was higher for HRT group in contrast to non-HRT group. The result clearly showed that HRT group has a good lipid profile composition. Conclusion: In conclusion, our data show that HRT has statistically significant role in determining BMI, fat percent mass and fat mass. The lipid profile including LDL, HDL, VLDL, ratio, triglycerides and total cholesterol found to be clinically better in HRT group as compared to the non-HRT group. The rationale for non-significant lipid profile probably lie in the fact that hormonal changes need a particular time period and might become significant in post-menopausal period.

Keywords: body composition, hormone replacement therapy, perimenopause, women health

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Authors: Leila Karshenas, Hamid Reza Khodaei, Behnaz Mahdavi

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We know that nitric oxide (NO) plays an important role in all sexual activities of animals. It is made in body from NO synthase enzyme and L-arginin molecule. NO can bound with sulfur-iron complexes and because production of steroid sexual hormones is related to enzymes which have this complex, NO can change the activity of these enzymes. NO affects many cells including endothelial cells of veins, macrophages and mast cells. These cells are found in testis leydig cells and therefore are important source of NO in testis tissue. Minimizing damages to sperm at the time of sperm freezing and thawing is really important. The goal of this study was to determine the function of NO before freezing and its effects on quality and viability of sperms after thawing and incubation. 4 Holstein bulls were selected from the age of 4, and artificial insemination was done for 3 weeks (2 times a week). Treatments were 0, 10, 50 and 100 nm of sodium nitroprusside (SNP). Data analysis was performed by SAS98 program. Also, mean comparison was done using Duncan's multiple ranges test (P<0.05). Concentrations used was found to increase motility and viability of spermatozoa at 1, 2 and 3 hours after thawing significantly (P<0.05), but there was no significant difference at zero time. SNP levels reduced the amount of lipid peroxidation in sperm membrane, increased acrosome health and improved sample membranes especially in 50 and 100 nm treatments. According to results, adding SNP to semen diluents increases motility and viability of spermatozoa. Also, it reduces lipid peroxidation in sperm membrane and improves sperm function.

Keywords: sperm motility, nitric oxide, lipid peroxidation, spermatozoa

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Authors: Venkata Srikanth Meka, Nur Arthirah Binti Ahmad Tarmizi Tan, Muhammad Syahmi Bin Md Nazir, Adinarayana Gorajana, Senthil Rajan Dharmalingam

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Biphasic drug delivery systems are designed to release drug at two different rates, either fast/prolonged or prolonged/fast. A fast/prolonged release system provides a burst drug release at initial stage followed by a slow release over a prolonged period of time and in case of prolonged/fast release system, the release pattern is vice versa. Terminalia catappa gum (TCG) is a natural polymer and was successfully proven as a novel pharmaceutical excipient. The main objective of the present research is to investigate the applicability of natural polymer, Terminalia catappa gum in the design of oral biphasic drug delivery system in the form of mini tablets by using a model drug, buspirone HCl. This investigation aims to produce a biphasic release drug delivery system of buspirone by combining immediate release and prolonged release mini tablets into a capsule. For immediate release mini tablets, a dose of 4.5 mg buspirone was prepared by varying the concentration of superdisintegrant; crospovidone. On the other hand, prolonged release mini tablets were produced by using different concentrations of the natural polymer; TCG with a buspirone dose of 3mg. All mini tablets were characterized for weight variation, hardness, friability, disintegration, content uniformity and dissolution studies. The optimized formulations of immediate and prolonged release mini tablets were finally combined in a capsule and was evaluated for release studies. FTIR and DSC studies were conducted to study the drug-polymer interaction. All formulations of immediate release and prolonged release mini tablets were passed all the in-process quality control tests according to US Pharmacopoeia. The disintegration time of immediate release mini tablets of different formulations was varied from 2-6 min, and maximum drug release was achieved in lesser than 60 min. Whereas prolonged release mini tablets made with TCG have shown good drug retarding properties. Formulations were controlled for about 4-10 hrs with varying concentration of TCG. As the concentration of TCG increased, the drug release retarding property also increased. The optimised mini tablets were packed in capsules and were evaluated for the release mechanism. The capsule dosage form has clearly exhibited the biphasic release of buspirone, indicating that TCG is a suitable natural polymer for this study. FTIR and DSC studies proved that there was no interaction between the drug and polymer. Based on the above positive results, it can be concluded that TCG is a suitable polymer for the biphasic drug delivery systems.

Keywords: Terminalia catappa gum, biphasic release, mini tablets, tablet in capsule, natural polymers

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Authors: Sharjeel Abid, Tanveer Hussain, Ahsan Nazir, Abdul Zahir, Nabyl Khenoussi

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Localized application of drug has various advantages and fewer side effects as compared with other methods. Burn patients suffer from swear pain and the major aspects that are considered for burn victims include pain and infection management. Nano-fibers (NFs) loaded with drug, applied on local wound area, can solve these problems. Therefore, this study dealt with the fabrication of drug loaded NFs for better pain management. Two layers of NFs were fabricated with different drugs. Contact layer was loaded with Gabapentin (a nerve painkiller) and the second layer with acetaminophen. The fabricated dressing was characterized using scanning electron microscope, Fourier Transform Infrared Spectroscopy, X-Ray Diffraction and UV-Vis Spectroscopy. The double layered based NFs dressing was designed to have both initial burst release followed by slow release to cope with pain for two days. The fabricated nanofibers showed diameter < 300 nm. The liquid absorption capacity of the NFs was also checked to deal with the exudate. The fabricated double layered dressing with dual drug loading and release showed promising results that could be used for dealing pain in burn victims. It was observed that by the addition of drug, the size of nanofibers was reduced, on the other hand, the crystallinity %age was increased, and liquid absorption decreased. The combination of fast nerve pain killer release followed by slow release of non-steroidal anti-inflammatory drug could be a good tool to reduce pain in a more secure manner with fewer side effects.

Keywords: pain management, burn wounds, nano-fibers, controlled drug release

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Authors: S. S. Patil, R. M. Mhetre, S. V. Patil

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Lisinopril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and heart failure in prophylactic treatment after myocardial infarction and in diabetic nephropathy. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of lisinopril by formulating intranasal microspheres with Carbopol 974P NF and HPMC K4 M along with film forming polymer ethyl cellulose.The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, ex vivo mucoadhesion, drug release, ex vivo diffusion studies. All formulations has shown entrapment efficiency between 80 to more than 95%, mucoadhesion was more than 80 % and drug release up to 90 %. Ex vivo studies revealed tht the improved bioavailability of drug compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres shown better results than single carbopol based microspheres for the delivery of lisinopril.

Keywords: microspheres, lisinopril, nasal delivery, solvent evaporation method

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Authors: Rashi Rajput, Manisha Singh

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Escitalopram oxalate (ETP), an FDA approved antidepressant drug from the category of SSRI (selective serotonin reuptake inhibitor) and is used in treatment of general anxiety disorder (GAD), major depressive disorder (MDD).When taken orally, it is metabolized to S-demethylcitalopram (S-DCT) and S-didemethylcitalopram (S-DDCT) in the liver with the help of enzymes CYP2C19, CYP3A4 and CYP2D6. Hence, causing side effects such as dizziness, fast or irregular heartbeat, headache, nausea etc. Therefore, targeted and sustained drug delivery will be a helpful tool for increasing its efficacy and reducing side effects. The present study is designed for formulating mucoadhesive nanoparticle formulation for the same Escitalopram loaded polymeric nanoparticles were prepared by ionic gelation method and characterization of the optimised formulation was done by zeta average particle size (93.63nm), zeta potential (-1.89mV), TEM (range of 60nm to 115nm) analysis also confirms nanometric size range of the drug loaded nanoparticles along with polydispersibility index of 0.117. In this research, we have studied the in vitro drug release profile for ETP nanoparticles, through a semi permeable dialysis membrane. The three important characteristics affecting the drug release behaviour were – particle size, ionic strength and morphology of the optimised nanoparticles. The data showed that on increasing the particle size of the drug loaded nanoparticles, the initial burst was reduced which was comparatively higher in drug. Whereas, the formulation with 1mg/ml chitosan in 1.5mg/ml tripolyphosphate solution showed steady release over the entire period of drug release. Then this data was further validated through mathematical modelling to establish the mechanism of drug release kinetics, which showed a typical linear diffusion profile in optimised ETP loaded nanoparticles.

Keywords: ionic gelation, mucoadhesive nanoparticle, semi-permeable dialysis membrane, zeta potential

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Authors: Jichan Jang

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Mycobacterium abscessus is a rapidly growing life-threatening mycobacterium with multiple drug-resistance mechanisms. In this study, we screened the library to identify active molecules targeting Mycobacterium abscessus using resazurin live/dead assays. In this screening assay, the Z-factor was 0.7, as an indication of the statistical confidence of the assay. A cut-off of 80% growth inhibition in the screening resulted in the identification of four different compounds at a single concentration (20 μM). Dose-response curves identified three different hit candidates, which generated good inhibitory curves. All hit candidates were expected to have different molecular targets. Thus, we found that compound X, identified, may be a promising candidate in the M. abscessus drug discovery pipeline.

Keywords: Mycobacterium abscessus, antibiotics, drug discovery, emerging Pathogen

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Authors: Nura Lawal, Lawal Suleiman Bilbis, Rabiu Aliyu Umar, Anas A. Sabir

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Metabolic syndrome (MS) a high-risk condition involving obesity, dyslipidemia, hypertension, and diabetes mellitus is prevalent in Nigeria. The study aims to formulate an antioxidant-rich nutraceutical from locally available foodstuff (onion, garlic, ginger, tomato, lemon, palm oil, watermelon seeds) and investigate their effects on blood pressure, body weight, serum glucose, lipid profile, insulin and oxidative stress markers in salt-induced rats. The rats were placed on 8% salt diet for 6 weeks and then supplementation and treatment with nutraceutical and nifedipine in the presence of salt diet for additional 4 weeks. Feeding rats with salt diet for 6 weeks increased blood pressure and body weight of the salt-loaded rats relative to control. Significant (P < 0.001) increase in serum blood glucose and lipid profile, and the decrease in high-density lipoprotein-cholesterol (HDL-C) was observed in salt-loaded rats as compared with control. Both supplementation and treatment (nifedipine) lowered the blood pressure but the only supplementation lowered the body weight. Supplementation with nutraceutical resulted in significant (P < 0.001) decrease in the serum blood glucose, lipid profile, malonyldialdehyde (MDA), insulin levels, insulin resistance, and increased HDL-C and antioxidant indices. The percentage protection against atherogenesis was 76.5±2.13%. There is strong positive correlation between blood pressure, body weight and serum blood glucose, lipid profile, markers of oxidative stress and strong negative correlation with HDL-C and antioxidant status. The results suggest that the nutraceuticals are useful in reversing most of the component of metabolic syndrome and might be beneficial in the treatment of patients with metabolic syndrome.

Keywords: metabolic syndrome, hypertension, diabetes mallitus, obesity

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Authors: Khadijat Ayanpeju Abdulsalam, Bolanle Mary Olawoye, Paul Babatunde Ayoola

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The potential of Baobab leaves is understudied and not yet fully documented. The purpose of this work is to highlight the important nutritional value and practical qualities of baobab leaves. In this research, proximate analysis was studied to determine the macronutrient quantitative analysis in baobab leaves. Studies were also conducted on other characteristics, such as moisture content, which is significant to the food business since it affects food quality, preservation, and resistance to deterioration. Dietary fiber, which was also studied, has important health benefits, such as lowering blood cholesterol levels by lowering low-density lipoprotein or "bad" cholesterol. It functions as an anti-obesity and anti-diabetic agent, lowering the likelihood of haemorrhoids developing. Additionally, increasing face bulk and short-chain fatty acid synthesis improves gastrointestinal health and overall wellness. Baobab leaves had a moisture content of 6.4%, fat of 16.1%, ash of 3.2%, protein of 18.7%, carbohydrate 57.2% and crude fiber of 4.1%. The minerals determined in the sample of baobab leaves are Ca, Fe, Mg, K, Na, P, and Zn with Potassium (347.6±0.70) as the most abundant mineral while Zn (9.31±0.60) is the least abundant. The functional properties studied include pH, gelation temperature, bulk density, water absorption capacity, oil absorption capacity, foaming property, emulsifying property, and stability and swelling capacity, which are 8.72, 29, 0.39, 138, 98.20, 0.80, 72.80, and 73.50 respectively. The Fourier Transform InfraRed absorption spectra show bands like C=O, C-Cl and N-H. Baobab leaves are edible, nutritious, and non-toxic, as the mineral contents are within the required range.

Keywords: dietary fibre, proximate analysis, macronutrients, minerals, baobab leaves, frequency range

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Authors: Zhipeng Dong, Jing Guo

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Graphene-semiconductor contacts have been extensively studied recently, both as a stand-alone diode device for potential applications in photodetectors and solar cells, and as a building block to vertical transistors. Graphene is a two-dimensional nanomaterial with vanishing density-of-states at the Dirac point, which differs from conventional metal. In this work, image-charge-induced barrier lowering (BL) in graphene-semiconductor contacts is studied and compared to that in metal Schottky contacts. The results show that despite of being a semimetal with vanishing density-of-states at the Dirac point, the image-charge-induced BL is significant. The BL value can be over 50% of that of metal contacts even in an intrinsic graphene contacted to an organic semiconductor, and it increases as the graphene doping increases. The dependences of the BL on the electric field and semiconductor dielectric constant are examined, and an empirical expression for estimating the image-charge-induced BL in graphene-semiconductor contacts is provided.

Keywords: graphene, semiconductor materials, schottky barrier, image charge, contacts

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Authors: Malith Premarathne, Shehan Bandara, Kaushalya G. Batawala, Thilini U. Ariyadasa

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The rapid depletion of fossil fuel supplies and the emission of carbon dioxide by their continued combustion have paved the way for increased production of carbon-neutral biodiesel from naturally occurring oil sources. The high biomass growth rate and lipid production of microalgae make it a viable source for biodiesel production compared to conventional feedstock. In Sri Lanka, the production of biodiesel by employing indigenous microalgae species is at its emerging stage. This work was an attempt to compare the various pre-treatment methods before extracting lipids such as autoclaving, microwaving and sonication. A mixed culture of microalgae predominantly consisting of Chlorella sp. was obtained from Beire Lake which is an algae rich, organically polluted water body located in Colombo, Sri Lanka. After each pre-treatment method, a standard solvent extraction using Bligh and Dyer’s method was used to compare the total lipid content in percentage dry weight (% dwt). The fatty acid profiles of the oils extracted with each pretreatment method were analyzed using gas chromatography-mass spectrometry (GC-MS). The properties of the biodiesels were predicted by Biodiesel Analyzer© Version 1.1, in order to compare with ASTM 6751-08 biodiesel standard.

Keywords: biodiesel, lipid extraction, microalgae, pre-treatment

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Authors: O. E. Okafor, L. U. S. Ezeanyika, C. G. Nkwonta, C. J. Okonkwo

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The effect of processing on plasma lipid profile and atherogenic indices of rats fed Artocarpus heterophyllus seed diets at different concentrations were investigated. Fifty five rats were used for this study, they were divided into eleven groups of five rats each (one control group and ten test groups), the test groups were fed raw, boiled, roasted, fermented, and soaked diets at 10 % and 40% concentrations. The study lasted for thirty five days. The diets led to significant decrease (p < 0.05) in plasma cholesterol and triacylglycerol of rats fed 10% and 40% concentrations of the diets, and a significant increase (p < 0.05) in high density lipoprotein (HDL) levels at 40% concentrations of the test diets. The diets also produced decrease in low density lipoprotein (LDL), very low density lipoprotein (VLDL), cardiac risk ratio (CRR), atherogenic index of plasma (AIP) and atherogenic coefficient (AC) at 40% concentrations except the soaked group that showed slight elevation of LDL, CRR, AC and AIP at 40% concentration. Artocarpus heterophyllus seeds could be beneficial to health because of its ability to increase plasma HDL and reduce plasma LDL, VLDL, cholesterol, triglycerides and atherogenic indices at higher diet concentration.

Keywords: artocarpus heterophyllus, atherogenic indices, concentrations, lipid profile

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Authors: Umairah Natasya Binti Mohd Omeershffudin, Suresh Kumar

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Klebsiella pneumoniae, a Gram-negative enteric bacterium that causes nosocomial and urinary tract infections. Particular concern is the global emergence of multidrug-resistant (MDR) strains of Klebsiella pneumoniae. Characterization of antibiotic resistance determinants at the genomic level plays a critical role in understanding, and potentially controlling, the spread of multidrug-resistant (MDR) pathogens. In this study, drug-resistant Klebsiella pneumoniae strain 825795-1 was investigated with extensive computational approaches aimed at identifying novel drug targets among hypothetical proteins. We have analyzed 1099 hypothetical proteins available in genome. We have used in-silico genome subtraction methodology to design potential and pathogen-specific drug targets against Klebsiella pneumoniae. We employed bioinformatics tools to subtract the strain-specific paralogous and host-specific homologous sequences from the bacterial proteome. The sorted 645 proteins were further refined to identify the essential genes in the pathogenic bacterium using the database of essential genes (DEG). We found 135 unique essential proteins in the target proteome that could be utilized as novel targets to design newer drugs. Further, we identified 49 cytoplasmic protein as potential drug targets through sub-cellular localization prediction. Further, we investigated these proteins in the DrugBank databases, and 11 of the unique essential proteins showed druggability according to the FDA approved drug bank databases with diverse broad-spectrum property. The results of this study will facilitate discovery of new drugs against Klebsiella pneumoniae.

Keywords: pneumonia, drug target, hypothetical protein, subtractive genomics

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Authors: Umme Hani, Mohammed Rahmatulla, Mohammed Ghazwani, Ali Alqahtani, Yahya Alhamhoom

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Background and introduction: Neratinib is a potent anticancer drug used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower gastrointestinal tract (GIT) leading to poor bioavailability. An attempt has been made to prepare and develop a gastro-retentive system of Neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. Materials and methods: In the present study a three-factor at two-level (23) factorial design based optimization was used to inspect the effects of three independent variables (factors) such as sodium alginate (A), sodium bicarbonate (B) and sodium citrate (C) on the dependent variables like in vitro gelation, in vitro floating, water uptake and percentage drug release. Results: All the formulations showed pH in the range 6.7 ±0.25 to 7.4 ±0.24, percentage drug content was observed to be 96.3±0.27 to 99.5 ±0.28%, in vitro gelation observed as gelation immediate remains for an extended period. Percentage of water uptake was in the range between 9.01±0.15 to 31.01±0.25%, floating lag time was estimated form 7±0.39 to 57±0.36 sec. F4 and F5 showed floating even after 12hrs. All formulations showed a release of around 90% drug release within 12hr. It was observed that the selected independent variables affect the dependent variables. Conclusion: The developed system may be a promising and alternative approach to augment gastric retention of drugs and enhances the therapeutic efficacy of the drug.

Keywords: neratinib, 2³ factorial design, sodium alginate, floating, in situ gelling system

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Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

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Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability

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