Search results for: drug target interaction

Authors: Mohammad Izadkhah, Mojtaba Hoseini, Alireza Khalili Tehrani

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In this paper we presented a new method for tracking flying targets in color video sequences based on contour and kernel. The aim of this work is to overcome the problem of losing target in changing light, large displacement, changing speed, and occlusion. The proposed method is made in three steps, estimate the target location by particle filter, segmentation target region using neural network and find the exact contours by greedy snake algorithm. In the proposed method we have used both region and contour information to create target candidate model and this model is dynamically updated during tracking. To avoid the accumulation of errors when updating, target region given to a perceptron neural network to separate the target from background. Then its output used for exact calculation of size and center of the target. Also it is used as the initial contour for the greedy snake algorithm to find the exact target's edge. The proposed algorithm has been tested on a database which contains a lot of challenges such as high speed and agility of aircrafts, background clutter, occlusions, camera movement, and so on. The experimental results show that the use of neural network increases the accuracy of tracking and segmentation.

Keywords: video tracking, particle filter, greedy snake, neural network

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Authors: Christine M. Corrales, Gloria G. Delan, Rachel Luz V. Rica, Alfonso S. Piquero

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Marine protected areas (MPAs) in the study sites were established 8-13 years ago and are presently operational. This study was conducted to gather baseline information on the diversity, density and biomass of coral reef fishes inside and outside the four marine protected areas (MPAs) of Cawayan, Dalaguete; Daan-Lungsod Guiwang, Alcoy; North Granada, Boljoon and Sta. Cruz, Ronda. Coral reef fishes in the MPAs were identified using Fish Visual Census Method. Results of the t-test showed that the mean diversity (fish species/250m2) of target and non-target reef fish species found inside and outside the MPAs were significantly different. Density (ind./1,000m2) of target species inside and outside the MPAs showed no significant difference. Similarly, density of non-target species inside and outside the MPAs also showed no significant difference. This is an indication that fish density inside and outside the MPAs were more or less of the same condition. The mean biomass (kg/1,000m2) of target species inside and outside the MPAs showed a significant difference in contrast with non-target species inside and outside the MPAs which showed a no significant difference. Higher biomass of target fish species belonging to family Caesonidae (fusiliers) and Scaridae (parrotfishes) were commonly observed inside the MPAs. Results showed that fish species were more diverse with higher density and biomass inside the MPAs than the outside area. However, fish diversity and density were mostly contributed by non-target species. Hence, long term protection and management of MPAs is needed to effectively increase fish diversity, density and biomass specifically on target fish species.

Keywords: biomass, density, diversity, marine protected area, target fish species

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Authors: Lorico D. S. Lapitan Jr., Yihan Xu, Yuan Guo, Dejian Zhou

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The ability of ultrasensitive detection of specific genes and discrimination of single nucleotide polymorphisms is important for clinical diagnosis and biomedical research. Herein, we report the development of a new ultrasensitive approach for label-free DNA detection using magnetic nanoparticle (MNP) assisted rapid target capture/separation in combination with signal amplification using poly-enzyme tagged polymer nanobead. The sensor uses an MNP linked capture DNA and a biotin modified signal DNA to sandwich bind the target followed by ligation to provide high single-nucleotide polymorphism discrimination. Only the presence of a perfect match target DNA yields a covalent linkage between the capture and signal DNAs for subsequent conjugation of a neutravidin-modified horseradish peroxidase (HRP) enzyme through the strong biotin-nuetravidin interaction. This converts each captured DNA target into an HRP which can convert millions of copies of a non-fluorescent substrate (amplex red) to a highly fluorescent product (resorufin), for great signal amplification. The use of polymer nanobead each tagged with thousands of copies of HRPs as the signal amplifier greatly improves the signal amplification power, leading to greatly improved sensitivity. We show our biosensing approach can specifically detect an unlabeled DNA target down to 10 aM with a wide dynamic range of 5 orders of magnitude (from 0.001 fM to 100.0 fM). Furthermore, our approach has a high discrimination between a perfectly matched gene and its cancer-related single-base mismatch targets (SNPs): It can positively detect the perfect match DNA target even in the presence of 100 fold excess of co-existing SNPs. This sensing approach also works robustly in clinical relevant media (e.g. 10% human serum) and gives almost the same SNP discrimination ratio as that in clean buffers. Therefore, this ultrasensitive SNP biosensor appears to be well-suited for potential diagnostic applications of genetic diseases.

Keywords: DNA detection, polymer beads, signal amplification, single nucleotide polymorphisms

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Authors: Annie Ramanbhai Mecwan

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Cleaning validation in a pharmaceutical manufacturing facility is documented evidence that a cleaning process has effectively removed contaminants, residues from previous drug products and cleaning agents below a pre-defined threshold from the reusable tools and parts of equipment. In shared manufacturing facilities more than one drug product is prepared. After cleaning of reusable tools and parts of equipment after one drug product manufacturing, there are chances that some residues of drug substance from previously manufactured drug products may be retained on the equipment and can carried forward to the next drug product and thus cause cross-contamination. Health-based limits through the derivation of a safe threshold value called permitted daily exposure (PDE) for the residues of drug substances should be employed to identify the risks posed at these manufacturing facilities. The PDE represents a substance-specific dose that is unlikely to cause an adverse effect if an individual is exposed to or below this dose every day for a lifetime. There are different practices to calculate PDE. Data for all APIs in the public domain are considered to calculate PDE value though, company to company may vary the final PDE value based on different toxicologist’s perspective or their subjective evaluation. Hence, Regulatory agencies should take responsibility for publishing PDE values for all APIs as it is done for elemental PDEs. This will harmonize the PDE values all over the world and prevent the unnecessary load on manufacturers for cleaning validation

Keywords: active pharmaceutical ingredient, good manufacturing practice, NOAEL, no observed adverse effect level, permitted daily exposure

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Authors: Qin Wei

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There has been an increased number of immigrants arriving in Canada and a concurrent rise in the number of immigrant youth suffering from drug abuse. Immigrant youths’ drug abuse has become a significant social and public health concern for researchers. This literature review explores the nature of immigrant youths’ drug abuse by examining the factors influencing the onset of substance misuse, the barriers that discourage youth to seek out treatment, and how to resolve addictions amidst immigrant youth. Findings from the literature demonstrate that diminished parental supervision, acculturation challenges, peer conformity, discrimination, and ethnic marginalization are all significant factors influencing youth to use drugs as an outlet for their pain, while culturally competent care and fear of family and culture-based addiction stigma act as barriers discouraging youth from seeking out addiction support. To resolve addiction challenges amidst immigrant youth, future research should focus on promoting and implementing culturally sensitive practices and psychoeducational initiatives into immigrant communities and within public health policies.

Keywords: approaches, barriers, drug abuse, Canada, immigrant youth, reasons

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Authors: Leslie Raphael de M. Ferraz, Salvana Priscylla M. Costa, Tarcyla de A. Gomes, Giovanna Christinne R. M. Schver, Cristóvão R. da Silva, Magaly Andreza M. de Lyra, Danilo Augusto F. Fontes, Larissa A. Rolim, Amanda Carla Q. M. Vieira, Miracy M. de Albuquerque, Pedro J. Rolim-Neto

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Efavirenz (EFV) is a drug used as first-line treatment of AIDS. However, it has poor aqueous solubility and wettability, presenting problems in the gastrointestinal tract absorption and bioavailability. One of the most promising strategies to improve the solubility is the use of solid dispersions (SD). Therefore, this study aimed to characterize SD EFZ with the polymers: PVP-K30, PVPVA 64 and SOLUPLUS in order to find an optimal formulation to compose a future pharmaceutical product for AIDS therapy. Initially, Physical Mixtures (PM) and SD with the polymers were obtained containing 10, 20, 50 and 80% of drug (w/w) by the solvent method. The best formulation obtained between the SD was selected by in vitro dissolution test. Finally, the drug-carrier system chosen, in all ratios obtained, were analyzed by the following techniques: Differential Scanning Calorimetry (DSC), polarization microscopy, Scanning Electron Microscopy (SEM) and spectrophotometry of absorption in the region of infrared (IR). From the dissolution profiles of EFV, PM and SD, the values of area Under The Curve (AUC) were calculated. The data showed that the AUC of all PM is greater than the isolated EFV, this result is derived from the hydrophilic properties of the polymers thus favoring a decrease in surface tension between the drug and the dissolution medium. In adittion, this ensures an increasing of wettability of the drug. In parallel, it was found that SD whom had higher AUC values, were those who have the greatest amount of polymer (with only 10% drug). As the amount of drug increases, it was noticed that these results either decrease or are statistically similar. The AUC values of the SD using the three different polymers, followed this decreasing order: SD PVPVA 64-EFV 10% > SD PVP-K30-EFV 10% > SD Soluplus®-EFV 10%. The DSC curves of SD’s did not show the characteristic endothermic event of drug melt process, suggesting that the EFV was converted to its amorphous state. The analysis of polarized light microscopy showed significant birefringence of the PM’s, but this was not observed in films of SD’s, thus suggesting the conversion of the drug from the crystalline to the amorphous state. In electron micrographs of all PM, independently of the percentage of the drug, the crystal structure of EFV was clearly detectable. Moreover, electron micrographs of the SD with the two polymers in different ratios investigated, we observed the presence of particles with irregular size and morphology, also occurring an extensive change in the appearance of the polymer, not being possible to differentiate the two components. IR spectra of PM corresponds to the overlapping of polymer and EFV bands indicating thereby that there is no interaction between them, unlike the spectra of all SD that showed complete disappearance of the band related to the axial deformation of the NH group of EFV. Therefore, this study was able to obtain a suitable formulation to overcome the solubility limitations of the EFV, since SD PVPVA 64-EFZ 10% was chosen as the best system in delay crystallization of the prototype, reaching higher levels of super saturation.

Keywords: characterization, dissolution, Efavirenz, solid dispersions

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Authors: Hana Ashique, Florence Onabanjo

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Objectives: Research on drug abuse education in secondary schools has highlighted the discrepancy between drug policies and practice. Drug abuse is closely associated with child mental health, and with increasing drug overdose deaths in the UK, approximately doubling in the last 30 years, it becomes important to revolutionise drug abuse education. Medical professionals from the University of Nottingham piloted a drug abuse workshop at a state school in Nottingham for children between the age of 14-15 years. An interactive and educational approach was implemented, which explained addiction from a medical perspective. The workshop aimed to debunk medical beliefs children harboured about drugs and to support children in making informed drug choices. Methods: The sample group consisted of six cohorts of 30 children from year 10. The workshop was delivered in three segments to each cohort. In the first segment, the children were introduced to the physiological mechanisms behind drug dependence and reward pathways. The second segment consisted of interactive discussions between the children and medical professionals. This also involved conversations between the children about their perspectives on drug abuse, thereby co-creating knowledge. The third segment used art to incorporate storytelling from the perspective of a year ten child. This exercise investigated the causes that led children to abuse drugs. A feedback questionnaire was distributed among the children to analyse the impact of the workshop. Results: The children answered eight questions. 56% agreed/strongly agreed that they found being taught by medical professionals effective. 50% disagreed, strongly disagreed, or felt neutral that they had received sufficient education about drug abuse previously. Notably, 20% agreed that they feel more likely to ask for help from a medical professional or organisation if they need it. Conclusion: The results highlighted the relevance of medical professionals to function as peer educators in drug abuse education to secondary school children. This would build trust between children and the medical profession within the community. However, a minority proportion of children showed keenness to seek support from medical professionals or organisations for their mental health if they needed it. This exposed the anxiety children have in coming forward to seek professional help. In order to work towards a child-centred approach, educational policies and practices need to align. Similar workshops and research may need to be conducted to expose different perspectives toward drug abuse education.

Keywords: adolescent mental health, evidence-based teaching, drug abuse awareness, medical professional led workshops

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Authors: Dequn Teng, Tianshuo Yang, Mingrui Wang, Qiuyu Chen, Xiao Wang, Katie Atkinson

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Currently, many students are kind of at a loss in the university due to the complex environment within the campus, where every information within the campus is isolated with fewer interactions with each other. However, if the on-campus resources are gathered and combined with the artificial intelligence modelling techniques, there will be a bridge for not only students in understanding themselves, and the teachers will understand students in providing a much efficient approach in education. The objective of this paper is to provide a competency level analysis method, apparatus, electronic equipment, and storage medium. It uses a user’s target competency level analysis model from a plurality of predefined candidate competency level analysis models by obtaining a user’s promotion target parameters, promotion target parameters including at least one of the following parameters: target profession, target industry, and the target company, according to the promotion target parameters. According to the parameters, the model analyzes the user’s ability level, determines the user’s ability level, realizes the quantitative and personalized analysis of the user’s ability level, and helps the user to objectively position his ability level.

Keywords: artificial intelligence, model, university, education, recommendation system, evaluation, job hunting

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Authors: Abhisek Sinha, Debobrata Rajak, Shilpa Rani, Ram Gopal, Vandana Sharma

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The interaction of femtosecond laser pulses with metallic tips has been studied extensively, and they have proved to be a very good source of ultrashort electron pulses. A study of the interaction of femtosecond Laguerre-Gaussian (LG) laser modes with Tungsten tips is presented here. Laser pulses of 35 fs pulse durations were incident on Tungsten tips, and their electron emission rates were studied for LG (l=1, p=0) and Gaussian modes. A change in the order of the interaction for LG beams is reported, and the difference in the order of interaction is attributed to ponderomotive shifts in the energy levels corresponding to the enhanced near-field intensity supported by numerical simulations.

Keywords: femtosecond, Laguerre-Gaussian, OAM, tip

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Authors: Eda Orhun

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Purpose: This paper analyzes a target firm’s decision to voluntarily disclose information during a takeover event and the effect of such disclosures on the outcome of the takeover. Such voluntary disclosures especially in the form of earnings forecasts made around takeover events may affect shareholders’ decisions about the target firm’s value and in return takeover result. This study aims to shed light on this question. Design/methodology/approach: The paper tries to understand the role of voluntary disclosures by target firms during a takeover event in the likelihood of takeover success both theoretically and empirically. A game-theoretical model is set up to analyze the voluntary disclosure decision of a target firm to inform the shareholders about its real worth. The empirical implication of model is tested by employing binary outcome models where the disclosure variable is obtained by identifying the target firms in the sample that provide positive news by issuing increasing management earnings forecasts. Findings: The model predicts that a voluntary disclosure of positive information by the target decreases the likelihood that the takeover succeeds. The empirical analysis confirms this prediction by showing that positive earnings forecasts by target firms during takeover events increase the probability of takeover failure. Overall, it is shown that information dissemination through voluntary disclosures by target firms is an important factor affecting takeover outcomes. Originality/Value: This study is the first to the author's knowledge that studies the impact of voluntary disclosures by the target firm during a takeover event on the likelihood of takeover success. The results contribute to information economics, corporate finance and M&As literatures.

Keywords: takeovers, target firm, voluntary disclosures, earnings forecasts, takeover success

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Authors: Ashish Jain, Shivam Tayal

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There has been great interest in the field of Iontophoresis since few years due to its great applications in the field of controlled transdermal drug delivery system. It is an technique which is used to enhance the transdermal permeation of ionized high molecular weight molecules across the skin membrane especially Peptides & Proteins by the application of direct current of 1-4 mA for 20-40 minutes whereas chemical must be placed on electrodes with same charge. Iontophoresis enhanced the delivery of drug into the skin via pores like hair follicles, sweat gland ducts etc. rather than through stratum corneum. It has wide applications in the field of experimental, Therapeutic, Diagnostic, Dentistry etc. Medical science is using it to treat Hyperhidrosis (Excessive sweating) in hands and feet and to treat other ailments like hypertension, Migraine etc. Nowadays commercial transdermal iontophoretic patches are available in the market to treat different ailments. Researchers are keen to research in this field due to its vast applications and advantages.

Keywords: iontophoresis, novel drug delivery, transdermal, permeation enhancer

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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: Eduardo Álvarez, Gerardo Quiroga, Jorge Orozco, Gabriel Chavira

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AmI proposes a new way of thinking about computers, which follows the ideas of the Ubiquitous Computing vision of Mark Weiser. In these, there is what is known as a Disappearing Computer Initiative, with users immersed in intelligent environments. Hence, technologies need to be adapted so that they are capable of replacing the traditional inputs to the system by embedding these in every-day artifacts. In this work, we present an approach, which uses Radiofrequency Identification (RFID) and Near Field Communication (NFC) technologies. In the latter, a new form of interaction appears by contact. We compare both technologies by analyzing their requirements and advantages. In addition, we propose using a combination of RFID and NFC.

Keywords: touching interaction, ambient intelligence, ubiquitous computing, interaction, NFC and RFID

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Authors: Bushra Nabi, Saleha Rehman, Sanjula Baboota, Javed Ali

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Aim: The objective of research undertaken is analytical method validation (HPLC method) of an anti-HIV drug Elvitegravir (EVG). Additionally carrying out the forced degradation studies of the drug under different stress conditions to determine its stability. It is envisaged in order to determine the suitable technique for drug estimation, which would be employed in further research. Furthermore, comparative pharmacokinetic profile of the drug from lipid architectonics and drug suspension would be obtained post oral administration. Method: Lipid Architectonics (LA) of EVR was formulated using probe sonication technique and optimized using QbD (Box-Behnken design). For the estimation of drug during further analysis HPLC method has been validation on the parameters (Linearity, Precision, Accuracy, Robustness) and Limit of Detection (LOD) and Limit of Quantification (LOQ) has been determined. Furthermore, HPLC quantification of forced degradation studies was carried out under different stress conditions (acid induced, base induced, oxidative, photolytic and thermal). For pharmacokinetic (PK) study, Albino Wistar rats were used weighing between 200-250g. Different formulations were given per oral route, and blood was collected at designated time intervals. A plasma concentration profile over time was plotted from which the following parameters were determined:

Keywords: AIDS, Elvitegravir, HPLC, nanostructured lipid carriers, pharmacokinetics

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Authors: Melkamu Tadesse Getachew

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Intelligent control systems have revolutionized biomedical engineering, advancing research and enhancing medical practice. This review paper examines the impact of intelligent control on various aspects of biomedical engineering. It analyzes how these systems enhance precision and accuracy in biomedical instrumentation, improving diagnostics, monitoring, and treatment. Integration challenges are addressed, and potential solutions are proposed. The paper also investigates the optimization of drug delivery systems through intelligent control. It explores how intelligent systems contribute to precise dosing, targeted drug release, and personalized medicine. Challenges related to controlled drug release and patient variability are discussed, along with potential avenues for overcoming them. The comparison of algorithms used in intelligent control systems in biomedical control is also reviewed. The implications of intelligent control in computational and systems biology are explored, showcasing how these systems enable enhanced analysis and prediction of complex biological processes. Challenges such as interpretability, human-machine interaction, and machine reliability are examined, along with potential solutions. Intelligent control in biomedical engineering also plays a crucial role in risk management during surgical operations. This section demonstrates how intelligent systems improve patient safety and surgical outcomes when integrated into surgical robots, augmented reality, and preoperative planning. The challenges associated with these implementations and potential solutions are discussed in detail. In summary, this review paper comprehensively explores the widespread impact of intelligent control on biomedical engineering, showing the future of human health issues promising. It discusses application areas, challenges, and potential solutions, highlighting the transformative potential of these systems in advancing research and improving medical practice.

Keywords: Intelligent control systems, biomedical instrumentation, drug delivery systems, robotic surgical instruments, Computational monitoring and modeling

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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: Kimmo J. Kurppa

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This paper describes the development of the buyer-supplier dyad concept over the years and proposes improvements, clarifications and extensions to the prevailing definitions published in 1970’s and 1980’s. This paper suggests a partition of the buyer-supplier dyad to concepts of Commercial Dyad (dyadic interaction in vertical relationships) and Innovative Dyad (dyadic interaction in horizontal relationship) since dyadic interaction takes place in two major types of contexts between industrial firms. Especially the context of joint product development in a dyadic relationship has not been adequately recognized being totally different from the interaction taking place in commercial buyer-supplier interaction. This paper provides therefore a solution to the existing gap in research by clarifying the descriptions and the context where dyadic interaction takes place between industrial firms. This paper also illustrates and explains how the firm’s organization and the interaction taking place inside it, is connected to the dyadic interaction structure between the firm and its partner firm. This theme has been discussed earlier but the phenomenon has not been adequately described and has not been illustrated in earlier research. This conceptual study has been interested in how the dyad concept of Industrial Marketing has been defined in the earlier research and how the definition could be improved. This conceptual paper has been constructed by using the systematic review methodology and proposes avenues for future research. The concept and existence of relationship and interaction between firm’s internal interaction network and external interaction between firm’s dyadic counterparts, need to be verified through empirical research.

Keywords: dyadic interaction, industrial dyad, buyer-supplier relationship, strategic reciprocity, experience, socially adjusted opportunism

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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: 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: Surendra Agrawal, Pravina Gurjar, Supriya Bhide, Ram Gaud

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Levamisole hydrochloride is a prominent anticancer drug in the treatment of colon cancer but resulted in toxic effects due poor bioavailability and poor cellular uptake by tumor cells. Levamisole is an unstable drug. Incorporation of this molecule in solid lipids may minimize their exposure to the aqueous environment and partly immobilize the drug molecules within the lipid matrix-both of which may protect the encapsulated drugs against degradation. The objectives of the study were to enhance bioavailability by sustaining drug release and to reduce the toxicities associated with the therapy. Solubility of the drug was determined in different lipids to select the components of Solid Lipid Nanoparticles (SLN). Pseudoternary phase diagrams were created using aqueous titration method. Formulations were subjected to particle size and stability evaluation to select the final test formulations which were characterized for average particle size, zeta potential, and in-vitro drug release and percentage transmittance to optimize the final formulation. SLN of Levamisole hydrochloride was prepared by Nanoprecipitation method. Glyceryl behenate (Compritol 888 ATO) was used as core comprising of Tween 80 as surfactant and Lecithin as co-surfactant in (1:1) ratio. Entrapment efficiency (EE) was found to be 45.89%. Particle size was found in the range of 100-600 nm. Zeta potential of the formulation was -17.0 mV revealing the stability of the product. In-vitro release study showed that 66 % drug released in 24 hours in pH 7.2 which represent that formulation can give controlled action at the intestinal environment. In pH 5.0 it showed 64% release indicating that it can even release drug in acidic environment of tumor cells. In conclusion, results revealed SLN to be a promising approach to sustain the drug release so as to increase bioavailability and cellular uptake of the drug with reduction in toxic effects as dose has been reduced with controlled delivery.

Keywords: SLN, nanoparticulate delivery of levamisole, pharmacy, pharmaceutical sciences

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Authors: Zohreh Bayat, Dariush Minai-Tehrani

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Pseudomonas aeruginosa is a Gram-negative, rode shape and aerobic bacterium that has shown to be resistance to many antibiotics. This resistance makes the bacterium very harmful in some diseases. It can also generate diseases in any part of the gastrointestinal tract from oropharynx to rectum. P. aeruginosa has become an important cause of infection, especially in patients with compromised host defense mechanisms. One of the most important reasons that make P. aeruginosa an emerging opportunistic pathogen in patients is its ability to use various compounds as carbon sources. Lipase is an enzyme that catalyzes the hydrolysis of lipids. Most lipases act at a specific position on the glycerol backbone of lipid substrate. Some lipases are expressed and secreted by pathogenic organisms during the infection. Muscarinic antagonist used as an antispasmodic and in urinary incontinence. The drug has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms. Aim: In this study the inhibitory effect of a muscarinic antagonist on lipase of P. aeruginosa was investigated. Methods: P. aeruginosa was cultured in minimal salt medium with 1% olive oil as carbon source. The cells were harvested and the supernatant, which contained lipase, was used for enzyme assay. Results: Our results showed that the drug can inhibit P. aeruginosa lipase by competitive manner. In the presence of different concentrations of the drug, the Vmax (2 mmol/min/mg protein) of enzyme did not change, while the Km raised by increasing the drug concentration. The Ki (inhibition constant) and IC50 (the half maximal inhibitory concentration) value of drug was estimated to be about 30 uM and 60 uM which determined that the drug binds to enzyme with high affinity. Maximum activity of the enzyme was observed at pH 8 in the absence and presence of muscarinic antagonist, respectively. The maximum activity of lipase was observed at 600C and the enzyme became inactive at 900C. Conclusion: The muscarinic antagonist drug could inhibit lipase of P. aeruginosa and changed the kinetic parameters of the enzyme. The drug binded to enzyme with high affinity and did not chang the optimum pH of the enzyme. Temperature did not affect the binding of drug to musmuscarinic antagonist.

Keywords: Pseudomonas aeruginosa, drug, enzyme, inhibition

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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: Pakhapoom Sarapat, James M. Hill, Duangkamon Baowan

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Carbon nanotori provide several properties such as high tensile strength and heat resistance. They are promised to be ideal structures for encapsulation, and their encapsulation ability can be determined by the interaction energy between the carbon nanotori and the encapsulated nanostructures. Such interaction energy is evaluated using Lennard-Jones potential and continuum approximation. Here, four problems relating to toroidal molecules are determined in order to find the most stable configuration. Firstly, the interaction energy between a carbon nanotorus and an atom is examined. The second problem relates to the energy of a fullerene encapsulated inside a carbon nanotorus. Next, the interaction energy between two symmetrically situated and parallel nanotori is considered. Finally, the classical mechanics is applied to model the interaction energy between the toroidal structure of cyclodextrin and the spherical DNA molecules. These mathematical models might be exploited to study a number of promising devices for future developments in bio and nanotechnology.

Keywords: carbon nanotori, continuum approximation, interaction energy, Lennard-Jones potential, nanotechnology

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Authors: Rahul Agarwal, Ashutosh Singh

Abstract:

Colorectal cancer (CRC) also refers as bowel cancer or colon cancer. It involves the development of abnormal growth of cells in colon or rectum part of the body. This work leads to the development of a miRNA database in colorectal cancer. We named this database- miCoRe. This database comprises of all validated colon-rectal cancer miRNAs information from various published literature with an effectual knowledge based information retrieval system. miRNAs have been collected from various published literature reports. MySQL is used for main-framework of miCoRe while the front-end was developed in PHP script. The aim of developing miCoRe is to create a comprehensive central repository of colorectal carcinoma miRNAs with all germane information of miRNAs and their target genes. The current version of miCoRe consists of 238 miRNAs which are known to be implicated in malignancy of CRC. Alongside with miRNA information, miCoRe also contains the information related to the target genes of these miRNA. miCoRe furnishes the information about the mechanism of incidence and progression of the disease, which would further help the researchers to look for colorectal specific miRNAs therapies and CRC specific targeted drug designing. Moreover, it will also help in development of biomarkers for the better and early detection of CRC and will help in better clinical management of the disease.

Keywords: colorectal cancer, database, miCoRe, miRNAs

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Authors: Seyed Reza Mirdehghan, Mohammad Reza Haeri Yazdi

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In this paper, the stability and the performance of a two-degree-of-freedom robot under an interaction with a unknown environment has been investigated. The time when the robot returns to its initial position after an interaction and the primary resistance of the robot against the impact must be reduced. Thus, the applied torque on the motor will be reduced. The impedance control is an appropriate method for robot control in these conditions. The stability of the robot at interaction moment was transformed to be a robust stability problem. The dynamic of the unknown environment was modeled as a weight function and the stability of the robot under an interaction with the environment has been investigated using the robust control concept. To improve the performance of the system, a force controller has been designed which the normalized impedance after interaction has been reduced. The resistance of the robot has been considered as a normalized cost function and its value was 0.593. The results has showed reduction of resistance of the robot against impact and the reduction of convergence time by lower than one second.

Keywords: impedance control, control system, robots, interaction

Procedia PDF Downloads 429

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

Procedia PDF Downloads 133

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

Abstract:

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

Procedia PDF Downloads 291