Search results for: drug withdrawal.

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

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The paper presents a process to obtain glutathione-modified titanium oxide nanoparticles. The processes were carried out in a microwave radiation field. The influence of the molar ratio of glutathione to titanium oxide and the effect of the fold of NaOH vs. stoichiometric amount on the size of the formed TiO2 nanoparticles was determined. The physicochemical properties of the obtained products were evaluated using dynamic light scattering (DLS), transmission electron microscope- energy-dispersive X-ray spectroscopy (TEM-EDS), low-temperature nitrogen adsorption method (BET), X-Ray Diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) microscopy methods. The size of TiO2 nanoparticles was characterized from 30 nm to 336 nm. The release of titanium ions from the prepared products was evaluated. These studies were carried out using different media in which the powders were incubated for a specific time. These were: water, SBF and Ringer's solution. The release of titanium ions from modified products is weaker compared to unmodified titanium oxide nanoparticles. The reduced release of titanium ions may allow the use of such modified materials as substances in drug delivery systems.

Keywords: titanium dioxide, nanoparticles, drug carrier, glutathione

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Authors: Oyelami M. Olufemi

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The menace of counterfeiting pharmaceuticals/drugs has become a major threat to consumers, healthcare providers, drug manufacturers and governments. It is a source of public health concern both in the developed and developing nations. Several solutions for detecting and authenticating counterfeit drugs have been adopted by different nations of the world. In this article, a dialogue system-based drug counterfeiting detection system was developed and the results of the user satisfaction and acceptability of the system are presented. The results show that the users were satisfied with the system and the system was widely accepted as a means of fighting counterfeited drugs.

Keywords: Counterfeiting, dialogue system, drugs, voice application.

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Authors: Amaneh Javid, Shahin Ahmadian, Ali A. Saboury, Saeed Rezaei-Zarchi

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This study determines the effect of naked and heparinbased super-paramagnetic iron oxide nanoparticles on the human cancer cell lines of A2780. Doxorubicin was used as the anticancer drug, entrapped in the SPIO-NPs. This study aimed to decorate nanoparticles with heparin, a molecular ligand for 'active' targeting of cancerous cells and the application of modified-nanoparticles in cancer treatment. The nanoparticles containing the anticancer drug DOX were prepared by a solvent evaporation and emulsification cross-linking method. The physicochemical properties of the nanoparticles were characterized by various techniques, and uniform nanoparticles with an average particle size of 110±15 nm with high encapsulation efficiencies (EE) were obtained. Additionally, a sustained release of DOX from the SPIO-NPs was successful. Cytotoxicity tests showed that the SPIO-DOX-HP had higher cell toxicity than the individual HP and confocal microscopy analysis confirmed excellent cellular uptake efficiency. These results indicate that HP based SPIO-NPs have potential uses as anticancer drug carriers and also have an enhanced anticancer effect.

Keywords: Heparin, A2780 cells, ovarian cancer, nanoparticles, doxorubicin.

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Authors: Minky Son, Chanin Park, Ayoung Baek, Shalini John, Keun Woo Lee

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3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) catalyzes the conversion of HMG-CoA to mevalonate using NADPH and the enzyme is involved in rate-controlling step of mevalonate. Inhibition of HMGR is considered as effective way to lower cholesterol levels so it is drug target to treat hypercholesterolemia, major risk factor of cardiovascular disease. To discover novel HMGR inhibitor, we performed structure-based pharmacophore modeling combined with molecular dynamics (MD) simulation. Four HMGR inhibitors were used for MD simulation and representative structure of each simulation were selected by clustering analysis. Four structure-based pharmacophore models were generated using the representative structure. The generated models were validated used in virtual screening to find novel scaffolds for inhibiting HMGR. The screened compounds were filtered by applying drug-like properties and used in molecular docking. Finally, four hit compounds were obtained and these complexes were refined using energy minimization. These compounds might be potential leads to design novel HMGR inhibitor.

Keywords: Anti-hypercholesterolemia drug, HMGR inhibitor, Molecular dynamics simulation, Structure-based pharmacophore modeling.

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Authors: A. Maitarad, P. Maitarad

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In order to find the particular interaction energy between cylcloguanil and the amino acids surrounding the pocket of wild type and quadruple mutant type PfDHFR enzymes, the MP2 method with basis set 6-31G(d,p) level of calculations was performed. The obtained interaction energies found that Asp54 has the strongest interaction energy to both wild type and mutant type of - 12.439 and -11.250 kcal/mol, respectively and three amino acids; Asp54, Ile164 and Ile14 formed the H-bonding with cycloguanil drug. Importantly, the mutation at Ser108Asn was the key important of cycloguanil resistant with showing repulsive interaction energy.

Keywords: Cycloguanil, DHFR, malaria disease, interactionenergy, quantum calculations

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Authors: Ritu Shitak

Abstract:

Humans are social mammals, of the primate order. Our biology, our behaviour and our pathologies are unique to us. In our desire to understand, reduce solitary confinement one source of information is the many reports of social isolation of other social mammals, especially primates. A behavioural study was conducted in the department of pharmacology at Indira Gandhi Medical College, Shimla in Himachalpradesh province in India using white albino mice. Different behavioural parameters were observed by using open field, tail suspension, tests for aggressive behaviour and social interactions and the effect of isolation was studied. The results were evaluated and the standard statistics were applied. The said study was done to establish facts that isolation itself impairs social behaviour and can lead to alcohol dependence as well as related drug dependence.

Keywords: Albino Mice, Drug Dependence, Social isolation.

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Authors: K. Jyothi, T. S. Mohamed Saleem, L. Vineela, C. Gopinath, K. B. Yadavender Reddy

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Objective: Acute coronary syndrome is a clinical condition encompassing ST segments elevation myocardial infraction, Non ST segment is elevation myocardial infraction and un stable angina is characterized by ruptured coronary plaque, stress and myocardial injury. Angina pectoris is a pressure like pain in the chest that is induced by exertion or stress and relived with in the minute after cessation of effort or using sublingual nitroglycerin. The present research was undertaken to study the drug utilization pattern of antiplatelet drugs for the ischemic heart disease in a tertiary care hospital. Method: The present study is retrospective drug utilization study and study period is 6months. The data is collected from the discharge case sheet of general medicine department from medical department Rajiv Gandhi institute of medical sciences, Kadapa. The tentative sample size fixed was 250 patients. Out of 250 cases 19 cases was excluded because of unrelated data. Results: A total of 250 prescriptions were collected for the study according to the inclusion criteria 233 prescriptions were diagnosed with ischemic heart disease 17 prescriptions were excluded due to unrelated information. out of 233 prescriptions 128 are male (54.9%) and 105 patients are were female (45%). According to the gender distribution, the prevalence of ischemic heart disease in males are 90 (70.31%) and females are 39 (37.1%). In the same way the prevalence of ischemic heart disease along with cerebrovascular disease in males are 39 (29.6%) and females are 66 (62.6%). Conclusion: We found that 94.8% of drug utilization of antiplatelet drugs was achieved in the Rajiv Gandhi institute of medical sciences, Kadapa from 2011-2012.

Keywords: Angina pectoris, aspirin, clopidogrel, myocardial infarction.

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Authors: G. Wagner, R. Herrmann

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Cytotoxic platinum compounds play a major role in the chemotherapy of a large number of human cancers. However, due to the severe side effects for the patient and other problems associated with their use, there is a need for the development of more efficient drugs and new methods for their selective delivery to the tumours. One way to achieve the latter could be in the use of nanoparticular substrates that can adsorb or chemically bind the drug. In the cell, the drug is supposed to be slowly released, either by physical desorption or by dissolution of the particle framework. Ideally, the cytotoxic properties of the platinum drug unfold only then, in the cancer cell and over a longer period of time due to the gradual release. In this paper, we report on our first steps in this direction. The binding properties of a series of cytotoxic Pt(II) oxadiazoline compounds to mesoporous silica particles has been studied by NMR and UV/vis spectroscopy. High loadings were achieved when the Pt(II) compound was relatively polar, and has been dissolved in a relatively nonpolar solvent before the silica was added. Typically, 6-10 hours were required for complete equilibration, suggesting the adsorption did not only occur to the outer surface but also to the interior of the pores. The untreated and Pt(II) loaded particles were characterised by C, H, N combustion analysis, BET/BJH nitrogen sorption, electron microscopy (REM and TEM) and EDX. With the latter methods we were able to demonstrate the homogenous distribution of the Pt(II) compound on and in the silica particles, and no Pt(II) bulk precipitate had formed. The in vitro cytotoxicity in a human cancer cell line (HeLa) has been determined for one of the new platinum compounds adsorbed to mesoporous silica particles of different size, and compared with the corresponding compound in solution. The IC50 data are similar in all cases, suggesting that the release of the Pt(II) compound was relatively fast and possibly occurred before the particles reached the cells. Overall, the platinum drug is chemically stable on silica and retained its activity upon prolonged storage.

Keywords: Cytotoxicity, mesoporous silica, nanoparticles platinum compounds.

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Authors: Norma Rodrigues Gomes

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This paper presents initiatives of Knowledge Management (KM) applied to Forensic Sciences field, especially developed at the Forensic Science Institute of the Brazilian Federal Police. Successful projects, related to knowledge sharing, drugs analysis and environmental crimes, are reported in the KM perspective. The described results are related to: a) the importance of having an information repository, like a digital library, in such a multidisciplinary organization; b) the fight against drug dealing and environmental crimes, enabling the possibility to map the evolution of crimes, drug trafficking flows, and the advance of deforestation in Amazon rain forest. Perspectives of new KM projects under development and studies are also presented, tracing an evolution line of the KM view at the Forensic Science Institute.

Keywords: Business Intelligence, Digital Library, Forensic Science, Knowledge Management

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Authors: Mohammad Sadeghi, Behrouz Heidari, Korush Montazeri

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In this article, we synthesize a novel chitosan -based superabsorbent hydrogel via graft copolymerization of mixtures acrylic acid (AA) and N-vinyl pyrollidon onto chitosan backbones. The polymerization reaction was carried out in an aqueous medium and in the presence of ammonium persulfate (APS) as an initiator and N,N'-methylene bisacrylamide (MBA) as a crosslinker.The hydrogel structures were confirmed by FTIR spectroscopy. The swelling behavior of these absorbent polymers was also investigated in various salt solutions. Results indicated that the swelling capacity decreased with an increase in the ionic strength of the swelling medium. Furthermore, the swelling of superabsorbing hydrogels was examined in solutions with pH values ranging between 1.0 and 13.0. It showed a reversible pH-responsive behavior at pHs 2.0 and 8.0. This on-off switching behavior makes the synthesized hydrogels as an excellent candidate for controlled delivery of bioactive agents.

Keywords: chitosan, acrylic acid, N-vinyl pyrollidon, hydrogel, Ibuprofen's drug delivery

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Authors: Muhammad Waseem Ashraf, Shahzadi Tayyaba, Nitin Afzulpurkar, Asim Nisar, Adisorn Tuantranont, Erik L J Bohez

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In this paper, design, fabrication and coupled multifield analysis of hollow out-of-plane silicon microneedle array with piezoelectrically actuated microfluidic device for transdermal drug delivery (TDD) applications is presented. The fabrication process of silicon microneedle array is first done by series of combined isotropic and anisotropic etching processes using inductively coupled plasma (ICP) etching technology. Then coupled multifield analysis of MEMS based piezoelectrically actuated device with integrated 2×2 silicon microneedle array is presented. To predict the stress distribution and model fluid flow in coupled field analysis, finite element (FE) and computational fluid dynamic (CFD) analysis using ANSYS rather than analytical systems has been performed. Static analysis and transient CFD analysis were performed to predict the fluid flow through the microneedle array. The inlet pressure from 10 kPa to 150 kPa was considered for static CFD analysis. In the lumen region fluid flow rate 3.2946 μL/min is obtained at 150 V for 2×2 microneedle array. In the present study the authors have performed simulation of structural, piezoelectric and CFD analysis on three dimensional model of the piezoelectrically actuated mcirofluidic device integrated with 2×2 microneedle array.

Keywords: Coupled multifield, finite element analysis, hollow silicon microneedle, transdermal drug delivery.

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Authors: M. Saravanan

Abstract:

Antimicrobial resistant is becoming a major factor in virtually all hospital acquired infection may soon untreatable is a serious public health problem. These concerns have led to major research effort to discover alternative strategies for the treatment of bacterial infection. Nanobiotehnology is an upcoming and fast developing field with potential application for human welfare. An important area of nanotechnology for development of reliable and environmental friendly process for synthesis of nanoscale particles through biological systems In the present studies are reported on the use of fungal strain Aspergillus species for the extracellular synthesis of bionanoparticles from 1 mM silver nitrate (AgNO3) solution. The report would be focused on the synthesis of metallic bionanoparticles of silver using a reduction of aqueous Ag+ ion with the culture supernatants of Microorganisms. The bio-reduction of the Ag+ ions in the solution would be monitored in the aqueous component and the spectrum of the solution would measure through UV-visible spectrophotometer The bionanoscale particles were further characterized by Atomic Force Microscopy (AFM), Fourier Transform Infrared Spectroscopy (FTIR) and Thin layer chromatography. The synthesized bionanoscale particle showed a maximum absorption at 385 nm in the visible region. Atomic Force Microscopy investigation of silver bionanoparticles identified that they ranged in the size of 250 nm - 680 nm; the work analyzed the antimicrobial efficacy of the silver bionanoparticles against various multi drug resistant clinical isolates. The present Study would be emphasizing on the applicability to synthesize the metallic nanostructures and to understand the biochemical and molecular mechanism of nanoparticles formation by the cell filtrate in order to achieve better control over size and polydispersity of the nanoparticles. This would help to develop nanomedicine against various multi drug resistant human pathogens.

Keywords: Bionanoparticles, UV-visible spectroscopy, AtomicForce Microscopy, Extracellular synthesis, Multi drug resistant, antimicrobial activity, Nanomedicine

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Authors: Q. Wei, D. G. Hwang, Z. Mohy-Udin, D. H. Shin, J. H. Park, M. Y. Kang, J. H. Cho

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This study presents design of a carbon silicon electrode for iontophorsis treatment towards alopecia. The alopecia is a medical description means loss of hair from the body. For solving this problem, the drug need to be delivered into the scalp, therefore, the iontophoresis was chosen to use in this treatment. However, almost common electrodes of iontophoresis device are made with metal material, the electrodes could give patients hurt when they using it, and it is hard to avoid the hair for attaching the hair. For this reason, an electrode is made with silicon material to decrease the hurt from the electrodes, and the carbon material is mixed in it for increasing conductance. The several cones with stainless material on the electrode make the electrode is able to void hair to attach the affected part. According to the results of a vivo-experiment, the carbon silicon electrode showed a good performance and in treatment comfortably.

Keywords: Carbon silicon, drug delivery system, iontophoresis

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Authors: Wudhichai Assawinchaichote

Abstract:

This paper examines the problem of designing robust H controllers for for HIV/AIDS infection system with dual drug dosages described by a Takagi-Sugeno (S) fuzzy model. Based on a linear matrix inequality (LMI) approach, we develop an H controller which guarantees the L2-gain of the mapping from the exogenous input noise to the regulated output to be less than some prescribed value for the system. A sufficient condition of the controller for this system is given in term of Linear Matrix Inequalities (LMIs). The effectiveness of the proposed controller design methodology is finally demonstrated through simulation results. It has been shown that the anti-HIV vaccines are critically important in reducing the infected cells.

Keywords: H∞ Fuzzy control; Takagi-Sugeno (TS) fuzzy model; Linear Matrix Inequalities (LMIs); HIV/AIDS infection system

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Authors: Asad Ullah Madni, Mahmood Ahmad, Naveed Akhtar, Muhammad Usman

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A new and cost effective RP-HPLC method was developed and validated for simultaneous analysis of non steroidal anti inflammatory dugs Diclofenac sodium (DFS), Flurbiprofen (FLP) and an opioid analgesic Tramadol (TMD) in advanced drug delivery systems (Liposome and Microcapsules), marketed brands and human plasma. Isocratic system was employed for the flow of mobile phase consisting of 10 mM sodium dihydrogen phosphate buffer and acetonitrile in molar ratio of 67: 33 with adjusted pH of 3.2. The stationary phase was hypersil ODS column (C18, 250×4.6 mm i.d., 5 μm) with controlled temperature of 30 C°. DFS in liposomes, microcapsules and marketed drug products was determined in range of 99.76-99.84%. FLP and TMD in microcapsules and brands formulation were 99.78 - 99.94 % and 99.80 - 99.82 %, respectively. Single step liquid-liquid extraction procedure using combination of acetonitrile and trichloroacetic acid (TCA) as protein precipitating agent was employed. The detection limits (at S/N ratio 3) of quality control solutions and plasma samples were 10, 20, and 20 ng/ml for DFS, FLP and TMD, respectively. The Assay was acceptable in linear dynamic range. All other validation parameters were found in limits of FDA and ICH method validation guidelines. The proposed method is sensitive, accurate and precise and could be applicable for routine analysis in pharmaceutical industry as well as in human plasma samples for bioequivalence and pharmacokinetics studies.

Keywords: Diclofenac Sodium, Flurbiprofen, Tramadol, HPLCUV detection, Validation.

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Authors: Raniah Al-Shalabi, Omaima Al- Gohary, Samar Afify, Eram Eltahir

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Acetaminophen (Paracetamol) tablets are popular OTC products among patients as analgesics and antipyretics. Paracetamol is marketed by a lot of suppliers around the world. The aim of the present investigation was to compare between many types of paracetamol tablets obtained from different suppliers (six brands produced by different pharmaceutical companies in middle east countries, and Panadol® manufactured in Ireland), by different quality control tests according to USP pharmacopeia.Using Non official tests-hardness and friability; official tests- disintegration, dissolution, and drug content. Additionally, evaluate the influence of temperatures 4°C, 25°C and 40°C at 75% relative humidity on the stability of the same brands in their original packaging has been conducted for two months. The results revealed that all paracetamol tablet brands complied with the official USP specifications. In conclusion, paracetamol tablets preferred to be stored at 25°C. All the tested brands being biopharmaceutically and chemically equivalent.

Keywords: Non official tests-hardness and friability, official tests –disintegration, dissolution, and drug content.

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Authors: Vipin Saini, Sunil Kamboj, Suman Bala, A. Pandurangan

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The present invention relates to multiple-unit tablet dosage forms, which is composed of several subunits (multiparticulates/pellets). Each small multiparticulate further composed of many layers. Some layer contains drug substance; others are rate controlling polymer. The resulting multiple-unit tablet dosage forms of pantoprazole were satisfactory fabricated. Pelletization technique has some advantages over coated tablet formulation. In coated tablet the coating may be damaged and a pinhole possibly formed that would result in increased release of drug in stomach and may be deactivated in stomach juices. If the coat of some pellets may be damaged that would not affect the release properties of the multiple-unit tablet. Hence they are beneficial in this aspect. The results confirmed the successful preparation of stable and bioequivalent once daily controlled release multiple-unit tablets of pantoprazole.

Keywords: Controlled release, multiple unit tablets, pantoprazole, pelletization.

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Authors: Hind Bouami, Patrick Millot

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Medication dispensing system is a life-critical system whose failure may result in preventable adverse events leading to longer patient stays in hospitals or patient death. Automation has led to great improvements in life-critical systems as it increased safety, efficiency, and comfort. However, critical risks related to medical organization complexity and automated solutions integration can threaten drug dispensing security and performance. Knowledge about the system’s complexity aspects and human machine parameters to control for automated equipment’s security and performance will help operators to secure their automation process and to optimize their system’s reliability. In this context, this study aims to document the operator’s situation awareness about automation risks and parameters involved in automation security and performance. Our risk management approach has been deployed in the North Luxembourg hospital center’s pharmacy, which is equipped with automated drug dispensing systems since 2009. With more than 4 million euros of gains generated, North Luxembourg hospital center’s success story was enabled by the management commitment, pharmacy’s involvement in the implementation and improvement of the automation project, and the close collaboration between the pharmacy and Sinteco’s firm to implement the necessary innovation and organizational actions for automated solutions integration security and performance. An analysis of the actions implemented by the hospital and the parameters involved in automated equipment’s integration security and performance has been made. The parameters to control for automated equipment’s integration security and performance are human aspects (6.25%), technical aspects (50%), and human-machine interaction (43.75%). The implementation of an anthropocentric analysis system before automation would have prevented and optimized the control of risks related to automation.

Keywords: Automated drug delivery systems, hospitals, human-centered automated system, risk management.

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Authors: Anastasia Katsamaki, Nikolaos Bilalis, Vassilis Dedoussis

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This work proposes a set of actions to assist redesign procedure in existing products of Electric and Electronic Equipment (EEE). The aim is to improve their environmental behavior after their withdrawal in the End-of-Life (EOL) phase. In the beginning data collection takes place. Then follows selection and implementation of the optimal EOL Treatment Strategy (EOL_TS) and its results- evaluation concerning the environment. In parallel, product design characteristics that can be altered are selected based on their significance for the environment in the EOL stage. All results from the previous stages are combined and possible redesign actions are formulated for further examination and afterwards configuration in the design stage. The applied method to perform these tasks is Lean Thinking (LT). At the end, results concerning the application of the proposed method on a distribution transformer are presented.

Keywords: End-of-life treatment, Lean thinking, WEEE

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Authors: Anurag Gaur, Nidhi, Shashi Sharma

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Targeted drug delivery is a method of delivering medication to a patient in a manner that increases the concentration of the medication in some parts of the body relative to others. Targeted drug delivery seeks to concentrate the medication in the tissues of interest while reducing the relative concentration of the medication in the remaining tissues. This improves efficacy of the while reducing side effects. In the present work, we investigate the effect of magnetic field, flow rate and particle concentration on the capturing of magnetic particles transported in a stent implanted fluidic channel. Iron oxide magnetic nanoparticles (Fe3O4) nanoparticles were synthesized via co-precipitation method. The synthesized Fe3O4 nanoparticles were added in the de-ionized (DI) water to prepare the Fe3O4 magnetic particle suspended fluid. This fluid is transported in a cylindrical tube of diameter 8 mm with help of a peristaltic pump at different flow rate (25-40 ml/min). A ferromagnetic coil of SS 430 has been implanted inside the cylindrical tube to enhance the capturing of magnetic nanoparticles under magnetic field. The capturing of magnetic nanoparticles was observed at different magnetic magnetic field, flow rate and particle concentration. It is observed that capture efficiency increases from 47-67% at magnetic field 2-5kG, respectively at particle concentration 0.6mg/ml and at flow rate 30 ml/min. However, the capture efficiency decreases from 65 to 44% by increasing the flow rate from 25 to 40 ml/min, respectively. Furthermore, it is observed that capture efficiency increases from 51 to 67% by increasing the particle concentration from 0.3 to 0.6 mg/ml, respectively.

Keywords: Capture efficiency, Implant assisted-Magnetic drug targeting (IA-MDT), Magnetic nanoparticles, in vitro study.

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Authors: Jayashree Ramana

Abstract:

An alarming emergence of multidrug-resistant strains of the tuberculosis pathogen Mycobacterium tuberculosis and continuing high worldwide incidence of tuberculosis has invigorated the search for novel drug targets. The enzyme glutamate racemase (MurI) in bacteria catalyzes the stereoconversion of L-glutamate to D-glutamate which is a component of the peptidoglycan cell wall of the bacterium. The inhibitors targeted against MurI from several bacterial species have been patented and are advocated as promising antibacterial agents. However there are none available against MurI from Mycobacterium tuberculosis, due to the lack of its threedimensional structure. This work accomplished two major objectives. First, the tertiary structure of MtMurI was deduced computationally through homology modeling using the templates from bacterial homologues. It is speculated that like in other Gram-positive bacteria, MtMurI exists as a dimer and many of the protein interactions at the dimer interface are also conserved. Second, potent candidate inhibitors against MtMurI were identified through docking against already known inhibitors in other organisms.

Keywords: Glutamate racemase, homology modeling, docking, drug resistance.

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Authors: Simone Galati, Adriano Troia

Abstract:

Ultrasound (US) is widely used in medical field for a variety diagnostic techniques but, in recent years, it has also been creating great interest for therapeutic aims. Regarding drug delivery, the use of US as an activation source provides better spatial delivery confinement and limits the undesired side effects. However, at present there is no complete characterization at a fundamental level of the different signals produced by sono-activated nanocarriers. Therefore, the aim of this study is to obtain a metrological characterization of the cavitation phenomena induced by US through three parallel investigation approaches. US was focused into a channel of a customized phantom in which a solution with oxygen-loaded nanodroplets (OLNDs) was led to flow and the cavitation activity was monitored. Both quantitative and qualitative real-time analysis were performed giving information about the dynamics of bubble formation, oscillation and final implosion with respect to the working acoustic pressure and the type of nanodroplets, compared with pure water. From this analysis a possible interpretation of the observed results is proposed.

Keywords: Cavitation, Drug Delivery, Nanodroplets, Ultrasound.

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Authors: Marios M. Hadjiandreou, Raul Conejeros, Ian Wilson

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This study presents a mathematical modeling approach to the planning of HIV therapies on an individual basis. The model replicates clinical data from typical-progressors to AIDS for all stages of the disease with good agreement. Clinical data from rapid-progressors and long-term non-progressors is also matched by estimation of immune system parameters only. The ability of the model to reproduce these phenomena validates the formulation, a fact which is exploited in the investigation of effective therapies. The therapy investigation suggests that, unlike continuous therapy, structured treatment interruptions (STIs) are able to control the increase in both the drug-sensitive and drug-resistant virus population and, hence, prevent the ultimate progression from HIV to AIDS. The optimization results further suggest that even patients characterised by the same progression type can respond very differently to the same treatment and that the latter should be designed on a case-by-case basis. Such a methodology is presented here.

Keywords: AIDS, chemotherapy, mathematical modeling, optimal control, progression.

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Authors: W. Kaowumpai, D. Koolpiruck, K. Viravaidya

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Female breast cancer is the second in frequency after cervical cancer. Surgery is the most common treatment for breast cancer, followed by chemotherapy as a treatment of choice. Although effective, it causes serious side effects. Controlled-release drug delivery is an alternative method to improve the efficacy and safety of the treatment. It can release the dosage of drug between the minimum effect concentration (MEC) and minimum toxic concentration (MTC) within tumor tissue and reduce the damage of normal tissue and the side effect. Because an in vivo experiment of this system can be time-consuming and labor-intensive, a mathematical model is desired to study the effects of important parameters before the experiments are performed. Here, we describe a 3D mathematical model to predict the release of doxorubicin from pluronic gel to treat human breast cancer. This model can, ultimately, be used to effectively design the in vivo experiments.

Keywords: Breast Cancer, Doxorubicin, Controlled ReleaseSystem, Diffusion and Convection Equation.

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Authors: Amlan Kumar Das, Avinash Marwal, Vikram Pareek

Abstract:

Liposome plays an important role in medical and pharmaceutical science as e.g. nano scale drug carriers. Liposomes are vesicles of varying size consisting of a spherical lipid bilayer and an aqueous inner compartment. Magnet-driven liposome used for the targeted delivery of drugs to organs and tissues. These liposome preparations contain encapsulated drug components and finely dispersed magnetic particles. Liposomes are vesicles of varying size consisting of a spherical lipid bilayer and an aqueous inner compartment that are generated in vitro. These are useful in terms of biocompatibility, biodegradability, and low toxicity, and can control biodistribution by changing the size, lipid composition, and physical characteristics. Furthermore, liposomes can entrap both hydrophobic and hydrophilic drugs and are able to continuously release the entrapped substrate, thus being useful drug carriers. Magnetic liposomes (MLs) are phospholipid vesicles that encapsulate magneticor paramagnetic nanoparticles. They are applied as contrast agents for magnetic resonance imaging (MRI). The biological synthesis of nanoparticles using plant extracts plays an important role in the field of nanotechnology. Green-synthesized magnetite nanoparticles-protein hybrid has been produced by treating Iron (III) / Iron (II) chloride with the leaf extract of Datura inoxia. The phytochemicals present in the leaf extracts act as a reducing as well stabilizing agents preventing agglomeration, which include flavonoids, phenolic compounds, cardiac glycosides, proteins and sugars. The magnetite nanoparticles-protein hybrid has been trapped inside the aqueous core of the liposome prepared by reversed phase evaporation (REV) method using oleic and linoleic acid which has been shown to be driven under magnetic field confirming the formation magnetic liposome (ML). Chemical characterization of stealth magnetic liposome has been performed by breaking the liposome and release of magnetic nanoparticles. The presence iron has been confirmed by colour complex formation with KSCN and UV-Vis study using spectrophotometer Cary 60, Agilent. This magnet driven liposome using nanoparticles-protein hybrid can be a smart vesicles for the targeted drug delivery.

Keywords: Nanoparticles-Protein Hybrid, Magnetic Liposome.

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Authors: Y. Sangsen, K. Likhitwitayawuid, B. Sritularak, K. Wiwattanawongsa, R. Wiwattanapatapee

Abstract:

Novel solid lipid nanoparticles (SLNs) were developed to improve oral bioavailability of oxyresveratrol (OXY). The SLNs were prepared by a high speed homogenization technique, at an effective speed and time, using Compritol^® 888 ATO (5% w/w) as the solid lipid. The appropriate weight proportions (0.3% w/w) of OXY affected the physicochemical properties of blank SLNs. The effects of surfactant types on the properties of the formulations such as particle size and entrapment efficacy were also investigated. Conclusively, Tween 80 combined with soy lecithin was the most appropriate surfactant to stabilize OXY-loaded SLNs. The mean particle size of the optimized formulation was 134.40 ± 0.57 nm. In vitro drug release study, the selected S2 formulation showed a retarded release profile for OXY with no initial burst release compared to OXY suspension in the simulated gastrointestinal fluids. Therefore, these SLNs could provide a suitable system to develop for the oral OXY delivery.

Keywords: Solid lipid nanoparticles, Physicochemical properties, in vitro drug release, Oxyresveratrol.

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Authors: Pamita Awasthi, Kirna, Shilpa Dogra, Manu Vatsal, Ritu Barthwal

Abstract:

Doxorubicin, also known as Adriamycin, is an anthracycline class of drug used in cancer chemotherapy. It is used in the treatment of non-Hodgkin’s lymphoma, multiple myeloma, acute leukemia, breast cancer, lung cancer, endometrium cancer and ovary cancers. It functions via intercalating DNA and ultimately killing cancer cells. The major side effects of doxorubicin are hair loss, myelosuppression, nausea & vomiting, oesophagitis, diarrhea, heart damage and liver dysfunction. The minor modifications in the structure of compound exhibit large variation in the biological activity, has prompted us to carry out the synthesis of sulfonamide derivatives. Sulfonamide is an important feature with broad spectrum of biological activity such as antiviral, antifungal, diuretics, antiinflammatory, antibacterial and anticancer activities. Structure of the synthesized compound N-(1-methyl-2-oxo-2-N-methyl anilinoethyl) benzene sulfonamide confirmed by proton nuclear magnetic resonance (1H NMR),13C NMR, Mass and FTIR spectroscopic tools to assure the position of all protons and hence stereochemistry of the molecule. Further we have reported the binding potential of synthesized sulfonamide analogues in comparison to doxorubicin drug using Auto Dock 4.2 software. Computational binding energy (B.E.) and inhibitory constant (Ki) has been evaluated for the synthesized compound in comparison of doxorubicin against Poly (dA-dT).Poly (dA-dT) and Poly (dG-dC).Poly (dG-dC) sequences. The in vitro cytotoxic study against human breast cancer cell lines confirms the better anticancer activity of the synthesized compound over currently in use anticancer drug doxorubicin. The IC50 value of the synthesized compound is 7.12 μM whereas for doxorubicin is 7.2 μM.

Keywords: Anticancer, Auto Dock, Doxorubicin, Sulfonamide.

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Authors: Ponshano Kaselekela, Simooya O. Oscar, Lunshano Boyd

Abstract:

The Copperbelt University Health Services (CBUHS) was designated by the Zambia Medicines Regulatory Authority (ZAMRA), formally the Pharmaceutical Regulatory Authority (PRA) as a regional pharmacovigilance centre to carryout activities of drug safety monitoring in four provinces in Zambia. CBUHS’s mandate included stimulating the reporting of adverse drug reactions (ADRs), as well as collecting and collating ADR reports from health institutions in the four provinces. This report covers the researchers’ experiences from May 2008 to September, 2016. The main objectives are 1) to monitor ADRs in the Zambian population, 2) to disseminate information to all health professionals in the region advising that the CBU health was a centre for reporting ADRs in the region, 3) to monitor polypharmacy as well as the benefit-risk profile of medicines, 4) to generate independent, evidence based recommendations on the safety of medicines, 5) to support ZAMRA in formulating safety related regulatory decisions for medicines, and 6) to communicate findings with all key stakeholders. The methodology involved monthly visits, beginning in early May 2008 to September, 2016, by the CBUHS to health institutions in the programme areas. Activities included holding discussions with health workers, distribution of ADR forms and collection of ADRs reports. These reports, once collected, were documented and assessed at the CBUHS. A report was then prepared for ZAMRA on quarterly basis. At ZAMRA, serious ADRs were noted and recommendations made to the Ministry of Health of the Republic of Zambia. The results show that 2,600 ADRs reports were received at the pharmacovigilance regional centre. Most of the ADRs reports that received were due to antiretroviral drugs, as well as a few from anti-malarial drugs like Artemether/Lumefantrine – Coartem®. Three hundred and twelve ADRs were entered in the Uppsala Monitoring Centre WHO Vigiflow for further analysis. It was concluded that in general, 2008-16 were exciting years for the pharmacovigilance group at CBUHS. From a very tentative beginning, a lot of strides were made and contacts established with healthcare facilities in the region. The researchers were encouraged by the support received from the Copperbelt University management, the motivation provided by ZAMRA and most importantly the enthusiasm of health workers in all the health care facilities visited. As a centre for drug safety in Zambia, the results show it achieves its objectives for monitoring ADRs, Pharmacovigilance (drug safety monitoring), and activities of monitoring ADRs as well as preventing them. However, the centre faces critical challenges caused by erratic funding that prevents the smooth running of the programme.

Keywords: Assessments, evaluation, monitoring, pharmacovigilance.

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Authors: Pramod Jagtap, Kisan Jadhav, Neha Dand

Abstract:

Risperidone (RISP) is an antipsychotic agent and has low water solubility and nontargeted delivery results in numerous side effects. Hence, an attempt was made to develop SLNs hydrogel for intranasal delivery of RISP to achieve maximum bioavailability and reduction of side effects. RISP loaded SLNs composed of 1.65% (w/v) lipid mass were produced by high shear homogenization (HSH) coupled ultrasound (US) method using glycerylmonostearate (GMS) or Imwitor 900K (solid lipid). The particles were loaded with 0.2% (w/v) of the RISP & surface-tailored with a 2.02% (w/v) non-ionic surfactant Tween® 80. Optimization was done using 32 factorial design using Design Expert® software. The prepared SLNs dispersion incorporated into Polycarbophil AA1 hydrogel (0.5% w/v). The final gel formulation was evaluated for entrapment efficiency, particle size, rheological properties, X ray diffraction, in vitro diffusion, ex vivo permeation using sheep nasal mucosa and histopathological studies for nasocilliary toxicity. The entrapment efficiency of optimized SLNs was found to be 76 ± 2%, polydispersity index <0.3., particle size 278 ± 5 nm. This optimized batch was incorporated into hydrogel. The pH was found to be 6.4 ± 0.14. The rheological behaviour of hydrogel formulation revealed no thixotropic behaviour. In histopathology study, there was no nasocilliary toxicity observed in nasal mucosa after ex vivo permeation. X-ray diffraction data shows drug was in amorphous form. Ex vivo permeation study shows controlled release profile of drug.

Keywords: Ex vivo, particle size, risperidone, solid lipid nanoparticles.

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Authors: Hong Yi Huang, Wei Ti Kuo, Yi You Huang

Abstract:

Non-viral gene carriers composed of biodegradable polymers or lipids have been considered as a safer alternative for gene carriers over viral vectors. We have developed multi-functional nano-micelles for both drug and gene delivery application. Polyethyleneimine (PEI) was modified by grafting stearic acid (SA) and formulated to polymeric micelles (PEI-SA) with positive surface charge for gene and drug delivery. Our results showed that PEI-SA micelles provided high siRNA binding efficiency. In addition, siRNA delivered by PEI-SA carriers also demonstrated significantly high cellular uptake even in the presence of serum proteins. The post-transcriptional gene silencing efficiency was greatly improved by the polyplex formulated by 10k PEI-SA/siRNA. The amphiphilic structure of PEI-SA micelles provided advantages for multifunctional tasks; where the hydrophilic shell modified with cationic charges can electrostatically interact with DNA or siRNA, and the hydrophobic core can serve as payloads for hydrophobic drugs, making it a promising multifunctional vehicle for both genetic and chemotherapy application.

Keywords: polyethyleneimine, gene delivery, micelles, siRNA

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