Search results for: drugs bioavailability

Authors: Ntokozo Dambuza, Maryna Van De Venter, Trevor Koekemoer

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Oxidative stress contributes to the pathogenesis of many diseases and consequently antioxidant therapy has attracted much attention as a potential therapeutic strategy. Regardless of the quantities ingested, antioxidants need to reach the diseased tissues at concentrations sufficient to combat oxidative stress. Bioavailability is thus a defining criterion for the therapeutic efficacy of antioxidants. In addition, therapeutic antioxidants must possess biologically relevant characteristics which can target the specific molecular mechanisms responsible for disease related oxidative stress. While many chemical antioxidant assays are available to quantify antioxidant capacity, they relate poorly to the biological environment and provide no information as to the bioavailability. The present comparative study thus aims to characterise green and fermented rooibos extracts, well recognized for their exceptional antioxidant capacity, in terms of antioxidant bioavailability and efficacy in a disease relevant cellular setting. Chinese green tea antioxidant activity was also evaluated. Chemical antioxidant assays (FRAP, DPPH and ORAC) confirmed the potent antioxidant capacity of both green and fermented rooibos, with green rooibos possessing antioxidant activity superior to that of fermented rooibos and Chinese green tea. Bioavailability was assessed using the PAMPA assay and the results indicate that green and fermented rooibos have a permeation coefficient of 5.7 x 10-6 and 6.9 x 10-6 cm/s, respectively. Chinese green tea permeability coefficient was 8.5 x 10-6 cm/s. These values were comparable to those of rifampicin, which is known to have a high permeability across intestinal epithelium with a permeability coefficient of 5 x 10 -6 cm/s. To assess the antioxidant efficacy in a cellular context, U937 and red blood cells were pre-treated with rooibos and Chinese green tea extracts in the presence of a dye DCFH-DA and then exposed to oxidative stress. Green rooibos exhibited highest activity with an IC50 value of 29 μg/ml and 70 μg/ml, when U937 and red blood cells were exposed oxidative stress, respectively. Fermented rooibos and Chinese green tea had IC50 values of 61 μg/ml and 57 μg/ml for U937, respectively, and 221 μg/ml and 405 μg/ml for red blood cells, respectively. These results indicate that fermented and green rooibos extracts were able to permeate the U937 cells and red blood cell membrane and inhibited oxidation of DCFH-DA to a fluorescent DCF within the cells.

Keywords: rooibos, antioxidants, permeability, bioavailability

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Authors: Akshita Jindal, Renu Chadha, Maninder Karan

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Supramolecular chemistry has gained recent eminence in a flurry of research documents demonstrating the formation of new crystalline forms with potentially advantageous characteristics. Mesalamine (5-amino salicylic acid) belongs to anti-inflammatory class of drugs, is used to treat ulcerative colitis and Crohn’s disease. Unfortunately, mesalamine suffer from poor solubility and therefore very low bioavailability. This work is focused on preparation and characterization of cocrystal of mesalamine with nicotinamide (MNIC) a coformer of GRAS status. Cocrystallisation was achieved by solvent drop grinding in stoichiometric ratio of 1:1 using acetonitrile as solvent and was characterized by various techniques including DSC (Differential Scanning Calorimetry), PXRD (X-ray Powder Diffraction), and FTIR (Fourier Transform Infrared Spectrometer). The co-crystal depicted single endothermic transitions (254°C) which were different from the melting peaks of both drug (288°C) and coformer (128°C) indicating the formation of a new solid phase. Different XRPD patterns and FTIR spectrums for the co-crystals from those of individual components confirms the formation of new phase. Enhancement in apparent solubility study and intrinsic dissolution study showed effectiveness of this cocrystal. Further improvement in pharmacokinetic profile has also been observed with 2 folds increase in bioavailability. To conclude, our results show that application of nicotinamide as a coformer is a viable approach towards the preparation of cocrystals of potential drug molecule having limited solubility.

Keywords: cocrystal, mesalamine, nicotinamide, solvent drop grinding

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Authors: Sophio Kobauri, Tengiz Kantaria, Temur Kantaria, David Tugushi, Nina Kulikova, Ramaz Katsarava

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Nanosized environmentally responsive materials are of special interest for various applications, including targeted drug to a considerable potential for treatment of many human diseases. The important technological advantages of nanoparticles (NPs) usage as drug carriers (nanocontainers) are their high stability, high carrier capacity, feasibility of encapsulation of both hydrophilic or hydrophobic substances, as well as a high variety of possible administration routes, including oral application and inhalation. NPs can also be designed to allow controlled (sustained) drug release from the matrix. These properties of NPs enable improvement of drug bioavailability and might allow drug dosage decrease. The targeted and controlled administration of drugs using NPs might also help to overcome drug resistance, which is one of the major obstacles in the control of epidemics. Various degradable and non-degradable polymers of both natural and synthetic origin have been used for NPs construction. One of the most promising for the design of NPs are amino acid-based biodegradable polymers (AABBPs) which can clear from the body after the fulfillment of their function. The AABBPs are composed of naturally occurring and non-toxic building blocks such as α-amino acids, fatty diols and dicarboxylic acids. The particles designed from these polymers are expected to have an improved bioavailability along with a high biocompatibility. The present work deals with a systematic study of the preparation of NPs by cost-effective polymer deposition/solvent displacement method using AABBPs. The influence of the nature and concentration of surfactants, concentration of organic phase (polymer solution), and the ratio organic phase/inorganic (water) phase, as well as of some other factors on the size of the fabricated NPs have been studied. It was established that depending on the used conditions the NPs size could be tuned within 40-330 nm. As the next step of this research an evaluation of biocompatibility and bioavailability of the synthesized NPs has been performed, using two stable human cell culture lines – HeLa and A549. This part of study is still in progress now.

Keywords: amino acids, biodegradable polymers, nanoparticles (NPs), non-toxic building blocks

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Authors: Meena K. Yadav, Rupak Aryal, Michael D. Short, Ben Van Den Akker, Christopher P. Saint, Cobus Gerber

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Illicit drugs are considered as emerging contaminants of concern that have become an interesting issue for the scientific community from last few years due to their existence in the water environment. A number of the literature has revealed their occurrence in the environment. This is mainly due to the fact that some drugs are partially removed during wastewater treatment processes, and remaining being able to enter the environment and contaminate surface and groundwater and subsequently, drinking water. Therefore, this paper evaluates the occurrence of key illicit drugs in wastewater (influent and effluent) samples in 4 wastewater treatment plants across Adelaide, South Australia over a 1 year period. This paper also compares the efficiency of wastewater treatment plants adopting different technologies in the removal of selected illicit drugs, especially in the context of which technology has higher removal rates. The influent and effluent samples were analysed using Liquid Chromatography tandem Mass Spectrometry (LC-MS/MS). The levels of drugs detected were in the range of mg/L – ng/L in effluent samples; thus emphasising the influence on water quality of receiving water bodies and the significance of removal efficiency of WWTPs(Wastewater Treatment Plants). The results show that the drugs responded differently in the removal depending on the treatment processes used by the WWTPs.

Keywords: illicit drugs, removal efficiency, treatment technology, wastewater

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Authors: Tahra Elobeid, Emmerich Berghofer

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The aim of this study is to find innovative approaches for the production of iron rich foods using natural iron sources. The vehicle used for fortification was sorghum whereas the iron fortificant was white bean. Fortified sorghum cookies were produced from five different mixtures; iron content, iron bioavailability, cookie texture and acceptability were measured. Cookies were prepared from the three fortified flours; 90% sorghum + 10% white bean (S9WB1), 75% sorghum + 25% white bean (S3WB1), 50% sorghum + 50% white bean (S1WB1) and 100% sorghum and 100% white bean. The functional properties gave good results in all the formulations. Statistical analysis of the iron content in the five different cookies showed that there was significant difference at the 95% confidence level (ANOVA). The iron content in all the recipes including the 100% sorghum improved, the increase ranging from 112% in 100% sorghum cookies to 476% in 100% white bean cookies. This shows that the increase in the amount of white bean used for fortification leads to the improvement of the iron content of cookies. The bioavailability of iron ranged from 21.3% in 100% sorghum to 28.6% in 100% white bean cookies. In the 100% sorghum cookies the iron bioavailability increased with reference to raw sorghum due to the addition of eggs. Bioavailability of iron in raw sorghum is 16.2%, therefore the percentage increase ranged from 5.1% to 28.6%. The cookies prepared from 10% white bean (S9WB1) scored the lowest 3.7 in terms of acceptability. They were the least preferred due to their somewhat soft texture. The 30% white bean cookies (S3WB1) gave results comparable to the 50% (S1WB1) and 100% white bean cookies. Cookies prepared with high percentage of white bean (50% and 100% white bean) gave the best results. Therefore cookie formulations from sorghum and white bean are successful in improving the iron status of anaemic individuals.

Keywords: sorghum, white bean, iron content, bioavailable iron, cookies

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Authors: Obinna Emmanuel Nkomadu

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The sea attracts many criminal activities including drug trafficking. The illicit traffic in narcotic drugs and psychotropic substances by sea poses a serious threat to maritime security globally. The seizure of drugs, particularly, on the African continent is on the raise. In terms of Southern Africa, South Africa is a major transit point for Latin American drugs and South Africa is the largest market for illicit drugs entering the Southern African region. Nigeria and South Africa have taken a number of steps to address this scourge, but, despite those steps, drugs trafficking at sea continues. For that reason and to combat a number of other threats to maritime security around the continent, a substantial number of AU members in 2016 adopted the African Charter on Maritime Security and Safety and Development in Africa (“the Charter”). However, the Charter is yet to come into force due to the number of States required to accede or ratify the Charter. This paper set out the pre-existing international instruments on drugs, to ascertain the domestic laws of Nigeria and South Africa relating to drugs with the relevant provisions of the Lomé Charter in order to establish whether any legal steps are required to ensure that Nigeria and South Africa comply with its obligations under the Charter. Indeed, should Nigeria and South Africa decide to ratify it and should it come into force, both States must cooperate with other relevant States in establishing policies, as well as a regional and continental institutions, and ensure the implementation of such policies. The paper urged the States to urgently ratify the Charter as it is a step in the right direction in the prevention and repression of drugs trafficking on the African maritime domain.

Keywords: cooperation against drugs trafficking at sea, Lomé Charter, maritime security, Nigerian and South Africa legislation on drugs

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Authors: Behcet Al, Şener Cindoruk, Suat Zengin, Mehmet Murat Oktay, Mehmet Mustafa Sunar, Hatice Eroglu, Cuma Yildirim

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Objective: In present study we aimed to investigate the chronic drug use due to chronic diseases in patients admitted to emergency department. Materials-Methods: 144 patients who applied to emergency department (ED) of medicine school of Gaziantep University between June 2013 and September 2013 with chronic diseases and use chronic drugs were included. Information about drugs used by patients were recorded. Results: Of patients, half were male, half were female, and the mean age was 58 years. The first three common diseases were diabetes mellitus, hypertension and coronary artery diseases. Of patients, %79.2 knew their illness. Fifty patients began to use drug within three months, 36 patient began to use within the last one year. While 42 patients brought all of their drugs with themselves, 17 patients brought along a portion of drugs. While three patients stopped their medication completely, 125 patients received medication on a regular basis. Fifty-two patient described the drugs with names, 13 patients described with their colors, 3 patients described by grammes, 45 patients described with the size of the tablet and 13 patients could not describe the drugs. Ninety-two patients explained which kind of drugs were used for each diseases, 17 patient explained partly, and 35 patients had no idea. Hundred patients received medication by themselves, 44 patients medications were giving by their relatives and med carers. Of medications, 140 were written by doctors directly, three medication were given by pharmacist; and one patient bought the drug by himself. For 11 patients the drugs were not harmonious to their diseases. Fifty-one patients admitted to the ED two times within last week, and 73 admitted two times within last month. Conclusion: The majority of patients with chronic diseases and use chronic drugs know their diseases and use the drugs in order, but do not have enough information about their medication.

Keywords: chronic disease, drug use, emergency department, medication

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

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

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

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Authors: M. S. Deshpande, Snehal D. Bomble

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Tuberculosis (TB) is a deadly contagious disease that is caused by a bacterium called Mycobacterium tuberculosis. More than sixty years ago, the introduction of the first anti-TB drugs for the treatment of TB (streptomycin (STR), p-aminosalcylic acid (PAS), isoniazid (INH), and then later ethambutol (EMB) and rifampicin (RIF)) gave optimism to the medical community, and it was believed that the disease would be completely eradicated soon. Worldwide, the number of TB cases has continued to increase, but the incidence rate has decreased since 2003. Recently, highly drug-resistant forms of TB have emerged worldwide. The prolonged use of classical drugs developed a growing resistance and these drugs have gradually become less effective and incapable to meet the challenges, especially those of multi drug resistant (MDR)-TB, extensively drug resistant (XDR)-TB, and HIV-TB co-infections. There is an unmet medical need to discover newer synthetic molecules and new generation of potent drugs for the treatment of tuberculosis which will shorten the time of treatment, be potent and safe while effective facing resistant strains and non-replicative, latent forms, reduce adverse side effect and not interfere in the antiretroviral therapy. This paper attempts to bring out the review of anti-TB drugs, and presents a novel method of synthesizing new anti-tuberculosis drugs and potential compounds to overcome the bacterial resistance and combat the re-emergence of tuberculosis.

Keywords: tuberculosis, mycobacterium, multi-drug resistant (MDR)-TB, extensively drug resistant (XDR)-TB

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Authors: Ahmed. Abdel Bary, Omneya. Khowessah, Mojahed. al-jamrah

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Introduction: The major challenge with the design of oral dosage forms lies with their poor bioavailability. The most frequent causes of low oral bioavailability are attributed to poor solubility and low permeability. The aim of this study was to develop solid nanodispersed tablet formulation of Glimepiride for the enhancement of the solubility and bioavailability. Methodology: Solid nanodispersions of Glimepiride (GMP) were prepared using two different ratios of 2 different carriers, namely; PEG6000, pluronic F127, and by adopting two different techniques, namely; solvent evaporation technique and fusion technique. A full factorial design of 2 3 was adopted to investigate the influence of formulation variables on the prepared nanodispersion properties. The best chosen formula of nanodispersed powder was formulated into tablets by direct compression. The Differential Scanning Calorimetry (DSC) analysis and Fourier Transform Infra-Red (FTIR) analysis were conducted for the thermal behavior and surface structure characterization, respectively. The zeta potential and particle size analysis of the prepared glimepiride nanodispersions was determined. The prepared solid nanodispersions and solid nanodispersed tablets of GMP were evaluated in terms of pre-compression and post-compression parameters, respectively. Results: The DSC and FTIR studies revealed that there was no interaction between GMP and all the excipients used. Based on the resulted values of different pre-compression parameters, the prepared solid nanodispersions powder blends showed poor to excellent flow properties. The resulted values of the other evaluated pre-compression parameters of the prepared solid nanodispersion were within the limits of pharmacopoeia. The drug content of the prepared nanodispersions ranged from 89.6 ± 0.3 % to 99.9± 0.5% with particle size ranged from 111.5 nm to 492.3 nm and the resulted zeta potential (ζ ) values of the prepared GMP-solid nanodispersion formulae (F1-F8) ranged from -8.28±3.62 mV to -78±11.4 mV. The in-vitro dissolution studies of the prepared solid nanodispersed tablets of GMP concluded that GMP- pluronic F127 combinations (F8), exhibited the best extent of drug release, compared to other formulations, and to the marketed product. One way ANOVA for the percent of drug released from the prepared GMP-nanodispersion formulae (F1- F8) after 20 and 60 minutes showed significant differences between the percent of drug released from different GMP-nanodispersed tablet formulae (F1- F8), (P<0.05). Conclusion: Preparation of glimepiride as nanodispersed particles proven to be a promising tool for enhancing the poor solubility of glimepiride.

Keywords: glimepiride, solid Nanodispersion, nanodispersed tablets, poorly water soluble drugs

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Authors: Khushbu Priyadarshi, Chandramani Pathak

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Cancer cells can develop resistance to conventional therapies especially chemotherapeutic drugs. Resistance to chemotherapy is another challenge in cancer therapeutics. Therefore, it is important to address this issue. Gallic acid (GA) is a natural plant compound that exhibits various biological properties including anti-proliferative, anti-inflammatory, anti-oxidant and anti-bacterial. Despite of the wide spectrum biological properties GA has cytotoxic response and low bioavailability. To overcome this problem, GA was conjugated with the Polyamidoamine(PAMAM) dendrimer for improving the bioavailability and efficient delivery in drug-resistant HCT-116 Colon Cancer cells. Gallic acid was covalently linked to 4.0 G PAMAM dendrimer. PAMAM dendrimer is well established nanocarrier but has cytotoxicity due to presence of amphiphilic nature of amino group. In our study we have modified surface of PAMAM dendrimer with Gallic acid and examine their anti-proliferative effects in drug-resistant HCT-116 cells. Further, drug-resistant colon cancer cells were established and thereafter treated with different concentration of PAMAM-GA to examine their anti-proliferative potential. Our results show that PAMAM-GA conjugate induces apoptotic cell death in HCT-116 and drug-resistant cells observed by Annexin-PI staining. In addition, it also shows that multidrug-resistant drug transporter P-gp protein expression was downregulated with increasing the concentration of GA conjugate. After that we also observed the significant difference in Rh123 efflux and accumulation in drug sensitive and drug-resistant cancer cells. Thus, our study suggests that conjugation of anti-cancer agents with PAMAM could improve drug resistant property and cytotoxic response to treatment of cancer.

Keywords: drug resistance, gallic acid, PAMAM dendrimer, P-glycoprotein

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Authors: Stella O. Olubodun, George E. Eriyamremu

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The study assessed the effect of crude oil applied at rates, 0, 2, 5, and 10% on the fractional chemical forms and availability of some metals in soils from Usen, Edo State, with no known crude oil contamination and soil from a crude oil spill site in Ubeji, Delta State, Nigeria. Three methods were used to determine the bioavailability of metals in the soils: maize (Zea mays) plant, EDTA and BCR sequential extraction. The sequential extract acid soluble fraction of the BCR extraction (most labile fraction of the soils, normally associated with bioavailability) were compared with total metal concentration in maize seedlings as a means to compare the chemical and biological measures of bioavailability. Total Fe was higher in comparison to other metals for the crude oil contaminated soils. The metal concentrations were below the limits of 4.7% Fe, 190mg/kg Cu and 720mg/kg Zn intervention values and 36mg/kg Cu and 140mg/kg Zn target values for soils provided by the Department of Petroleum Resources (DPR) guidelines. The concentration of the metals in maize seedlings increased with increasing rates of crude oil contamination. Comparison of the metal concentrations in maize seedlings with EDTA extractable concentrations showed that EDTA extracted more metals than maize plant.

Keywords: availability, crude oil contamination, EDTA, maize, metals

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Authors: Aniya Everette

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In June of 1971, President Richard Nixon made his first public declaration regarding the “War on Drugs,” deeming it America’s number one public enemy. Since then, the drug war has been a divisive topic in the US. Black and brown children have been unfairly targeted and imprisoned at alarming rates as a result of this policy, which has had a negative effect on them. Black and Latino youth have faced significant obstacles that have impacted their educational opportunities, employment prospects, and general quality of life due to harsh mandatory sentences, aggressive policing tactics, and racial profiling.

Keywords: war, drugs, crime, racial profiling

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Authors: Bulent Topcuoglu

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Repeated amendments of organic matter and intensive use of fertilizers, metal-enriched chemicals and biocides may cause soil and environmental pollution in greenhouses. Specially, the impact of heavy metal pollution of soils on food metal content and underground water quality has become a public concern. Due to potential toxicity of heavy metals to human life and environment, determining the chemical form of heavy metals in greenhouse soils is an important approach of chemical characterization and can provide useful information on its mobility and bioavailability. A sequential extraction procedure was used to estimate the availability of heavy metals (Zn, Cd, Ni, Pb and Cr) in greenhouse soils of Antalya Aksu. Zn was predominantly associated with Fe-Mn oxide fraction, major portion of Cd associated with carbonate and organic matter fraction, a major portion of (>65 %) Ni and Cr were largely associated with Fe-Mn oxide and residual fractions and Pb was largely associated with organic matter and Fe-Mn oxide fractions. Results of the present study suggest that the mobility and bioavailability of metals probably increase in the following order: Cr < Pb < Ni < Cd < Zn. Among the elements studied, Zn and Cd appeared to be the most readily soluble and potentially bioavailable metals and these metals may carry a potential risk for metal transfer in food chain and contamination to ground water.

Keywords: metal speciation, metal mobility, greenhouse soils, biosystems engineering

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Authors: Mahiout Tassadit

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As part of the study of a compliance and quality aspect concerning one of the plant-based products: drugs for herbal teas sold in pharmacies, a survey targeting: the general population (100 people of different age groups) as well as dispensary pharmacists (40 pharmacists from rural or urban areas) of the wilaya of Tizi-Ouzou (central Algeria) was carried out followed by a macroscopic and microscopic analysis of 4 samples of the said drugs, the survey carried out using two questionnaires, the data of which were collected and then analyzed, made it possible to estimate the population's use of herbal products and medicinal plants, and the place occupied by herbal medicine in our pharmacies. The second part made it possible to control and evaluate the information present on the packaging of drugs for herbal teas; anomalies concerning the packaging, labeling and composition of these products were noted. As a result, it is more than necessary to establish regulations for this type of product; the community pharmacist again places himself as an essential element for the proper dispensation of these remedies.

Keywords: drugs, herbal teas, macroscopic analysis, microscopic analysis

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Authors: Zeeshan Hamid, Asher Ramish

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The purpose of this paper is to focus on security and safety issues facing by pharmaceutical industry globally when counterfeit drugs are in question. Hence, there is an intense need to secure and authenticate pharmaceutical products in the emerging counterfeit product market. This paper will elaborate the application of radio frequency identification (RFID) in pharmaceutical industry and to identify its key benefits for patient’s care. The benefits are: help to co-ordinate the stream of supplies, accuracy in chains of supplies, maintaining trustworthy information, to manage the operations in appropriate and timely manners and finally deliver the genuine drug to patient. It is discussed that how RFID supported supply chain information sharing (SCIS) helps to combat against counterfeit drugs. And a solution how to tag pharmaceutical products; since, some products prevent RFID implementation in this industry. In this paper, a proposed model for pharma industry distribution suggested to combat against the counterfeit drugs when they are in supply chain.

Keywords: supply chain, RFID, pharmaceutical industry, counterfeit drugs, patients care

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Authors: Priya Patel, Paresh Patel, Mihir Raval

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Silibinin, a flavanone as an antimicrotubular agent used in the treatment of cancer, was encapsulated in nanoparticles (NPs) of poly (lactide-co-glycolide) (PLGA) polymer using the spray-drying technique. The effects of various experimental parameters were optimized by box-behnken experimental design. Production yield, encapsulation efficiency and dissolution study along with characterization by scanning electron microscopy, DSC, FTIR followed by bioavailability study. Particle size and zeta potential were evaluated by using zetatrac particle size analyzer. Experimental design it was evaluated that inlet temperature and polymer concentration influence on the drug release. Feed flow rate impact on particle size. Results showed that spray drying technique yield 149 nm indicate nanosize range. The small size of the nanoparticle resulted in an enhanced cellular entry and greater bioavailability. Entrapment efficiency was found between 89.35% and 98.36%. Zeta potential shows good stability index of nanoparticle formulation. The in vitro release studies indicated the silibinin loaded PLGA nanoparticles provide controlled drug release over a period of 32 h. Pharmacokinetic studies demonstrated that after oral administration of silibinin-loaded PLGA nanoparticles to rats at a dose of 10 mg/kg, relative bioavailability was enhanced about 8.85-fold, compared to silibinin suspension as control hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of silibinin loaded PLGA nanoparticles. These results describe an effective strategy of silibinin loaded PLGA nanoparticles and might provide a promising approach against the cancer.

Keywords: silibinin, cancer, nanoparticles, PLGA, bioavailability

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Authors: I. Ahumada, L. Ascar, C. Pedraza, J. Montecino

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It has been found that the addition of biosolids to soil is beneficial to soil health, enriching soil with essential nutrient elements. Although this sludge has properties that allow for the improvement of the physical features and productivity of agricultural and forest soils and the recovery of degraded soils, they also contain trace elements, organic trace and pathogens that can cause damage to the environment. The application of these biosolids to land without the total reclamation and the treated wastewater can transfer these compounds into terrestrial and aquatic environments, giving rise to potential accumulation in plants. The general aim of this study was to evaluate the bioavailability of bisphenol A (BPA), and 17 α-ethynyl estradiol (EE2) in a soil-biosolid system using wheat (Triticum aestivum) plant assays and a predictive extraction method using a solution of hydroxypropyl-β-cyclodextrin (HPCD) to determine if it is a reliable surrogate for this bioassay. Two soils were obtained from the central region of Chile (Lo Prado and Chicauma). Biosolids were obtained from a regional wastewater treatment plant. The soils were amended with biosolids at 90 Mg ha-1. Soils treated with biosolids, spiked with 10 mgkg-1 of the EE2 and 15 mgkg-1 and 30 mgkg-1of BPA were also included. The BPA, and EE2 concentration were determined in biosolids, soils and plant samples through ultrasound assisted extraction, solid phase extraction (SPE) and gas chromatography coupled to mass spectrometry determination (GC/MS). The bioavailable fraction found of each one of soils cultivated with wheat plants was compared with results obtained through a cyclodextrin biosimulator method. The total concentration found in biosolid from a treatment plant was 0.150 ± 0.064 mgkg-1 and 12.8±2.9 mgkg-1 of EE2 and BPA respectively. BPA and EE2 bioavailability is affected by the organic matter content and the physical and chemical properties of the soil. The bioavailability response of both compounds in the two soils varied with the EE2 and BPA concentration. It was observed in the case of EE2, the bioavailability in wheat plant crops contained higher concentrations in the roots than in the shoots. The concentration of EE2 increased with increasing biosolids rate. On the other hand, for BPA, a higher concentration was found in the shoot than the roots of the plants. The predictive capability the HPCD extraction was assessed using a simple linear correlation test, for both compounds in wheat plants. The correlation coefficients for the EE2 obtained from the HPCD extraction with those obtained from the wheat plants were r= 0.99 and p-value ≤ 0.05. On the other hand, in the case of BPA a correlation was not found. Therefore, the methodology was validated with respect to wheat plants bioassays, only in the EE2 case. Acknowledgments: The authors thank FONDECYT 1150502.

Keywords: emerging compounds, bioavailability, biosolids, endocrine disruptors

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Authors: Somdutt Mujwar, Kamal Raj Pardasani

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Cholera pandemics are caused by facultative pathogenic Vibrio cholera bacteria persisting in the countries having warmer climatic conditions as well as the presence of large water bodies with huge amount of organic matter, it is responsible for the millions of deaths annually. Presently the available therapy for cholera is Oral Rehydration Therapy (ORT) with an antibiotic drug. Excessive utilization of life saving antibiotics drugs leads to the development of resistance by the infectious micro-organism against the antibiotic drugs resulting in loss of effectiveness of these drugs. Also, many side effects are also associated with the use of these antibiotic drugs. This riboswitch is explored as an alternative drug target for Vibrio cholera bacteria to overcome the problem of drug resistance as well as side effects associated with the antibiotics drugs. The bacterial riboswitch is virtually screened with 24407 legends to get possible drug candidates. The 10 ligands showing best binding with the riboswitch are selected to design a pharmacophore, which can be utilized to design lead molecules by using the phenomenon of bioisosterism.

Keywords: cholera, drug design, ligand, riboswitch, pharmacophore

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Authors: Wantana Amatariyakul, Chumnong Amatariyakul

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The research aims to examine the spread of drugs in higher education, especially amphetamine which is rapidly increasing in Thai society, its causes and effects, including the sociological perspective, in order to explain, prevent, control, and solve the problems. The students who participated in this research are regular students of Rajamangala University of Technology Isan, Khon Kaen Campus. The data were collected using questionnaires, group discussions, and in-depth interviews. The quantity data were analyzed using frequency, percentage, mean and standard deviation and using content analysis to analyzed quality data. The result of the study showed that the students had the results of examination on level of knowledge and understanding on drug abuse projected that the majority of sample group attained their knowledge on drug abuse respectively. Despite their uncertainty, the majority of samples presumed that amphetamine, marijuana and grathom (Mitragyna Speciosa Korth) would most likely be abused. The reason for first drug abuse is because they want to try and their friends convince them, as well as, they want to relax or solve the problems in life, respectively. The bad effects appearing to the drug addicts shows that their health deteriorates or worsens, as well as, they not only lose their money but also face with worse mental states. The reasons that respondents tried to avoid using drugs or refused drugs offered by friends were: not wanting to disappoint or upset their family members, fear of rejection by family members, afraid of being arrested by the police, afraid of losing their educational opportunity and ruining their future respectively. Students therefore defended themselves against drug addiction by refusing to try all drugs. Besides this, the knowledge about the danger and the harm of drugs persuaded them to stay away from drugs.

Keywords: drugs, higher education, drug addiction, spread of drugs

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Authors: Hardeep

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The aim of this research work to improve the solubility and bioavailability of Simvastatin using a self nanoemulsifying drug delivery system (SNEDDS). Self emulsifying property of various oils including essential oils was evaluated with suitable surfactants and co-surfactants. Validation of a method for accuracy, repeatability, Interday and intraday precision, ruggedness, and robustness were within acceptable limits. The liquid SNEDDS was prepared and optimized using a ternary phase diagram, thermodynamic, centrifugation and cloud point studies. The globule size of optimized formulations was less than 200 nm which could be an acceptable nanoemulsion size range. The mean droplet size, drug loading, PDI and zeta potential were found to be 141.0 nm, 92.22%, 0.23 and -10.13 mV and 153.5nm, 93.89 % ,0.41 and -11.7 mV and 164.26 nm, 95.26% , 0.41 and -10.66mV respectively.

Keywords: simvastatin, self nanoemulsifying drug delivery system, solubility, bioavailability

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Authors: Muhammed Saeed Rasheed

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Knowledge of the zinc and phytic acid (PA) concentrations of staple cereal crops are essential when evaluating the nutritional health of national and regional populations. In the present study, a total of 120 farmers’ fields in Iraqi Kurdistan were surveyed for zinc status in soil and wheat grain samples; wheat is the staple carbohydrate source in the region. Soils were analysed for total concentrations of phosphorus (PT) and zinc (ZnT), available P (POlsen) and Zn (ZnDTPA) and for pH. Average values (mg kg-1) ranged between 403-3740 (PT), 42.0-203 (ZnT), 2.13-28.1 (POlsen) and 0.14-5.23 (ZnDTPA); pH was in the range 7.46-8.67. The concentrations of Zn, PA/Zn molar ratio and estimated Zn bioavailability were also determined in wheat grain. The ranges of Zn and PA concentrations (mg kg⁻¹) were 12.3-63.2 and 5400 – 9300, respectively, giving a PA/Zn molar ratio of 15.7-30.6. A trivariate model was used to estimate intake of bioaccessible Zn, employing the following parameter values: (i) maximum Zn absorption = 0.09 (AMAX), (ii) equilibrium dissociation constant of zinc-receptor binding reaction = 0.680 (KP), and (iii) equilibrium dissociation constant of Zn-PA binding reaction = 0.033 (KR). In the model, total daily absorbed Zn (TAZ) (mg d⁻¹) as a function of total daily nutritional PA (mmole d⁻¹) and total daily nutritional Zn (mmole Zn d⁻¹) was estimated assuming an average wheat flour consumption of 300 g day⁻¹ in the region. Consideration of the PA and Zn intake suggest only 21.5±2.9% of grain Zn is bioavailable so that the effective Zn intake from wheat is only 1.84-2.63 mg d-1 for the local population. Overall results suggest available dietary Zn is below recommended levels (11 mg d⁻¹), partly due to low uptake by wheat but also due to the presence of large concentrations of PA in wheat grains. A crop breeding program combined with enhanced agronomic management methods is needed to enhance both Zn uptake and bioavailability in grains of cultivated wheat types.

Keywords: phosphorus, zinc, phytic acid, phytic acid to zinc molar ratio, zinc bioavailability

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Authors: Asma A. Ben Ahmed, Hajer M. Alborawy, Alaa A. Mashina, Pradeep K. Velautham, Abdulmonem Gobassa, Emhemmed Elgallal, Mohamed N. El Attug

Abstract:

Generic medicines are those where patent protection has expired, and which may be produced by manufacturers other than the innovator company. Use of generic medicines has been increasing in recent years, primarily as a cost saving measure in healthcare provision. Generic medicines are typically 20 – 90 % cheaper than originator equivalents. Physicians often continue to prescribe brand-name drugs to their patients even when less expensive pharmacologically equivalent generic drugs are available. Because generics are less expensive than their brand-name counterparts, the cost-savings to the patient is not the only factor that physicians consider when choosing between generic and brand-name drugs. Unfortunately Physicians in general and Libyan Physicians in particular tend to prescribe brand-name drugs, even without evidence of their therapeutic superiority, because neither they nor their insured patients bear these drugs’ increased cost with respect to generic substitutes. This study is to compare the quality of five different prednisolone tablets of the same strength from different companies under different trade names: Julphar, October pharma, Akums, Actavis, Pfizer compared them with pure prednisolone reference (BPCRS).

Keywords: quality control, pharmaceutical analysis, generic medicines, prednisolone

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Authors: Chi Wu, Dean Wu, Wen-Te Liu, Cheng-Yu Tsai, Shin-Mei Hsu, Yin-Tzu Lin, Ru-Yin Yang

Abstract:

Background: The results of previous studies compared the benefits and risks of receiving insomnia medication. However, the effects between hypnotic drugs used and enhancement of sleep quality were still unclear. Objective: The aim of this study is to establish a prediction model for hypnotic drugs' dosage used for insomnia subjects and associated the relationship between sleep stage ratio change and drug types. Methodologies: According to American Academy of Sleep Medicine (AASM) guideline, sleep stages were classified and transformed to hypnogram via the polysomnography (PSG) in a hospital in New Taipei City (Taiwan). The subjects with diagnosis for insomnia without receiving hypnotic drugs treatment were be set as the comparison group. Conversely, hypnotic drugs dosage within the past three months was obtained from the clinical registration for each subject. Furthermore, the collecting subjects were divided into two groups for training and testing. After training convolution neuron network (CNN) to predict types of hypnotics used and dosages are taken, the test group was used to evaluate the accuracy of classification. Results: We recruited 76 subjects in this study, who had been done PSG for transforming hypnogram from their sleep stages. The accuracy of dosages obtained from confusion matrix on the test group by CNN is 81.94%, and accuracy of hypnotic drug types used is 74.22%. Moreover, the subjects with high ratio of wake stage were correctly classified as requiring medical treatment. Conclusion: CNN with hypnogram was potentially used for adjusting the dosage of hypnotic drugs and providing subjects to pre-screening the types of hypnotic drugs taken.

Keywords: convolution neuron network, hypnotic drugs, insomnia, polysomnography

Procedia PDF Downloads 159

Authors: Nitin Jadhav, Pradeep R. Vavia

Abstract:

Poor water soluble drugs are difficult to promote for oral drug delivery as they demonstrate poor and variable bioavailability because of its poor solubility and dissolution in GIT fluid. Nowadays lipid based formulations especially self microemulsifying drug delivery system (SMEDDS) is found as the most effective technique. With all the impressive advantages, the need of high amount of surfactant (50% - 80%) is the major drawback of SMEDDS. High concentration of synthetic surfactant is known for irritation in GIT and also interference with the function of intestinal transporters causes changes in drug absorption. Surfactant may also reduce drug activity and subsequently bioavailability due to the enhanced entrapment of drug in micelles. In chronic treatment these issues are very conspicuous due to the long exposure. In addition the liquid self microemulsifying system also suffers from stability issues. Recently one novel approach of solid stabilized micro and nano emulsion (Pickering emulsion) has very admirable properties such as high stability, absence or very less concentration of surfactant and easily converts into the dry form. So here we are exploring pickering dry emulsion system for dissolution enhancement of anti-lipemic, extremely poorly water soluble drug (Fenofibrate). Oil moiety for emulsion preparation was selected mainly on the basis of higher solubility of drug. Captex 300 was showed higher solubility for fenofibrate, hence selected as oil for emulsion. With Silica (solid stabilizer); Span 20 was selected to improve the wetting property of it. Emulsion formed by Silica and Span20 as stabilizer at the ratio 2.5:1 (silica: span 20) was found very stable at the particle size 410 nm. The prepared emulsion was further preceded for spray drying and formed microcapsule evaluated for in-vitro dissolution study, in-vivo pharmacodynamic study and characterized for DSC, XRD, FTIR, SEM, optical microscopy etc. The in vitro study exhibits significant dissolution enhancement of formulation (85 % in 45 minutes) as compared to plain drug (14 % in 45 minutes). In-vivo study (Triton based hyperlipidaemia model) exhibits significant reduction in triglyceride and cholesterol with formulation as compared to plain drug indicating increasing in fenofibrate bioavailability. DSC and XRD study exhibit loss of crystallinity of drug in microcapsule form. FTIR study exhibit chemical stability of fenofibrate. SEM and optical microscopy study exhibit spherical structure of globule coated with solid particles.

Keywords: captex 300, fenofibrate, pickering dry emulsion, silica, span20, stability, surfactant

Procedia PDF Downloads 472

Authors: Sarwar Beg, Gajanand Sharma, O. P. Katare, Bhupinder Singh

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The current studies entail development of self-nano emulsifying drug delivery systems (SNEDDS) of rosuvastatin, employing rational QbD-based approach for enhancing its oral bioavailability. SNEDDS were prepared using the blend of lipidic and emulsifying excipients, i.e., Peceol, Tween 80, and Transcutol HP. The prepared formulations evaluated for in vitro drug release, ex vivo permeation, in situ perfusion studies and in vivo pharmacokinetic studies in rats, which demonstrated 3-4 fold improvement in biopharmaceutical performance of the developed formulations. Cytotoxicity studies using MTT assay and histopathological studies in intestinal cells revealed the lack of cytotoxicity and thereby safety and efficacy of the developed formulations.

Keywords: SNEDDS, bioavailability, solubility, Quality by Design (QbD)

Procedia PDF Downloads 481

Authors: J. Silva, P. Arezes, R. Schierl, N. Costa

Abstract:

In order to study environmental contamination by cytostatic drugs in Portugal hospitals, sampling campaigns were conducted in three hospitals in 2015 (112 samples). Platinum containing drugs and fluorouracil were chosen because both were administered in high amounts. The detection limit was 0.01 pg/cm² for platinum and 0.1 pg/cm² for fluorouracil. The results show that spills occur mainly on the patient`s chair, while the most referenced occurrence is due to an inadequately closed wrapper. Day hospitals facilities were detected as having the largest number of contaminated samples and with higher levels of contamination.

Keywords: cytostatic, contamination, hospital, procedures, handling

Procedia PDF Downloads 269

Authors: S. Boulenouar, M. Sefir, M. Benahmed

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All facilities need medication and other pharmaceuticals for their operation. Management and supply is therefore to provide the different services of the facility goods and services in required quantity and quality. The permanent availability of drugs in the facilities is very difficult because most face many difficulties at the inventory management and drug supplies. Therefore, it is necessary for each health facility to know the causes for the malfunction of its management system to cope with them. It is in this context that we have undertaken to conduct this study to know the causes which should be taken into consideration by the concerned authorities to carry out their mission, which is to provide quality health care for the population. In terms of financial resources, the budget for medicines represents a significant part of the budget of the pharmacy. Our study shows that the share of the hospital budget reserved for the drugs procurement represent on average 70% of the budget of the pharmacy. The results show a state of lack of anticancer drugs at Oran teaching hospital. The analysis of the management process allowed us to know the level that the problem of stock-outs of anti-cancer drugs is at. Suggestions were made to that effect to improve the availability for these products and to respond better to the needs of patients.

Keywords: anticancer drugs, health care facility, budget, hospital pharmacist, hospital service

Procedia PDF Downloads 411

Authors: Sara Assi, Berthe Hayar, Claudio Pisano, Nadine Darwiche, Walid Saad

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Nanomedicine, the application of nanotechnology to medicine, is an emerging discipline that has gained significant attention in recent years. Current breakthroughs in nanomedicine have paved the way to develop effective drug delivery systems that can be used to target cancer. The use of nanotechnology provides effective drug delivery, enhanced stability, bioavailability, and permeability, thereby minimizing drug dosage and toxicity. As such, the use of nanoparticle (NP) formulations in drug delivery has been applied in various cancer models and have shown to improve the ability of drugs to reach specific targeted sites in a controlled manner. Cancer is one of the major causes of death worldwide; in particular, colorectal cancer (CRC) is the third most common type of cancer diagnosed amongst men and women and the second leading cause of cancer related deaths, highlighting the need for novel therapies. Retinoids, consisting of natural and synthetic derivatives, are a class of chemical compounds that have shown promise in preclinical and clinical cancer settings. However, retinoids are limited by their toxicity and resistance to treatment. To overcome this resistance, various synthetic retinoids have been developed, including the adamantyl retinoid ST1926, which is a potent anti-cancer agent. However, due to its limited bioavailability, the development of ST1926 has been restricted in phase I clinical trials. We have previously investigated the preclinical efficacy of ST1926 in CRC models. ST1926 displayed potent inhibitory and apoptotic effects in CRC cell lines by inducing early DNA damage and apoptosis. ST1926 significantly reduced the tumor doubling time and tumor burden in a xenograft CRC model. Therefore, we developed ST1926-NPs and assessed their efficacy in CRC models. ST1926-NPs were produced using Flash NanoPrecipitation with the amphiphilic diblock copolymer polystyrene-b-ethylene oxide and cholesterol as a co-stabilizer. ST1926 was formulated into NPs with a drug to polymer mass ratio of 1:2, providing a stable formulation for one week. The contin ST1926-NP diameter was 100 nm, with a polydispersity index of 0.245. Using the MTT cell viability assay, ST1926-NP exhibited potent anti-growth activities as naked ST1926 in HCT116 cells, at pharmacologically achievable concentrations. Future studies will be performed to study the anti-tumor activities and mechanism of action of ST1926-NPs in a xenograft mouse model and to detect the compound and its glucuroconjugated form in the plasma of mice. Ultimately, our studies will support the use of ST1926-NP formulations in enhancing the stability and bioavailability of ST1926 in CRC.

Keywords: nanoparticles, drug delivery, colorectal cancer, retinoids

Procedia PDF Downloads 72

Authors: Mohana Babu Amberkar, Meena Kumari K, Ravi, Arjun, Christopher Rockson

Abstract:

The aim of this research is to evaluate the hepatoprotective activity of Terminalia paniculata (Tp) against ATT induced hepatic damage in rats.Three hepatotoxic ATT drugs Isoniazid + Rifampicin + Pyrazinamide, silymarin as standard hepatoprotective drug and 0.5% carboxymethylcellulose (CMC) as a control were used. Tp extract and silymarin were administered orally with ATT drugs for 90 days. Two doses 250 and 500 mg/kg of Tp extract, ATT drugs and silymarin were administered as suspensions with 0.5% CMC. ATT treated rats showed a significant increase in aspartate transaminase, alanine transaminase, alkaline phosphatase, lactate dehydrogenase, and lipid peroxides in the serum vs. control. Treatment of silymarin and Tp (250mg/kg) extract showed hepatoprotective activity against the hepatic damage by ATT. This was evident from significant reduction in serum liver enzymes levels, and also there was a significant increase in serum proteins, albumin and total liver tissue thiols as compared to the ATT treated groups. Tp was found to possess hepatoprotective property.

Keywords: antitubercular drugs, hepatoprotective, liver enzymes, Terminalia paniculata

Procedia PDF Downloads 405