Search results for "IPA"
showing 10 items of 5795 documents
Potential transbuccal delivery of l-DOPA methylester prodrug: stability in the environment of the oral cavity and ability to cross the mucosal tissue
2016
Levodopa (l-DOPA) is the most effective pharmacologic agent in Parkinson's disease and remains the "gold standard". Nevertheless, in long-term treatments, dyskinesias and motor complications can emerge. In this work, the combined use of l-DOPA methylester hydrochloride prodrug (LDME) with transbuccal drug delivery was supposed as a good alternative method to optimize the bioavailability of l-DOPA, to maintain constant plasma levels and to decrease the drug unwanted effects. The effects of environmental pH on buccal delivery of LDME were evaluated ex vivo. The increase of pH value from 5.8 to 6.2 implies an improvement of drug permeation. Since the pH increase causes the raising of hydrolyti…
Functionalized Poly(N-isopropylacrylamide)-Based Microgels in Tumor Targeting and Drug Delivery
2021
Over the past several decades, the development of engineered small particles as targeted and drug delivery systems (TDDS) has received great attention thanks to the possibility to overcome the limitations of classical cancer chemotherapy, including targeting incapability, nonspecific action and, consequently, systemic toxicity. Thus, this research aims at using a novel design of Poly(N-isopropylacrylamide) p(NIPAM)-based microgels to specifically target cancer cells and avoid the healthy ones, which is expected to decrease or eliminate the side effects of chemotherapeutic drugs. Smart NIPAM-based microgels were functionalized with acrylic acid and coupled to folic acid (FA), targeting the f…
Molecular interaction of artemisinin with translationally controlled tumor protein (TCTP) of Plasmodium falciparum
2012
Malaria causes millions of death cases per year. Since Plasmodium falciparum rapidly develops drug resistance, it is of high importance to investigate potential drug targets which may lead to novel rational therapy approaches. Here we report on the interaction of translationally controlled tumor protein of P. falciparum (PfTCTP) with the anti-malarial drug artemisinin. Furthermore, we investigated the crystal structure of PfTCTP. Using mass spectrometry, bioinformatic approaches and surface plasmon resonance spectroscopy, we identified novel binding sites of artemisinin which are in direct neighborhood to amino acids 19-46, 108-134 and 140-163. The regions covered by these residues are know…
5-Aminosalicylsäure-assoziierte Pankreatitis
2008
Acute pancreatitis with severe belt-like upper abdominal pain developed within 1-4 weeks of starting medication in three patients (29-year-old man with ulcerative colitis; 43-year-old woman and 22-year-old woman with Crohn's disease) treated, for the first time, with 5-aminosalicylic acid (mesalazine), 500 mg three times daily. Concentrations of lipase initially were 545, 1182 and 3000 U/l, and of amylase 243, 449 and 129 U/l, respectively. Symptoms receded within a few hours after the drug had been discontinued, enzyme levels returning to normal in the course of the next 2-3 weeks. On repeating the drug in two of the patients, in lower dosage, the pancreatitis recurred within a few days. T…
Development of a Multiparametric Cell-based Protocol to Screen and Classify the Hepatotoxicity Potential of Drugs
2012
Hepatotoxicity is a major reason for drug nonapprovals and withdrawals. The multiparametric analysis of xenobiotic toxicity at the single cells level using flow cytometry and cellular imaging-based approaches, such as high-content screening (HCS) technology, could play a key role in the detection of toxicity and the classification of compounds based on patterns of cellular injury. This study aimed to develop and validate a practical, reproducible, in vitro multiparametric cell-based protocol to assess those drugs that are potentially hepatotoxic to humans and to suggest their mechanisms of action. The assay was applied to HepG2 human cell line cultured in 96-well plates and exposed to 78 di…
Cytometric analysis for drug-induced steatosis in HepG2 cells
2009
Drugs are capable of inducing hepatic lipid accumulation. When fat accumulates, lipids are primarily stored as triglycerides which results in steatosis and provides substrates for lipid peroxidation. An in vitro multiparametric flow cytometry assay was performed in HepG2 cells by using fluorescent probes to analyze cell viability (propidium iodide, PI), lipid accumulation (BODIPY493/503), mitochondrial membrane potential (tetramethyl rhodamine methyl ester, TMRM) and reactive oxygen species generation (ROS) (2',7'-dihydrochlorofluorescein diacetate, DHCF-DA) as functional markers. All the measurements were restricted to live cells by gating the cells that excluded PI or those that exhibited…
TABLE 3. QUESTIONS DE DURABILITÉ CULTURELLE ET ENVIRONNEMENTALE
2016
Il contributo gli esiti di un forum dei soggetti territoriali, sottolineando come il tema della partecipazione sia un prerequisito per la sostenibilità delle scelte progettuali. L'article porte sur les résultats d'un forum régional du sujet et met l'accent sur la participation comme une exigence pour la durabilité des choix de conception. Le Forum, organisé dans le cadre du programme DO.RE.MI.HE., a représenté l’une des rares occasions de voir plusieurs organismes territoriaux et associations, qui travaillent à divers niveaux sur le territoire, réunis autour d’une même table en vue d’imaginer un futur pour la ville et le territoire au départ du site UNESCO.
Stability Analysis of Routing Strategies for the Maximum Lifetime Problem in One-Dimensional Ad-Hoc Wireless Networks
2017
In the paper we discuss solutions of the maximum network lifetime problem in one-dimensional, regular ad-hoc wireless networks. For the problem, nodes of the network generate given amount of data and send it possibly via other nodes to the data collector. To extend the network lifetime the data should be transmitted in such a way, that the energy utilized by the most overloaded node is minimized. We assume, that the nodes use the point-to-point data transmission scheme and the cost of transmission of one unit of data is arbitrary superadditive function of a distance between transmitter and receiver. We show that for the one-dimensional network in which the nodes are evenly distributed on th…
A Branch-and-Cut method for the Capacitated Location-Routing Problem
2011
International audience; Recent researches in the design of logistic networks have shown that the overall distribution cost may be excessive if routing decisions are ignored when locating depots. The Location-Routing Problem (LRP) overcomes this drawback by simultaneously tackling location and routing decisions. The aim of this paper is to propose an exact approach based on a Branch-and-Cut algorithm for solving the LRP with capacity constraints on depots and vehicles. The proposed method is based on a zero-one linear model strengthened by new families of valid inequalities. The computational evaluation on three sets of instances (34 instances in total), with 5–10 potential depots and 20–88 …
TBRA: A scalable routing algorithm in highly mobile large scale pure ad hoc wireless mesh networks
2009
In highly mobile pure ad-hoc wireless mesh networks, fast rerouting within low routing discovery delay is a mandatory requirement for routing algorithm to support interactive applications such as VoIP. Also, the communication overhead should be thwarted when networks grow to a large scale. We propose a Tree-Based Routing Algorithm - TBRA to facilitate such two goals. On one hand, TBRA has very low routing discovery delay due to its proactive property. On the other hand, TBRA performs more efficiently than other proactive protocols with respect to low communication overhead, which thanks to its short routing packet length, less numbers and smaller routing table size. Our modeling analysis an…