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Liposomal drug delivery, a novel approach: PLARosomes.

100%
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2000
|
vol. 47
|
issue 3
639-649
EN
Almost from the time of their rediscovery in the 60's and the demonstration of their entrapment potential, liposomal vesicles have drawn attention of researchers as potential carriers of various bioactive molecules that could be used for therapeutic applications in humans and animals. Several commercial liposome-based drugs have already been discovered, registered and introduced with great success on the pharmaceutical market. However, further studies, focusing on the elaboration of more efficient and stable amphiphile-based vesicular (or non-viral) drug carriers are still under investigation. In this review we present the achievements of our group in this field. We have discovered that natural amphiphilic dihydroxyphenols and their semisynthetic derivatives are promising additives to liposomal lipid compositions. The presence of these compounds in lipid composition enhances liposomal drug encapsulation, reduces the amount of the lipid carrier necessary for efficient entrapment of anthracycline drugs by a factor of two, stabilizes liposomal formulation of the drug (both in suspension and in a lyophilized powder), does not influence liposomal fate in the blood circulation system and benefits from other biological activities of their resorcinolic lipid modifiers.
EN
Fungi, in comparison with other pathogenic factors, have high pathogenecity. The number of fungal species which are able to infect people is over 500. The upper respiratory tract and ear have permanent contact with external environment which makes their ontocenoses open to continuous exchange of microorganisms of which they consist. In etiology of inflammatory processes 21 species which belonging to 3 genera (Zygomycota, Asomycota, Basidiomycota) of fungi play important role. Administration of antifungal drugs can be: prophylactic, empiric preemptive and therapeutic. Physicians may prescribe antibiotics (mainly poliens: amphotericin B, natamycin and nystatin) and chemiotherapeutics (mainly azoles and fluorpirymidins, pigments, chlorhexidine and chlorquinaldol). In ENT practice topical and systemic drugs can be administrated. Topical lozenges include amphotericin B, clotrimazole, chlorhexidine or chlorquinaldol and oral gels: nystatin and miconazole. Some of drugs are in the form of suspension/solution, which can be used for inhalation, into the sinus, for swabbing or for lavage: amphotericin B, natamycin, nystatin, clotrimazol, flucytosine, miconazole, fluconazole, vorykonazole, caspofungin. It should be underlined that only a few of dugs can be absorbed from the digestive tract: flucytosine, fluconazole, itraconazole, ketoconazole, miconazole, vorykonazole.
EN
ABSTRACT Introduction. Considering that small number of drugs are completely safe for use during pregnancy, right choice and adequate risk assessment is extremely important. Objective. The aim of this study was to analyze factors associated with estimate of high teratogenic risk (as judged by clinical pharmacologist) in pregnant females who were prescribed anti-infective drugs or mild analgesics. Methods. A cross-sectional study included 284 pregnant women who came for an advice about teratogenic risk to clinical pharmacologist in Clinical Centre Kragujevac, Serbia during the period from 1997 to 2012. All of included pregnant women were prescribed mild analgesics and/or anti-infective drugs during the first 3 months of pregnancy. The data were collected from patient files and by phone interviews. Results. Clinical pharmacologists estimated the risk of teratogenicity as “high” in pregnant females who were using tetracyclines or propionic acid derivatives. Disorders of development reported by mothers during phone interviews were associated with cephalosporin use during first 3 months of pregnancy, while miscarriages or abortions happened more often in women who used a tetracycline. Conclusions. Estimate of risk from congenital anomalies after use of drugs during pregnancy, which make clinical pharmacologists as part of their routine healthcare services, depends on amount of published data about previous experiences with specific drugs during the first 3 months of pregnancy. Key Words: pregnancy; drugs; risk of teratogenicity; risk estimate
4
88%
EN
Concern for the natural environment increasingly devotes more attention to growing potential hazards resulting from the release of various substances. Currently, one of the main problems associated with environmental pollution is the derivation of organic compounds from wastewater. Substances derived from sewage leaks into the environment in the form of a multicomponent mixtures often enhances the toxic effects caused by these compounds. While analyzing the reports in the literature of the last two decades it can be seen that substantial efforts are devoted to the determination of selected trace contaminants present in wastewater. Among the most marked there are endocrine disrupting compounds, residues of pharmaceuticals and personal care products, plastics and sunscreens. Recently, a new group of compounds joined the aforementioned contaminants, namely drugs, whose legality and availability is increasing every year. Exposure to these type of compounds, named in the literature as emerging contaminants (ECs), involves, among others, such effects as hormonal imbalance, reduction of the survivability of aquatic organisms and reproductive problems. This paper provides a review of the types of emerging organic groundwater contaminants (EGCs) which are beginning to be found in the natural environment in many countries all around the world.
6
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Content available

Scoring ligand efficiency

75%
EN
Ligand efficiency (LE) is a molecular descriptor that probes the ratio of potency vs. heavy atom count (HAC). As an estimator of drug candidates, LE emphasizes a low heavy atom count more than potency. The objective was to design a novel transform where potency and the HAC would be balanced more evenly. A series of novel descriptors SCORE was defined to evaluate the co-influence of potency and the HAC. In particular, the product ligand efficiency (PLE) was designed and tested using the data of the ChEMBL, PubChem as well as the selected series of drugs and drug-fragments.
EN
Nanoscale magnetic materials may have several potential applications in the biomedical area. An example thereof are superparamagnetic iron oxide nanoparticles, which, due to large own surface and ability to interact with various tissues, are used to detect and analyze biological molecules, in targeted drug delivery, for contrast enhancement in magnetic resonance imaging studies and, last but not least, in therapeutic hyperthermia. When used for medical purposes, magnetic nanoparticles often require coating with a biocompatible polymer, preventing its detection by the immune system, encapsulation by plasma proteins and excretion, while at the same time facilitating binding with organic complexes, which subsequently may accumulate in definite pathological foci. Widespread use of magnetic nanoparticles is associated with heat generation. When placed within neoplastic tissue and exposed to alternating external magnetic field, magnetic nanoparticles generate a local heating effect. Local elevation of tissue temperature has a potent cytostatic effect mediated by denaturation of proteins and destruction of intracellular structures, leading to reduction of tumor mass. Temperature obtained within the tumor depends on properties of magnetic nanoparticles used and parameters of external magnetic field applied, i.e. amplitude and frequency of field oscillations. This physical phenomenon results in direct destruction of tumor cells. Furthermore, local elevation of body temperature contributes to enhanced effectiveness of chemo- and radiotherapy. The paper is a review of current applications of superparamagnetic metal nanoparticles in oncology.
PL
Nanomateriały magnetyczne mogą znaleźć szerokie zastosowanie zarówno w naukach biologicznych, jak i medycznych. Przykładem takich materiałów są superparamagnetyczne nanocząstki żelaza, które z uwagi na dużą powierzchnię właściwą i możliwość oddziaływania z różnymi tkankami są stosowane między innymi w detekcji i analizie biocząsteczek, docelowym transporcie leków, poprawie kontrastu przy badaniach metodą rezonansu magnetycznego i hipertermii. Do zastosowań medycznych nanocząstki magnetyczne wymagają często pokrycia biokompatybilnym polimerem, który z jednej strony ekranuje cząstkę przed układem immunologicznym, uniemożliwiając otoczenie jej białkami plazmy i usunięcie z organizmu, z drugiej zaś ułatwia wiązanie innych kompleksów organicznych, które mogą być transportowane do określonych obszarów patologicznych. Szerokie zastosowanie medyczne magnetycznych nanocząstek jest związane z efektem generowania ciepła. Jeżeli nanocząstki magnetyczne zostaną umiejscowione w zmienionym nowotworowo obszarze ciała, to w obecności zmiennego zewnętrznego pola magnetycznego można uzyskać efekt cieplny. Uśmiercając komórki nowotworowe i niszcząc białka oraz struktury wewnątrzkomórkowe wygenerowaną w tych miejscach wysoką temperaturą, możemy powodować zmniejszenie się guza. Wysokość uzyskanego przez nas poziomu temperatury w guzie nowotworowym zależy od właściwości użytych magnetycznych nanocząstek oraz od parametrów przyłożonego zmiennego pola magnetycznego (amplituda, częstotliwość). To zjawisko fizyczne wykorzystuje się do bezpośredniego niszczenia komórek nowotworowych. Dodatkowo wzrost temperatury obszaru ciała chorego zwiększa efektywność zastosowanej chemio- lub radioterapii. W pracy zaprezentowano przegląd zastosowania superparamagnetycznych cząsteczek metali w terapii nowotworowej.
EN
Introduction. Adolescents’ self-esteem is an issue that deserves our attention. Puberty is a stage of many changes. It is a time of constant development, searching for one's place among peers. Adolescents feel a constant need to experiment, therefore they are exposed to addiction to psychotropic substances. Educational and preventive activities carried out by guardians and nurses play a significant role in preventing addiction and life-threatening situations. Aim. The goal of the study was to investigate the need of belonging to a peer group and its impact on the initiation of the use of legal highs and smoking marijuana. Material and methods. The research method used was the diagnostic survey method, the research technique was to conduct a survey, and the research tools were the KIDSCREEN questionnaires, PUN Test, PUM and the questionnaires of own authorship. The survey was carried out among 104 people aged from 16 to 19 years old. Results. According to the analysis of research results, legal highs are becoming less and less popular, but marijuana’s number of recipients is increasing, which is influenced by the need of belonging to a peer group. As many as 23% of teenagers believe that smoking marijuana has improved their relationship with friends, most of whose also smokes. Conclusions. Relationship with peers influences the decision to smoke marijuana, nonetheless it does not affect people taking legal highs. People who decide to initiate drugs intake are also not influenced by self-confidence, nor relationships with peers and parents.
PL
Wstęp. Poczucie własnej wartości u nastolatka jest zagadnieniem zasługującym na naszą uwagę. Dojrzewanie jest etapem pełnym zmian. Jest to czas ciągłego rozwoju, poszukiwania swojego miejsca w grupie rówieśniczej. Młodzież czuje ciągłą potrzebę eksperymentowania, dlatego jest narażona na uzależnienia od środków psychotropowych. Działania edukacyjne i profilaktyczne prowadzone przez opiekunów i pielęgniarki odgrywają znaczącą rolę w zapobieganiu powstawania uzależnień i stanów zagrożenia życia. Cel. Celem pracy było zbadanie wpływu potrzeby przynależności do grupy rówieśniczej na rozpoczęcie zażywania dopalaczy i palenia marihuany. Materiał i metody. Użytą metodą badawczą była metoda sondażu diagnostycznego, techniką badawczą było przeprowadzenie ankiety, a narzędziami badawczymi był Kwestionariusz KIDSCREEN, Test PUN, PUM oraz kwestionariusz ankiety własnego autorstwa.  Badanie przeprowadzono wśród 104 osób od 16 do 19 roku życia. Wyniki. Według analizy wyników badań dopalacze stają się mniej popularne, a marihuana trafia do coraz liczniejszej grupy odbiorców na co wpływ ma potrzeba przynależności do grupy rówieśniczej. Aż 23% nastolatków uważa, że zapalenie marihuany poprawiło ich kontakt z koleżankami i kolegami, a większość z nich również pali. Wnioski. Relacja z rówieśnikami wpływa na decyzję o zapaleniu marihuany, nie ma wpływu na osoby zażywające dopalacze. Na osoby decydujące się na inicjację narkotykową nie wpływa również pewność siebie, relacja z rówieśnikami oraz rodzicami.
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