High-throughput screening (HTS) is one of the newest techniques used in drug design and may be applied in biological and chemical sciences. This method, due to utilization of robots, detectors and software that regulate the whole process, enables a series of analyses of chemical compounds to be conducted in a short time and the affinity of biological structures which is often related to toxicity to be defined. Since 2008 we have implemented the automation of this technique and as a consequence, the possibility to examine 100,000 compounds per day. The HTS method is more frequently utilized in conjunction with analytical techniques such as NMR or coupled methods e.g., LC-MS/MS. Series of studies enable the establishment of the rate of affinity for targets or the level of toxicity. Moreover, researches are conducted concerning conjugation of nanoparticles with drugs and the determination of the toxicity of such structures. For these purposes there are frequently used cell lines. Due to the miniaturization of all systems, it is possible to examine the compound’s toxicity having only 1–3 mg of this compound. Determination of cytotoxicity in this way leads to a significant decrease in the expenditure and to a reduction in the length of the study.
Copper is one of the most interesting elements for various biomedical applications. Copper compounds show vast array of biological actions, including anti-inflammatory, anti-proliferative, biocidal and other. It also offers a selection of radioisotopes, suitable for nuclear imaging and radiotherapy. Quick progress in nanotechnology opened new possibilities for design of copper based drugs and medical materials. To date, copper has not found many uses in medicine, but number of ongoing research, as well as preclinical and clinical studies, will most likely lead to many novel applications of copper in the near future.
Radiolabeled peptides
are a relatively new, very specific radiotracer
group, which is still expanding. This group is very diverse in terms
of peptide size. It contains very small structures containing several
amino acids and whole antibodies. Moreover, radiolabeled peptides
are diverse in terms of the binding aim and therapeutic or diagnostic
applications. The majority of this class of radiotracers is utilized
in oncology, where the same structure can be used in therapy and diagnostic
imaging by varying the radionuclide. In this study, we collected new
reports of radiolabeled peptide applications in diagnosis and therapy
in oncology and other fields of medicine. Radiolabeled peptides are
also increasingly being used in rheumatology, cardiac imaging, or
neurology. The studies collected in this review concern new therapeutic
and diagnostic procedures in humans and new structures tested on animals.
We also performed an analysis of clinical trials, which concerns application
of radiolabeled peptides and antibodies that were reported in the
clinicaltrials.gov database between 2008 and 2018.
Randomized trials of thienopyridines in patients with vascular disease demonstrate that thienopyridines are effective in reducing vascular events when compared with placebo/control or aspirin, as well as when used in combination with aspirin in patients undergoing intracoronary stent implantation. The CURE trial is a large international study to determine if acute and long-term treatment with the combination of clopidogrel and aspirin is superior to aspirin alone in patients with acute coronary syndrome.
Nanotechnology, a separate field of knowledge since 1980s, involves utilization of nanomaterials not only in electronics and catalysis, but also in biomedical research including drug delivery, bioimaging, biomedical-diagnostics and tissue engineering. Multidisciplinary of this science has led to the development of different areas of technology and might contribute to innovations that will, as a final consequence, help humanity. Dendrimers are large and complex molecules that are characterized by well-defined nanoscale architecture, monodispersity and structural versatility. These highly interesting polymers consist of three elements: core, branches and peripheral groups. There is a wide variety of potential applications of dendritic polymers. One of the most promising is utilization of polyamidoamine (PAMAM) dendrimers as drug delivery devices. Among pharmaceuticals that have been connected with different types of dendrimers are nonsteroidal anti-inflammatory drugs (NSAIDs), anticancer drugs and other. Dendrimers application as drug carriers improves pharmacokinetic properties of drug particles, decreases drugs' side effects and, by possibility of surface modification with different ligands, enables to target specific tissues and tumor cells. Dendrimers might be also utilized as devices for delivery of genetic material and contrast agents for magnetic resonance imaging (MRI).
The interactions between dendrimers and different types of drugs are nowadays one of the most actively investigated areas of the pharmaceutical sciences. The interactions between dendrimers and drugs can be divided into: internal encapsulation, external electrostatic interaction, and covalent conjugation. In the present study, we investigated the potential of poly(amidoamine) (PAMAM) dendrimers for solubility of four iminodiacetic acid derivatives. We reported that PAMAM dendrimers contribute to significant solubility enhancement of iminodiacetic acid analogues. The nature of the dendrimer–drug complexes was investigated by 1H NMR and 2D-NOESY spectroscopy. The 1H NMR analysis proved that the water-soluble supramolecular structure of the complex was formed on the basis of ionic interactions between terminal amine groups of dendrimers and carboxyl groups of drug molecules, as well as internal encapsulation. The 2D-NOESY analysis revealed interactions between the primary amine groups of PAMAM dendrimers and the analogues of iminodiacetic acid. The results of solubility studies together with 1H NMR and 2D-NOESY experiments suggest that the interactions between PAMAM dendrimers of generation 1–4 and derivatives of iminodiacetic acid are based on electrostatic interactions and internal encapsulation.Electronic supplementary material The online version of this article (doi:10.1007/s10867-012-9277-5) contains supplementary material, which is available to authorized users.
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