Archive of Journal
Volume 70, Issue 5, May. 2014

Non-Systemic Delivery of Ocular Brimonidine to the Brain: Extending the Therapeutic Benefits of Brimonidine to the CNS

Volume 70, May 2014

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Abstract: Background. Despite recent advancements in neuroscience, and ever-emerging novelties in the field of drug delivery, the blood brain barrier is still considered a major obstacle that critically limits the delivery to the brain of hydrophilic drugs or those with modest or weak hydrophobic character. Brimonidine, a selective alpha-2 agonist, is a widely used ocular hypotensive agent with promising merits as neuroprotectant. Aim. To demonstrate the efficient delivery to the brain of Brimonidine following ocular administration and to elucidate the route of non-systemic drug flow along the eye-brain axis. Methods. Brimonidine was used as a probe to study the eye and brain pharmacokinetics following topical ocular administration of one droplet of the radio-labeled drug. Animals were sacrificed at different time points following the administration of single 0.2% 3H-Brimonidine droplet to the rabbit eye. Brain and eyes were dissected and selected brain and eye tissues, as well as systemic blood samples, were processed for detecting the concentration of radio-labeled Brimonidine. Fluorescent-labeled Dextran with molecular weight of 40 kDa was used as a probe to elucidate the route of the non-systemically mediated eye-to-brain drug flow following periocular administration. Results. Brimonidine accumulation in studied intracranial tissues was significant already at 5 minutes following single ocular administration while the detected Brimonidine levels in the systemic blood were very low at all time points. Evaluation by fluorescent microscopy showed that 40 kDa fluorescent-labeled Dextran that was administered to the periocular space didnt permeate the ocular barriers and was flowing through veins that drain the eye and orbital tissues towards the intracranial cavernous sinus. Tissue sections that included the eye and its major vessels showed extensive accumulation in veins but with no signal of the fluorescented probe inside the ciliary artery, which corresponds to non-significant flow of the probe through the systemic circulation. Conclusion. Brimonidine, a non-toxic agent to the eye with well appreciated therapeutic merits, can accumulate in intracranial tissues at significant concentrations already at few minutes after simple ocular administration with very low systemic accumulation. Our results suggest an efficient method for the extension of Brimonidine therapeutic merits to the brain while avoiding systemic side effects.

Author(s): ABDULRAZIK M, TAMILVANAN S, BENITA S

INFLUENCE OF PROCESS PARAMETERS ON STRUCTURE OF TIALN COATING PREPARED BY A SYSTEM WITH ROTARY ARC CATHODES

Volume 70, May 2014

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Abstract: It is advantageous to have a tool for a coating stoichiometry calculation to control coating deposition made from two different cathodes. Stoichiometry depends not only on arc currents ratio, but also on intensity and shape of magnetic field. This relation has been experimentally verified and is presented for TiAlN coating prepared by a new coating device Pi111. With the aid of this tool, it is possible to estimate coating parameters and to reach the desired Al/Ti ratio in a coating. With increasing content of Al in a coating, cubic structure shifts to hexagonal structure. This change proves itself not only by hardness decrease, but also by a change of coating growth rate. For detailed description of this effect, method of calculation of coating stoichiometry described above was used.

Author(s): Mojm?r J?lek, Ond?ej Zindulka

Sustainability of Annotated Resources in Linguistics

Volume 70, May 2014

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Abstract: In practically all scientifi c fi elds the task of ensuring the sustainability of resources, data collections, personal research journals, and databases is an increasingly important topic ? linguistics is no exception (Dipper et al., 2006, Trilsbeek and Wittenburg, 2006). We report on ongoing work in a project that is concerned with providing methods, tools, bestpractice guidelines, and solutions for sustainable linguistic resources. Our overall goal is to make sure that a large and very heterogeneous set of ca. 65 linguistic resources will be accessible, readable, and processible by interested parties such as, for example, other researchers than the ones who originally created said resources, in fi ve, ten, or even 20 years time. In other words, the agency that funded both our project as well as the projects who created the linguistic resources ? the German Research Foundation ? would like to avoid a situation in which they have to fund yet another project to (re)create a corpus for whose creation they already provided funding in the past, but the ?existing? version is no longer available or readable due to a proprietary fi le format, because it has been locked away in an academics hidden vault, or the person who developed the annotation format can no longer be asked questions concerning specifi c details of the custombuilt annotation format (Schmidt et al., 2006).

Author(s): Georg Rehm, Andreas Witt, Erhard Hinrichs, Marga Reis