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Amorphization serves as a strategy for the improvement of poor dissolution characteristics of many drug compounds. However, in many formulations the content of polymeric stabilizer is high, which is undesirable from the perspective of future applications. Thus, studying the compositiondependent stability of amorphous solid dispersions seems to be demanded. In this paper, we describe the amorphization of ezetimibe, a lipid-lowering drug, in the spray drying process and investigate the effect of polyvinylpyrrolidone-co-poly(vinyl acetate) (PVP/VA) content on the physical stability and dissolution characteristics of the drug. Fully amorphous systems were obtained when the concentration of the polymer in solid dispersion was as low as 20%. The amorphization led to the dissolution enhancement by even 70%, with a noticeable sudden increase at around 40% of PVP/VA content and very small variations for systems having 66–90% PVP/VA. It was also correlated to wettability characteristics of solid dispersions, which may suggest that in the vicinity of 40% of the polymer content, the behavior of the system becomes independent of the PVP/VA content., Polish National Science Centre, grant number 2015/16/W/NZ7/00404

Nonsteroidal anti-inflammatory drugs (NSAIDs) constitute a heterogeneous group of compounds that exhibit analgesic, anti-inflammatory and antipyretic activity. However, the GI damage produced by NSAIDs has been widely studied. Thus, the aim of the present study was the development of mesoporous silica nanoparticles in order to increase the capacity of drug transport, emphasizing those with low solubility such as NSAIDs. The morphology and structure characteristics of the synthesized nanoparticles were studied by transmission electron microscopy (TEM), besides, its particle size, surface charge, specific area and cell viability will be determined. The analytical application of mesoporous silica nanoparticles as ibuprofen carrier was also evaluated by measuring their drug loading characteristics and release behavior. The results showed that the synthesized NPs had efficient physicochemical characteristics, high EE%, low toxicity, and controlled ibuprofen release., CTS-205

The formation of solid dispersions with the amorphous drug dispersed in the polymeric matrix improves the dissolution characteristics of poorly soluble drugs. Although they provide an improved absorption after oral administration, the recrystallization, which can occur upon absorption of moisture or during solidification and other formulation stages, serves as a major challenge. This work aims at understanding the amorphization-recrystallization changes of bicalutamide. Amorphous solid dispersions with poly(vinylpyrrolidone-co-vinyl acetate) (PVP/VA) were obtained by either ball milling or spray drying. The applied processes led to drug amorphization as confirmed using X-ray diffraction and differential scanning calorimetry. Due to a high propensity towards mechanical activation, the changes of the crystal structure of physical blends of active pharmaceutical ingredient (API) and polymer upon pressure were also examined. The compression led to drug amorphization or transition from form I to form II polymorph, depending on the composition and applied force. The formation of hydrogen bonds confirmed using infrared spectroscopy and high miscibility of drug and polymer determined using non-isothermal dielectric measurements contributed to the high stability of amorphous solid dispersions. They exhibited improved wettability and dissolution enhanced by 2.5- to 11-fold in comparison with the crystalline drug. The drug remained amorphous upon compression when the content of PVP/VA in solid dispersions exceeded 20% or 33%, in the case of spray-dried and milled systems, respectively., Polish National Science Centre 2015/16/W/NZ7/00404

Therapies against stroke can restore the blood supply but cannot prevent the ischemic damage nor stimulate the recovery of the infarcted zone. The neuroglobin protein plays an important role in the neuro-regeneration process after stroke, however, the method for its effective systemic application has not been identified yet, as neuroglobin is unable to pass through the blood-brain barrier. Previously, we developed different types of sodium hyaluronate nanoparticles, which successfully cross the blood-brain barrier after stroke. In this work, these nanoparticles have been used to carry neuroglobin through the bloodstream to the nerve cells in rats submitted to stroke. We have biosynthesized rat-recombinant neuroglobin and determined the formulation of sodium hyaluronate nanoparticles loaded with neuroglobin, as well as its size and &zeta, potential, encapsulation efficiently, in vitro release, and its kinetic of liberation. The results show that the formulation achieved is highly compatible with pharmaceutical use and may act as a delivery system to transport neuroglobin within the blood. We have found that this formulation injected intravenously immediately after stroke reached the damaged cerebral parenchyma at early stages (2 h). Neuroglobin colocalizes with its nanocarriers inside the nerve cells and remains after 24 h of reperfusion. In conclusion, the systemic administration of neuroglobin linked to nanoparticles is a potential neuroprotective drug-delivery strategy after stroke episodes.

Objetivos: La bibliometría es un tipo de estudio estadístico sobre datos científicos. Mediante esta herramienta queremos valernos para visualizar distintos aspectos que presentan los medicamentos biosimilares, su importancia y el impacto que generan en su entorno. Métodos: se ha utilizando como motor de búsqueda Science Direct, así como de publicaciones científicas referenciadas en la bibliografía y como de algunas webs sobre la materia. Resultados: Casi todos los indicadores señalan la gran importancia económica que concierne entorno a los medicamentos biosimilares, la actualidad que presenta y que gran parte de su estudio se concentra alrededor de los pacientes. Conclusiones: Con este trabajo se comprueba el gran interés que ofrecen los biosimilares y sobre todo el impacto que tendrán en un futuro, así como las repercusiones que traerán consigo, sobre todo en los campos económicos y de la salud., Objectives: A bibliometrics study is a type of statistical study on scientific data. With this tool we want to visualize different aspects of biosimilar drugs, their importance and the impact they generate in their environment. Methods: Science Direct was utilized as a search engine, in addition to the scientific publications referenced in the bibliography as well as some websites concerning the subject. Results: Almost all the indicators point to the great economic importance of biosimilar drugs, their novelty and their patient-coentered focus. Conclusions: It is of great interest to know the future impact that these medicines will have and the repercussions they will bring, especially in the economic and health fields., Grupo de Farmacia practica (CTS-205 Junta de Andalucía) proyecto investigación BFU2016-80316-R. Ministerio de Economía y Competitividad.