Calcium silicate–poly(n-butyl-2-cyanoacrylate) nanocomposite has been studied as a promising biomaterial to immobilize small bone fragments in order to achieve adequate fracture healing. The aim of ...this work was to investigate the in-vitro and in-vivo biocompatibility of the synthetic nanocomposite produced. The samples were characterized by means of infrared spectroscopy, thermogravimetric analysis, scanning and transmission electron microscopy. Bioactivity, degradability, cytotoxicity and implantation tests were performed. Experimental results showed the degradability of the nanocomposite, no cytotoxicity and a significant apatite nucleation and growth on the material surfaces after seven days of immersion in simulated body fluid. The new bone formation observed on the surface of the nanocomposite implanted in vivo is an indicator of its biocompatibility.
Abstract
Calcium silicate–poly(n-butyl-2-cyanoacrylate) nanocomposite has been studied as a promising biomaterial to immobilize small bone fragments in order to achieve adequate fracture healing. The ...aim of this work was to investigate the in-vitro and in-vivo biocompatibility of the synthetic nanocomposite produced. The samples were characterized by means of infrared spectroscopy, thermogravimetric analysis, scanning and transmission electron microscopy. Bioactivity, degradability, cytotoxicity and implantation tests were performed. Experimental results showed the degradability of the nanocomposite, no cytotoxicity and a significant apatite nucleation and growth on the material surfaces after seven days of immersion in simulated body fluid. The new bone formation observed on the surface of the nanocomposite implanted in vivo is an indicator of its biocompatibility.
N-Acylhydrazones as drugs Thota, Sreekanth; Rodrigues, Daniel A.; Pinheiro, Pedro de Sena Murteira ...
Bioorganic & medicinal chemistry letters,
09/2018, Letnik:
28, Številka:
17
Journal Article
Recenzirano
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•N-Acylhydrazone (NAH) motif in Drug Design and Medicinal Chemistry.•NAH-related approved drugs.•N-Acylhydrazone motif scaffolds in clinical trials.•Preclinical ...N-acylhydrazones.•Stability and Pharmacokinetic profile of N-acylhydrazones.
Over the last two decades, N-acylhydrazone (NAH) has been proven to be a very versatile and promising motif in drug design and medicinal chemistry. Herein, we discuss the current and future challenges in the emergence of bioactive NAH-based scaffolds and to developing strategies to overcome the failures in drug discovery. The NAH-related approved drugs nitrofurazone, nitrofurantoin, carbazochrome, testosterone 17-enanthate 3-benzilic acid hydrazine, nifuroxazide, dantrolene, and azumolene are already used as therapeutics in various countries. PAC-1 is an NAH-based therapeutic agent that entered clinical trials in 2015. Another NAH-derived scaffold, LASSBio-294, is in preclinical trials. This review highlights the detailed comprehensive assessment and therapeutic landscape of bioactive NAH motif scaffolds in preclinical and clinical studies published to date and their promise and associated challenges in current and future drug discovery of NAH-based drugs that will progress to clinical use.
Auditory hallucinations are defined as experiences of auditory perceptions in the absence of a provoking external stimulus. They are the most prevalent symptoms of schizophrenia with high capacity ...for chronicity and refractoriness during the course of disease. The transcranial direct current stimulation (tDCS) - a safe, portable, and inexpensive neuromodulation technique - has emerged as a promising treatment for the management of auditory hallucinations.
The aim of this study is to analyze the level of evidence in the literature available for the use of tDCS as a treatment for auditory hallucinations in schizophrenia.
A systematic review was performed, searching in the main electronic databases including the Cochrane Library and MEDLINE/PubMed. The searches were performed by combining descriptors, applying terms of the Medical Subject Headings (MeSH) of Descriptors of Health Sciences and descriptors contractions. PRISMA protocol was used as a guide and the terms used were the clinical outcomes ("Schizophrenia" OR "Auditory Hallucinations" OR "Auditory Verbal Hallucinations" OR "Psychosis") searched together ("AND") with interventions ("transcranial Direct Current Stimulation" OR "tDCS" OR "Brain Polarization").
Six randomized controlled trials that evaluated the effects of tDCS on the severity of auditory hallucinations in schizophrenic patients were selected. Analysis of the clinical results of these studies pointed toward incongruence in the information with regard to the therapeutic use of tDCS with a view to reducing the severity of auditory hallucinations in schizophrenia. Only three studies revealed a therapeutic benefit, manifested by reductions in severity and frequency of auditory verbal hallucinations in schizophrenic patients.
Although tDCS has shown promising results in reducing the severity of auditory hallucinations in schizophrenic patients, this technique cannot yet be used as a therapeutic alternative due to lack of studies with large sample sizes that portray the positive effects that have been described.
Wollastonite-poly(n-butyl-2-cyanoacrylate) composite (W-BCA) has been proposed to immobilize anatomically bone fragments in order to achieve an optimal healing process. The present study evaluated ...the in vitro and in vivo behavior of three types of fillers: powdered natural wollastonite (Wn), synthetic pseudowollastonite powder (Ws), and synthetic pseudowollastonite powder coated with 5% acetyl tributyl citrate (Wst). The Wst-BCA composite underwent a higher degradability in the real-time degradation test and a superior cytotoxic effect; whereas the Wn-BCA composite showed a higher degradability in the accelerated test with no cytotoxicity. The formation of an extracellular collagenous matrix deposit on its surface and the most favorable new bone formation on Wn-BCA indicate its potential for bone adhesive use in unstable orthopedic traumas.
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A potential standard method for measuring the relative dissolution rate to estimate the resorbability of calcium-phosphate-based ceramics is proposed. Tricalcium phosphate (TCP), ...magnesium-substituted TCP (MgTCP) and zinc-substituted TCP (ZnTCP) were dissolved in a buffer solution free of calcium and phosphate ions at pH 4.0, 5.5 or 7.3 at nine research centers. Relative values of the initial dissolution rate (relative dissolution rates) were in good agreement among the centers. The relative dissolution rate coincided with the relative volume of resorption pits of ZnTCP in vitro. The relative dissolution rate coincided with the relative resorbed volume in vivo in the case of comparison between microporous MgTCPs with different Mg contents and similar porosity. However, the relative dissolution rate was in poor agreement with the relative resorbed volume in vivo in the case of comparison between microporous TCP and MgTCP due to the superimposition of the Mg-mediated decrease in TCP solubility on the Mg-mediated increase in the amount of resorption. An unambiguous conclusion could not be made as to whether the relative dissolution rate is predictive of the relative resorbed volume in vivo in the case of comparison between TCPs with different porosity. The relative dissolution rate may be useful for predicting the relative amount of resorption for calcium-phosphate-based ceramics having different solubility under the condition that the differences in the materials compared have little impact on the resorption process such as the number and activity of resorbing cells.
The evaluation and subsequent optimization of the resorbability of calcium phosphate are crucial in the use of resorbable calcium phosphates. Although the resorbability of calcium phosphates has usually been evaluated in vivo, establishment of a standard in vitro method that can predict in vivo resorption is beneficial for accelerating development and commercialization of new resorbable calcium phosphate materials as well as reducing use of animals. However, there are only a few studies to propose such an in vitro method within which direct comparison was carried out between in vitro and in vivo resorption. We propose here an in vitro method based on measuring dissolution rate. The efficacy and limitations of the method were evaluated by international round-robin tests as well as comparison with in vivo resorption studies for future standardization. This study was carried out as one of Versailles Projects on Advanced Materials and Standards (VAMAS).
Calcium phosphate salts, or more specifically hydroxyapatite, are products of great interest in the fields of medical and dental science due to their biocompatibility and osteoconduction property. ...Deproteinized xenografts are primarily constituted of natural apatites, sintered or not. Variations in the industrial process may affect physicochemical properties and, therefore, the biological outcome. The purpose of this work was to characterize the physical and chemical properties of deproteinized xenogenic biomaterials, Bio-Oss (Geistlich Biomaterials, Wolhuser, Switzerland) and Gen-Ox (Baumer S.A., Brazil), widely used as bone grafts. Scanning electron microscopy, infrared region spectroscopy, X-ray diffraction, thermogravimetry and degradation analysis were conducted. The results show that both materials presented porous granules, composed of crystalline hydroxyapatite without apparent presence of other phases. Bio-Oss presented greater dissolution in Tris-HCl than Gen-Ox in the degradation test, possibly due to the low crystallinity and the presence of organic residues. In conclusion, both commercial materials are hydroxyapatite compounds, Bio-Oss being less crystalline than Gen-Ox and, therefore, more prone to degradation.
Purpose. This study aimed to evaluate reports of patents for oral care formulations, based on Camellia sinensis (C. sinensis), deposited and granted in intellectual property banks. Methods. A survey ...was conducted through collection, treatment, and analysis of extracted information from patent reports selected. The documentary research was conducted in January 2021 on formulations with C. sinensis for dental applications, including since the first patent deposits until the current time. The risk of bias of clinical trials with these formulations was analyzed to verify the scientific evidence. The data extracted represent the distribution of the number of patents by banks, annual evolution of patent deposits, applicant of patents by country, distribution of patents according to International Patent Classification codes, and the types of patented products. Results. Data and information from 20 selected patents were extracted. The United States Patent and Trademark Office (USPTO) and World Intellectual Property Organization (WIPO) were the banks with the largest number of patents for products/formulations with C. sinensis for oral care applications with 7 (35%) and 6 (30%) patent registrations, respectively. Other banks did not provide patents related to the search. Patents of compositions were the largest with 14 filings, and the remainder of formulations are represented specially by mouthwashes and toothpastes. As for clinical application, 18 patents were filed as products with antimicrobial and antibiofilm action, while 2 patents are directed to the treatment of xerostomia. In general, the aspects of the studies of clinical efficacy pointed to a low risk of bias. Conclusion. The study pointed out a small number of products protected by patents for Camellia sinensis for oral care indication, highlighting mainly mouthwash compositions and formulations. In the methodological parameters of clinical trials carried out with the formulations, the majority pointed out a low risk of bias.
Compatibility of the new environmentally-friendly alternative of diesel engine fuels, biodiesel, with storage and engine part materials, is still an open issue. In this work, the interaction between ...three fuels (petroleum diesel and two types of biodiesel — soybean and sunflower) and two materials (carbon steel and high density polyethylene) used in storage and automotive tanks, is analyzed in detail. A wide set of characterization techniques was used to evaluate the changes in both solid and fluid materials, as weight change measurement, optical, scanning electron and atomic force (AFM) microscopies, Raman and FTIR spectroscopies, and differential scanning calorimetry. The AFM technique allowed detecting surface roughness and morphology changes in the metallic material following the trends in the weight losses. In the case of polymeric material, weight gain by fluid absorption occurred, being detected by the spectroscopic techniques. The biodiesel fuels underwent some ageing however this phenomenon did not affect the interaction between the biodiesel fuels and the substrates. The petrodiesel, which did not age, caused more significant degradation of the substrates.
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