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Yang,Zhenlei; Wang,Longmei; Tian,Liu; Zhang,Xiuping; Huang,Guihua. |
Tadalafil, a long-acting PED-5 inhibitor, is commonly used for the treatment of pulmonary arterial hypertension (PAH). However, its efficacy and clinical application are severely limited by the poor water solubility, low bioavailability and a series adverse effects (e.g. headaches, indigestion). In this study, tadalafil was prepared and loaded into biodegradable PLGA (poly(lactic-co-glycolic acid)) microspheres (TDF-PLGA-MS) via emulsification-solvent evaporation. The resulting microspheres were processed into pulmonary inhalant by freeze drying. The TDF-PLGA-MS was spherical and uniform, with an average particle diameter ~10.29 µm. The encapsulation efficiency and drug loading yield of TDF-PLGA-MS were 81.68% and 8.52%, respectively. The investigation of... |
Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Pulmonary arterial hypertension; Tadalafil; PLGA; Microspheres; Pulmonary administration; Micromeritic; In vitro release; Pharmacokinetic; Tissue distribution. |
Ano: 2019 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100587 |
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Jauffrais, Thierry; Marcaillou-le Baut, Claire; Herrenknecht, Christine; Truquet, Philippe; Sechet, Veronique; Nicolau, Elodie; Tillmann, Urban; Hess, Philipp. |
Azadinium spinosum (Elbrächter and Tillmann), a small marine dinoflagellate, has been recently described as a de novo producer of azaspiracid-1 and -2 (AZA1 and -2) diarrhoeic toxins. A culture of A. spinosum was established in our laboratory and optimised for pilot-scale production of this organism, to evaluate and understand AZA1 and -2 accumulation and biotransformation in blue mussels (Mytilus edulis) fed with A. spinosum. Adult mussels were continuously exposed to A. spinosum over 1 week in 160 L cylindrical conical tanks. Three different diets were tested for contamination: 5000, 10 000 cells mL−1 of A. spinosum and a mixture of 5000 cells mL−1 of A. spinosum with 5000 cells mL−1 of Isochrysis aff. galbana (T-Iso, CCAP 927/14). During the subsequent... |
Tipo: Text |
Palavras-chave: Azaspiracid; Azadinium spinosum; Marine biotoxins; AZA; Tissue distribution; Histology; Bivalve molluscs; Liquid chromatography coupled to tandem mass spectrometry. |
Ano: 2012 |
URL: http://archimer.ifremer.fr/doc/00088/19877/17566.pdf |
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Jauffrais, Thierry; Kilcoyne, Jane; Herrenknecht, Christine; Truquet, Philippe; Sechet, Veronique; Miles, Christopher O.; Hess, Philipp. |
The relationship between azaspiracid shellfish poisoning and a small dinoflagellate, Azadinium spinosum, has been shown recently. The organism produces AZA1 and -2, while AZA3 and other analogues are metabolic products formed in shellfish. We evaluated whether mussels were capable of accumulating dissolved AZA1 and -2, and compared the toxin profiles of these mussels at 24 h with profiles of those exposed to live or lysed A. spinosum. We also assessed the possibility of preparative production of AZA metabolites by exposing mussels to semi-purified AZA1. We exposed mussels to similar concentration of AZAs: dissolved AZA1+2 (crude extract) at 7.5 and 0.75 µg L-1, dissolved AZA1+2 (7.5 µg L-1) in combination with Isochrysis affinis galbana, and lysed and live... |
Tipo: Text |
Palavras-chave: Dissolved marine biotoxins; AZA; Tissue distribution; Bivalve molluscs; LC-MS/MS; Azaspiracid. |
Ano: 2013 |
URL: http://archimer.ifremer.fr/doc/00136/24757/22867.pdf |
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Seyedian,R; Jalali,A; Babaee,MH; Pipelzadeh,MH; Rezaee,S. |
The purpose of the present study was to investigate the biodistribution profile of the venom of Hemiscorpius lepturus, the most dangerous scorpion in Iran. Blood and tissue samples were taken at various predetermined intervals during a 400-minute period for the venom and a 360-minute period for the antivenom in rats. The radio-iodination was carried out using the chloramine-T method. The results showed that the descending order of venom uptake was skin, kidneys and intestine, respectively. The descending order of polyclonal antivenom uptake was kidneys, intestine, heart and lungs. The calculated pharmacokinetic parameters of the venom were Telimination half-life = 521.5 ± 12.6 minutes; Vd/F (apparent volume of distribution) = 14.9 ± 3.3 mL; clearance... |
Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Hemiscorpius lepturus scorpion venom; Polyvalent antivenom; Pharmacokinetic parameters; Tissue distribution. |
Ano: 2012 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992012000400005 |
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