Pharmacokinetics of cisplatin administered by the pulmonary route were established in mice using dry powders inhaler (DPI) formulations showing immediate (F1) and controlled release (cR, solid lipid microparticles) in...
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Pharmacokinetics of cisplatin administered by the pulmonary route were established in mice using dry powders inhaler (DPI) formulations showing immediate (F1) and controlled release (cR, solid lipid microparticles) in vitro, without (F2) or with PEGylated excipients (F3, F4). Formulation administration was realized using dry powder blends (correspondingly named thereafter F1(B) to F4(B)) able to reproducibly deliver particles in vivo using a DP-4M Dry Powder Insufflator (TM). Their platinum pharmacokinetics were established over 48 h in lungs, total blood and non-target organs vs. IV and endotracheal nebulization (EN). EN and FIB were rapidly distributed from the lungs (t(1/2)(i) 2.6 and 5.0 min). F2(B) was eliminated in similar to 1 h (t(1/2)(i) 9.0 min). F3(B) lung retention was sustained for similar to 7 h (t(1/2)(i) 59.9 min), increasing lung AUc 11-, 4 and 3-fold vs. IV, F1(B) and F2(B). Total blood t(max) were higher and AUc and c-max lower using the pulmonary route vs. IV. Kidney c-max was reduced 6-, 2- and 3-fold for F1(B), F2(B) and F3(B). AUc in kidneys were 2- to 3-fold lower for F1(B) and F2(B) vs. IV but comparable for IV vs. F3(B), probably because of kidney saturation. PEGylated solid lipid microparticles provided cisplatin particles with interesting lung retention and cR properties. (c) 2016 Elsevier B.V. All rights reserved.
calotropis procera and calotropis gigantea are medicinal plant having therapeutic value. The leaf extracts of c. procera have been investigated, its pharmacological actions in detail and leaf extracts of c. gigantea w...
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calotropis procera and calotropis gigantea are medicinal plant having therapeutic value. The leaf extracts of c. procera have been investigated, its pharmacological actions in detail and leaf extracts of c. gigantea were not studied till date. The objective of present work was to find the bioactive constituents present in the ethanolic leaf extract of c. procera and c. gigantea to evaluate their antibacterial and anifungal activities. The major phytochemical groups in c. procera ethanolic leaf extracts were fatty acid ethyl ester (21.36%), palmitic acid ester (10.24%), linoleic acid (7.43%) and amino acid (8.10%) respectively, whereas ethanolic leaf extracts of c. gigantea contain palmitic acid (46.01%), diterpene (26.53%), triterpene (17.39%), linoleic acid (5.13%) as the major phytochemical groups. Ethanol extract of c. procera leaves showed the highest inhibition (11mm) against Escherichia coli, while ethanolic extract of c. gigantea leaves inhibited Klebsiella (20mm). These findings will use in new directions in pharmacological investigations. [GRAPHIcS] .
candida albicans is one of the most common fungal pathogens, and causes systemic and invasive infections in humans. c. albicans biofilms are composed of yeast and hyphal and pseudohyphal elements, and the transition o...
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candida albicans is one of the most common fungal pathogens, and causes systemic and invasive infections in humans. c. albicans biofilms are composed of yeast and hyphal and pseudohyphal elements, and the transition of yeast to the hyphal stage could be a virulence factor. In this study, diverse essential oils were initially investigated for anti-biofilm activity against c. albicans strains, and cascarilla bark oil and helichrysum oil and their components -longipinene (a major constituent of both) and linalool were found to markedly inhibit biofilm formation without affecting planktoniccell growth. Moreover, -longipinene and linalool were found to synergistically reduce biofilm formation. Notably, treatments with cascarilla bark oil, helichrysum oil, -longipinene, or linalool clearly inhibited hyphal formation, and this appeared to be largely responsible for their anti-biofilm effect. Furthermore, the two essential oils, -longipinene and linalool, reduced c. albicans virulence in caenorhabditis elegans.
在神话传说与现实世界中,并蒂双生的命运成就了无数令人艳羡的两全其美。无论高居奥林匹斯十二主神的同胞姐弟狩猎女神阿尔忒弥斯与太阳神阿波罗,还是实现人类翱翔蓝天梦想的菜特兄弟,亦或16年来横贯网坛的大小威廉姆斯姐妹,都如闪耀的双子星一般造就了一段段佳话。而在赛道上,当全新梅赛德斯-AMG c 63轿跑车于2015年法兰克福车展横空问世后,便与梅赛德斯-AMG c 63轿车组成了叱咤风云的双子战神。两者以无与伦比的惊艳设计、极具爆发力的动力表现以及卓越安全科技,成为当今车坛的传奇双生车型。
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