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8 papers 0 to 25 followers Artigos Seminário
Thierry Burnouf, Ming-Li Chou, Hadi Goubran, Fabrice Cognasse, Olivier Garraud, Jerard Seghatchian
Blood cells and tissues generate heterogeneous populations of cell-derived vesicles, ranging from approximately 50 nm to 1 µm in diameter. Under normal physiological conditions and as an essential part of an energy-dependent natural process, microparticles (MPs) are continuously shed into the circulation from membranes of all viable cells such as megakaryocytes, platelets, red blood cells, white blood cells and endothelial cells. MP shedding can also be triggered by pathological activation of inflammatory processes and activation of coagulation or complement systems, or even by shear stress in the circulation...
October 2015: Transfusion and Apheresis Science
Linda C Alskär, Christopher J H Porter, Christel A S Bergström
Identification of the usefulness of lipid-based formulations (LBFs) for delivery of poorly water-soluble drugs is at date mainly experimentally based. In this work we used a diverse drug data set, and more than 2,000 solubility measurements to develop experimental and computational tools to predict the loading capacity of LBFs. Computational models were developed to enable in silico prediction of solubility, and hence drug loading capacity, in the LBFs. Drug solubility in mixed mono-, di-, triglycerides (Maisine 35-1 and Capmul MCM EP) correlated (R(2) 0...
January 4, 2016: Molecular Pharmaceutics
Silki, Vivek Ranjan Sinha
Poor aqueous solubility is one of the key concerns of the majority of new drug molecules. One of the important problems associated with such drugs is that they often lead to low bioavailability. Researchers have used various techniques, but little success has been achieved due to poor stability and industrial viability, including technique cost. Of the numerous techniques, nanosuspensions (NSs) have drawn interest in improving solubility. NSs are dispersions of nanosized drug particles stabilized with the aid of appropriate agents...
2015: Critical Reviews in Therapeutic Drug Carrier Systems
Chetan Yewale, Sushilkumar Patil, Atul Kolate, Girish Kore, Ambikanandan Misra
Transport of a drug across the biological membrane of the gastrointestinal tract has turned out to be a critical barrier against the success of any oral drug delivery technology. The unique advantages of the oral route, along with need for an oral substitute of invasive parenteral formulations and the reduction of intersubject variability in plasma profiles, has been an incentive for the use of excipients with absorption-enhancing properties to boost the bioavailability of poorly absorbed drugs. The development of such excipients is not a simple task, so understanding enhancement mechanisms in relation to physiology can facilitate the identification of structure-function relationships as well as the development of newer agents for customary applications...
2015: Critical Reviews in Therapeutic Drug Carrier Systems
B Wahlang, D Kabra, Y B Pawar, K Tikoo, A K Bansal
Curcumin (CRM) (CAS number 458-37-07), a naturally-occurring molecule, has diverse pharmacological actions. Recently our research group demonstrated that poor permeability also contributes to its poor oral bioavailability. A self nano-emulsifying drug delivery system (CRM SNEDDS) consisting of Labrasol, Gelucire 44/14, Vitamin E TPGS and PEG 400 was designed and provided 16 times improvement in oral bioavailability in rats, at a dose of 250 mg/kg body weight. Caco-2 cell transport studies were conducted for CRM SNEDDS and CRM in the presence of individual excipients, to determine the extent of improvement in permeability...
February 2012: Arzneimittel-Forschung
Jonathan Goole, David J Lindley, Wyatt Roth, Stephen M Carl, Karim Amighi, Jean-Michel Kauffmann, Gregory T Knipp
Traditionally most pharmaceutical excipients used for peroral dosage forms have been considered to be inert, although they have been known to play an important role in governing the release of the active pharmaceutical ingredient (API) required for the desired therapeutic effect. Of considerable interest is the emerging data demonstrating that many of these "inert" excipients may produce subtle changes that could directly or indirectly alter the activity of membrane-spanning proteins such as transporters...
June 30, 2010: International Journal of Pharmaceutics
Xiuhua Ren, Xinliang Mao, Luqin Si, Lei Cao, Hui Xiong, Jun Qiu, Aaron D Schimmer, Gao Li
Excipients are largely used as inert vehicles in formulation. Recent studies indicated that some excipients could affect drug transport and disposition. But the effects of most excipients on drug metabolism are yet to be unveiled. To evaluate the actual action of pharmaceutical excipients in biotransformation, we examined the effects of 22 common excipients on cytochrome P450 3A4, the main CYP in intestinal and liver, using midazolam as the probe. The results showed that 15 of 22 (68.2%) tested excipients could inhibit the activity of CYP3A4 more than 50% in vitro, particularly the surfactants and polymers...
September 2008: European Journal of Pharmaceutics and Biopharmaceutics
Huba Kalász, István Antal
The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming the preparation of improved pharmaceuticals. The recently introduced Biopharmaceutical Classification System provides guidance for dosage form design, taking the molecular and physico-chemical properties of drugs into consideration through their solubility and permeability characteristics...
2006: Current Medicinal Chemistry
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