scholarly journals Carrier mediated transport of actinides using hexa–n-hexylnitrilotriacetamide (HHNTA)

Author(s):  
Bholanath Mahanty ◽  
Ananda Karak ◽  
Prasanta K. Mohapatra ◽  
Richard J.M. Egberink ◽  
Thichur P. Valsala ◽  
...  
Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 272
Author(s):  
Arik Dahan ◽  
Isabel González-Álvarez

The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In this Editorial we provide an overview of the Special Issue "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation". The objective of this Special Issue is to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.


Drug Research ◽  
2020 ◽  
Author(s):  
Meenakshi Dhanawat ◽  
Sumeet Gupta ◽  
Dinesh Kumar Mehta ◽  
Rina Das

Nipecotic acid is considered to be one of the most potent inhibitors of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Due to its hydrophilic nature, nipecotic acid does not readily cross the blood-brain barrier (BBB). Large neutral amino acids (LAT1)-knotted nipecotic acid prodrug was designed and synthesized with the aim to enhance the BBB permeation by the use of carrier-mediated transport. The synthesized prodrug was tested in animal models of Pentylenetetrazole (PTZ)-induced convulsions in mice. Further pain studies were carried out followed by neurotoxicity estimation by writhing and rota-rod test respectively. HPLC data suggests that the synthesized prodrug has improved penetration through BBB. Nipecotic acid-L-serine ester prodrug with considerable anti-epileptic activity, and the ability to permeate the BBB has been successfully synthesized. Graphical Abstract.


2004 ◽  
Vol 39 (16) ◽  
pp. 3821-3838 ◽  
Author(s):  
R. Bucci ◽  
S. Canepari ◽  
E. Cardarelli ◽  
A. M. Girelli ◽  
A. Pietrodangelo ◽  
...  

1981 ◽  
Vol 648 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Lawrence E. Lavi ◽  
James B. Hermiller ◽  
Charles C. Griffin

2004 ◽  
Vol 244 (1-2) ◽  
pp. 251-257 ◽  
Author(s):  
S KUSUMOCAHYO ◽  
T KANAMORI ◽  
K SUMARU ◽  
S AOMATSU ◽  
H MATSUYAMA ◽  
...  

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