ization with a pKa value of pH 8.8, is classified as a type IA antiarrhythmic drug, and has been used for the management of ventricular arrhythmias. The drug is absorbed rapidly and almost entirely after oral administration, and is detected in the plasma within 15 min. Quinidine binds to both albumin and a1-acid glycoprotein, and the proportion that binds to plasma protein is 70 to 95%. However...

The present study aimed at exploring the potential of the P-glycoprotein (P-gp) transporters as a barrier to the repaglinide (REG) epithelial permeability. In-vitro intestinal absorption models, the everted gut sac, and Caco-2 cell line, were used to study the possible role of P-gp in intestinal transport of REG. In the everted gut sacs, apparent permeability coefficients showed cargo concentra...

The vascular endothelium presents a major transport barrier to drug delivery by only allowing selective extravasation of solutes and small molecules. Therefore, enhancing drug transport across the endothelial barrier has to rely on leaky vessels arising from disease states such as pathological angiogenesis and inflammatory response. Here we show that the permeability of vascular endothelium can...

This review focuses on epithelial drug transport mechanisms in mucosal drug delivery: the final step of a four-part process. Reference is made to the mucosae lining the oral cavity and the gastrointestinal tract, the two mucosae most often succumbing to the side effects of cytotoxic chemotherapeutic drugs. This review will be devoted to carrier-mediated transport, particularly as it relates to ...

Intestinal lymphatic drug delivery has been widely studied because drugs can bypass the first-pass metabolism in the liver via the lymphatic route, which increases oral bioavailability. Various lipid-based nanoparticles have been used to deliver hydrophobic drugs to the lymphatic pathway. This review focuses on the liposomal delivery systems used for intestinal lymphatic drug transport. Liposom...

nowadays apphcanon of nanotubes in biology and medicinal science is more investigated. nanotubes can passthroueh cell walls and transport and release drugs in special tissues. the purpose of this paper is to investigatethe interaction of a nanotube having hydroxyl functional groups (oh) with an anticancer agent. in this worktransporting of an anticancer drug named 2-(2-amino 6,7-dimethyl pterid...

celecoxib is used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, joint inflammation and sport injuries. long term administration of the drug results in such complications as gastrointestinaland renal disturbances and cardio-vascular complications. the main objective of the present study was to investigate the feasibility of delivering celecoxib incorporated in gel formula...

the drug pump protein mrp2 is a membrane drug efflux transporter widely distributed in normal and tumor tissues. its role is thought to be crucial for the disposition of many drugs and their substrates in different tissues. in this study, we aimed to examine the effects of systematic inflammation induced by lipopolysaccharide (lps) on the expression and function of this transporter in rats. jug...

Human serum albumin (HSA) is the most abundant plasma protein in the human body. HSA plays an important role in drug transport and metabolism. This protein has a high affinity to a very wide range of materials, including metals such as Cu2+ and Zn2+, fatty acids, amino acids and metabolites such as bilirubin and many drug compounds. In this study, we investigated the effects of co-amoxiclav, as...

Characteristics of Methotrexate transport by normal and leukemic human leukocytes were measured in vitro. At high external drug levels (3:20 MM) drug uptake by all cell types was temperature-insensitive, nonsaturable, and nonconcentrative. The steady-state cell/medium drug distribution ratio was about 0.03. During clinical treatment with Methotrexate, plasma drug levels generally reach 0.2 MM. ...