Transporter properties of drugs

Polar surface area (PSA) - defined simply as the part of a molecular surface that is polar - is probably, together with the octanol-water partition coefficient, one of the most important parameters used to characterize the transport properties of drugs. PSA has been shown to provide very good correlations with intestinal... 

Klopman, G., Zhu, H. Recent methodologies for the estimation of tt-odanol/water partition coeffidents and their use in the prediction of membrane transport properties of drugs. Minirev. Med. Chem. 2005, 5, 127-133. 

V. Use of Immobilized Artificial Membranes and Liposomes to Predict Transport Properties of Drugs or Toxicants... 

V. USE OF IMMOBILIZED ARTIFICIAL MEMBRANES AND LIPOSOMES TO PREDICT TRANSPORT PROPERTIES OF DRUGS OR TOXICANTS... 

Sjostrom M, Sjoberg A, Utter L, Hyltander A, KarlssonJ, Stockman E, and Ungell AL. Excised Human Intestinal Segments as a Mechanistic Tool for Verifying Transport Properties of Drug Candidates. Abstract AAPS 2000. Pharm Sci 2000 suppl. 

Mixed micelle formation and complex formation will achieve similar alterations in the transport properties of drug molecules. When the drug molecules themselves can aggregate, this will result in a reduction in permeability above their critical micelle concentration [221, 223]. 

Norinder, U., Osterberg, Th. The applicability of computational chemistry in the evaluation and prediction of drug transport properties. Perspect. Drug Discov. Des. 2000, 19, 1-18. 

Improved characterization of the morphological/microstructural properties of porous solids, and the associated transport properties of fluids imbibed into these materials, is crucial to the development of new porous materials, such as ceramics. Of particular interest is the fabrication of so-called functionalized ceramics, which contain a pore structure tailored to a specific biomedical or industrial application (e.g., molecular filters, catalysts, gas storage cells, drug delivery devices, tissue scaffolds) [1-3]. Functionalization of ceramics can involve the use of graded or layered pore microstructure, morphology or chemical composition. 

Belinsky, M.G., Chen, Z.S., Shchaveleva, I., Zeng, H. and Kruh, G.D. (2002) Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6). Cancer Research, 62, 6172-6177. 

Brouneus, F., et al. 2001. Diffusive transport properties of some local anesthetics applicable for iontophoretic formulation of the drugs. Int J Pharm 218 57. 

Apiwattanakul N, Sekine T, Chairoungdua A, et al. Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. Mol Pharmacol 1999 55 847-854. 

Both of these objectives are achievable provided the delivery (transport) properties of the drug are improved while maintaining its biological activity in vivo. In this context, the parent drug properties, such as lipid solubility, aqueous solubility, partition coefficient, and chemical and metabolic stability, are optimized, often in a balanced combination. 

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