In vitro investigation on the impact of Solutol HS 15 on the uptake of colchicine into rat hepatocytes

International Journal of Pharmaceutics
Roberto C Bravo GonzálezBeate Bittner

Abstract

In the current investigation, the impact of the surface-active formulation ingredient Solutol HS 15 on the uptake of colchicine into freshly isolated rat hepatocytes was investigated using a centrifugal filtration technique through a silicone oil layer. Colchicine is taken up into the cells by an active transport mechanism. When conducting the experiment at 37 degrees C, it was found that at concentrations below its critical micellar concentration (CMC) of 0.021% (0.0003 and 0.003%, w/v), Solutol HS 15 did not impact the uptake of colchicine. By contrast, at a Solutol HS 15 concentration above its CMC (0.03%, w/v), the amount of colchicine taken up into the cells as well as its uptake velocity were significantly decreased. However, in control experiments performed at 4 degrees C, a temperature at which active transport processes should be significantly slowed down, Solutol HS 15 at 0.03% did not affect colchicine uptake and/or its association with the cells. The described findings might be rationalized by inhibition of colchicine transport either due to direct interaction at the transport site or due to alterations of membrane properties in the presence of Solutol HS 15 at concentrations above its CMC. Moreover, a strong molecu...Continue Reading

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Jul 6, 2004·International Journal of Pharmaceutics·Roberto Carlos Bravo GonzálezBeate Bittner

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Citations

Dec 14, 2011·Antimicrobial Agents and Chemotherapy·Todd J JohnsonPatrick F Kiser
Jun 20, 2012·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Anne-Joy M de GraanAlex Sparreboom
Oct 4, 2006·Expert Opinion on Drug Metabolism & Toxicology·Anna Seelig, Grégori Gerebtzoff
Mar 10, 2015·Chemical & Pharmaceutical Bulletin·Yasunori IwaoShigeru Itai
Jun 28, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Emilie AllardJean-Pierre Benoit
Jan 17, 2008·Advanced Drug Delivery Reviews·Talia R BugginsGlyn Taylor
Jul 6, 2004·International Journal of Pharmaceutics·Roberto Carlos Bravo GonzálezBeate Bittner
Jan 1, 2014·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jason A Sprowl, Alex Sparreboom

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