Does the Digestibility of Cyclodextrins Influence the In Vivo Absorption of Benzo[a]pyrene in Rats?

Journal of Pharmaceutical Sciences
Niels E OlesenRené Holm

Abstract

An important excipient used to overcome poor solubility is cyclodextrin. However, data in the literature suggest that excessive overdosing of cyclodextrins can decrease the absorption of compounds administered with cyclodextrins, due to their lack of release from the complex. γ-Cyclodextrin is digestible in contrast to β-cyclodextrins. This could potentially limit the sensitivity toward overdose, which was evaluated using benzo[a]pyrene in this study, in which rats were administered benzo[a]pyrene and different doses of the 2 cyclodextrins. Both cyclodextrins lowered the area under the curve and therefore the absorption of benzo[a]pyrene by up to a factor of 2 when dosed in high concentrations, thus indicating that overdosing of cyclodextrins may limit the oral absorption of a compound. This limitation may be artificial because the molar ratio of benzo[a]pyrene:cyclodextrin was >1:50,000 at the concentration where a significant decrease in the absorption was observed. No difference was observed between the 2 cyclodextrins, so digestibility seemed less important. More interesting was that the decrease in absorption was relatively small when compared with literature values, suggesting that the effect of overdosing a compound with...Continue Reading

References

Jan 1, 1988·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·H FothG F Kahl
Jan 5, 1971·Biochimica Et Biophysica Acta·E D ReesH Lipscomb
Jul 1, 1996·Journal of Pharmaceutical Sciences·R A Nash
Apr 30, 1998·Journal of Toxicology and Environmental Health. Part a·D MoirE McMullen
Feb 17, 2001·Journal of Applied Toxicology : JAT·K H DiehlUNKNOWN European Federation of Pharmaceutical Industries Association and European Centre for the Validation of Alternative Methods
Feb 19, 2002·Chemical Reviews·József Szejtli
Feb 19, 2002·Chemical Reviews·Kaneto UekamaTetsumi Irie
Aug 12, 2004·Chemical & Pharmaceutical Bulletin·Kaneto Uekama
Dec 2, 2004·Nature Reviews. Drug Discovery·Mark E Davis, Marcus E Brewster
Mar 12, 2005·Journal of Pharmaceutical Sciences·Goran Westerberg, Lars Wiklund
Jul 3, 2007·Advanced Drug Delivery Reviews·Marcus E Brewster, Thorsteinn Loftsson
Jul 17, 2007·Journal of Pharmaceutical Sciences·Thorsteinn LoftssonFífa Konrádsdóttir
Aug 9, 2007·Expert Opinion on Drug Delivery·Alfred Fahr, Xiangli Liu
Sep 25, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Rebecca L CarrierImran Ahmed
Jul 8, 2008·International Journal of Pharmaceutics·Emma L McConnellAbdul W Basit
Apr 11, 2009·Journal of Hazardous Materials·Etienne VeignieGheorghe Surpateanu
Jun 30, 2009·Physical Chemistry Chemical Physics : PCCP·René HolmPeter Westh
Aug 11, 2011·The Journal of Pharmacy and Pharmacology·Thorsteinn Loftsson, Marcus E Brewster
Feb 16, 2012·Journal of Pharmaceutical Sciences·Thorsteinn Loftsson, Marcus E Brewster
Apr 20, 2013·International Journal of Pharmaceutics·René HolmHuiling Mu

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Citations

Mar 13, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Niels Erik OlesenRené Holm

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