Inclusion complexation of propofol with 2-hydroxypropyl-beta-cyclodextrin. Physicochemical, nuclear magnetic resonance spectroscopic studies, and anesthetic properties in rat. trapani@ippo.uniba.it

Journal of Pharmaceutical Sciences
G TrapaniGaetano Liso

Abstract

An aqueous formulations of propofol 1 can be prepared by solubilizing it in the presence of 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD). This is potentially useful for parenteral administration of the drug. The aqueous solubility of 1 linearly increased as a function of HP-beta-CD concentration and showed features of an AL type diagram. Thermodynamic parameters were obtained by using the temperature dependence of the stability constant at temperatures of between 25 and 37 degrees C. The results indicate that complex formation is enthalpically, rather than entropically, driven and that it may involve van der Waals (dispersive) forces, rather than hydrophobic interactions. The structure of the inclusion complex propofol/HP-beta-CD was investigated in D2O, using 1H and 13C NMR spectroscopy. These studies revealed that the whole aromatic ring, as well as part of the isopropyl groups of the guest molecule, is located inside the HP-beta-CD cavity, while the hydroxy group is located at the rim of the wider cavity end. The geometrical features of the inclusion complex 1-HP-beta-CD are confirmed by 1D NOE difference spectra and molecular modeling experiments. The anesthetic activity in rat was investigated, and it was found that ther...Continue Reading

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Citations

Apr 20, 2005·Pharmaceutical Research·Hongming ChenColin R Gardner
Sep 19, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Cosimo AltomareGaetano Liso
May 1, 2008·AAPS PharmSciTech·Abhijit A Date, Mangal S Nagarsenker
Jan 9, 2010·Therapeutics and Clinical Risk Management·Eric A HarrisKeith A Candiotti
May 26, 2004·International Journal of Pharmaceutics·Adriana TrapaniGaetano Liso
Apr 30, 2015·Pharmaceutical Development and Technology·Noorullah Naqvi MohammedMichael A Repka
Mar 7, 2015·Journal of Materials Science. Materials in Medicine·Alireza Hassani NajafabadiSina Farzaneh
Oct 22, 2013·Journal of Biomolecular Structure & Dynamics·Aura SilvaDavid A Ferreira
Oct 5, 2006·Current Opinion in Anaesthesiology·Guy L Ludbrook, Richard N Upton
Jul 7, 2007·Pharmaceutical Development and Technology·Chantal HolvoetJacqueline Plaizier-Vercammen
Apr 18, 2017·Journal of Anaesthesiology, Clinical Pharmacology·Aiden Y FengRichard D Urman
Oct 29, 2002·Anesthesia and Analgesia·Mariusz G BanaszczykSheldon S Hendler
Sep 30, 2005·Anesthesiology·Max T Baker, Mohamed Naguib
Oct 19, 2020·Journal of Pharmaceutical Sciences·Thorsteinn Loftsson

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