<oai_dc:dc xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:oai_dc="http://www.openarchives.org/OAI/2.0/oai_dc/" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xsi:schemaLocation="http://www.openarchives.org/OAI/2.0/oai_dc/ http://www.openarchives.org/OAI/2.0/oai_dc.xsd">
  <dc:creator>Wenk MR</dc:creator>
  <dc:creator>Fahr A</dc:creator>
  <dc:creator>Reszka R</dc:creator>
  <dc:creator>Seelig J</dc:creator>
  <dc:date>1996</dc:date>
  <dc:description xmlns:ns0="xml" ns0:lang="en">Paclitaxel (taxol) is diterpenoid anticancer drug with a new mechanism of cytostatic action. It is under investigation in clinical trials for treatment of various types of human cancer. A major difficulty in developing paclitaxel as a chemotherapeutic agent in its poor water solubility. In order to improve the bioavailability of paclitaxel, novel vehicle systems such as mixed micelles or liposome-based formulations are being developed. In this study we determined the partition coefficient of paclitaxel partitioning into small unilamellar lipid vesicles composed of 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine using two different methods, namely high-sensitivity titration calorimetry and fluorescence spectrometry. We measured a partition coefficient of Kp approximately equal to 9,500 M-1, a partition enthalpy of Delta H = -25 +/- 3 kcal mol-1 and a free energy of binding of Delta G = -7.9 kcal mol-1. The binding reaction is enthalpy-driven, which can be explained by van der Waals interactions between the hydrophobic drug and the strong temperature dependence of the partition equilibrium. A temperature increase of 10 degrees C reduces the paclitaxel solubility in the lipid phase by a factor of 4.</dc:description>
  <dc:identifier>https://sonar.ch/global/documents/129370</dc:identifier>
  <dc:language>eng</dc:language>
  <dc:relation>info:eu-repo/semantics/altIdentifier/doi/10.1021/js950120i</dc:relation>
  <dc:relation>info:eu-repo/semantics/altIdentifier/pmid/8683453</dc:relation>
  <dc:source>Journal of pharmaceutical sciences. - 1996</dc:source>
  <dc:subject xmlns:ns1="xml" ns1:lang="en">Lipid Bilayers</dc:subject>
  <dc:subject xmlns:ns2="xml" ns2:lang="en">Paclitaxel</dc:subject>
  <dc:subject xmlns:ns3="xml" ns3:lang="en">Temperature</dc:subject>
  <dc:subject xmlns:ns4="xml" ns4:lang="en">Time Factors</dc:subject>
  <dc:title xmlns:ns5="xml" ns5:lang="en">Paclitaxel partitioning into lipid bilayers.</dc:title>
  <dc:type>http://purl.org/coar/resource_type/c_6501</dc:type>
</oai_dc:dc>
