Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Spectrofluorimetric study of eflucimibe-gamma-cyclodextrin inclusion complex.

Nathalie Mesplet1, Philippe Morin, Jean-Paul Ribet

  • 1Institut de Chimie Organique et Analytique (I.C.O.A), Université d'Orléans, Orléans, France.

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V
|March 12, 2005
PubMed
Summary

Eflucimibe, a potent ACAT inhibitor, forms a 1:1 inclusion complex with gamma-cyclodextrin (gamma-CD). This complex formation, evidenced by fluorescence, enhances drug solubility for pharmaceutical formulation.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

40  W of supercontinuum generated by a self-pulsed pump-sharing oscillator-amplifier.

Applied optics·2024
Same author

Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-<i>d</i>]Pyrimidine Series as Novel PI3K/mTOR Inhibitors.

Molecules (Basel, Switzerland)·2021
Same author

30  TW and 33  fs pulses delivered by a Ti:Sa amplifier system seeded with a frequency-doubled fiber laser.

Applied optics·2020
Same author

Capillary electrophoresis with dual detection UV/C<sup>4</sup>D for monitoring myrosinase-mediated hydrolysis of thiol glucosinolate designed for gold nanoparticle conjugation.

Analytica chimica acta·2019
Same author

Effect of modified di- and trisaccharides on hyaluronidase activity assessed by capillary electrophoresis-based enzymatic assay.

Carbohydrate research·2019
Same author

Monitoring of successive phosphorylations of thymidine using free and immobilized human nucleoside/nucleotide kinases by Flow Injection Analysis with High-Resolution Mass Spectrometry.

Analytica chimica acta·2019

Area of Science:

  • Pharmaceutical Chemistry
  • Drug Delivery
  • Supramolecular Chemistry

Background:

  • Eflucimibe is a novel, potent acyl-coenzyme A cholesterol O-acyl-transferase (ACAT) inhibitor.
  • Eflucimibe exhibits poor aqueous solubility and weak natural fluorescence, posing formulation challenges.

Purpose of the Study:

  • To investigate the complexation of eflucimibe with gamma-cyclodextrin (gamma-CD).
  • To determine the stoichiometry and association constant of the eflucimibe-gamma-CD inclusion complex.
  • To assess the utility of gamma-CD for improving eflucimibe's aqueous solubility.

Main Methods:

  • Fluorescence spectroscopy was employed to monitor complex formation.
  • The Benesi-Hildebrand method (double reciprocal plots) was used to analyze fluorescence data.

Related Experiment Videos

  • Complex stoichiometry and association constants were calculated from the spectral changes.

    • Main Results:

    • A significant increase in eflucimibe's fluorescence signal was observed upon addition of gamma-CD, indicating complex formation.
    • The stoichiometry of the inclusion complex was determined to be 1:1 (eflucimibe:gamma-CD).
    • The formation constant (association constant) for the complex was calculated as 20 M⁻¹ in a 10% methanol aqueous solution.

    Conclusions:

    • Eflucimibe forms a non-covalent 1:1 inclusion complex with gamma-CD.
    • The determined formation constant provides valuable data for pharmaceutical formulation development.
    • Gamma-cyclodextrin shows potential for enhancing the aqueous solubility and formulation of hydrophobic drugs like eflucimibe.