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Characterization of the Mode of Incorporation of Lipophilic Compounds in Solid Dispersions at the Nanoscale Using Fluorescence Resonance Energy Transfer (FRET)

✍ Scribed by Dirk Jan van Drooge; Kevin Braeckmans; Wouter L. J. Hinrichs; Katrien Remaut; Stefaan C. De Smedt; Henderik W. Frijlink


Publisher
John Wiley and Sons
Year
2006
Tongue
English
Weight
217 KB
Volume
27
Category
Article
ISSN
1022-1336

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✦ Synopsis


Abstract

Summary: Efficient engineering of solid dispersions stagnates by the current inability to establish the mode of drug distribution on a molecular level at a low drug load. This study describes the application of fluorescence resonance energy transfer (FRET) to characterize the mode of incorporation of dispersed lipophilic molecules in a solid matrix. Two different lipophilic fluorophores (donor and acceptor) were used as model substances and were incorporated in polyvinylpyrrolidone to form solid dispersions using two different production processes: lyophilization and fusion. The efficiency of the resonance energy transfer from donor to acceptor was measured by confocal microscopy. We show that the method can be used to compare the modes of drug incorporation of solid dispersions at the nanoscale.

Absorption and emission spectra of Bodipy R6G (donor) and Bodipy 650/665 (acceptor).

magnified imageAbsorption and emission spectra of Bodipy R6G (donor) and Bodipy 650/665 (acceptor).