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

• Published in: Macromolecular rapid communications. Vol. 27; no. 14; pp. 1149 - 1155
• Main Authors: van Drooge, Dirk Jan, Braeckmans, Kevin, Hinrichs, Wouter L. J., Remaut, Katrien, De Smedt, Stefaan C., Frijlink, Henderik W.
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 24.07.2006; WILEY‐VCH Verlag; Wiley
• Subjects: amorphous clusters; Application fields; Applied sciences; Biological and medical sciences; drug delivery systems; Exact sciences and technology; fluorescence resonance energy transfer (FRET); General pharmacology; imaging; Medical sciences; molecular dispersion; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymer industry, paints, wood; Technology of polymers; drug delivery systems; amorphous clusters; Control release polymer; fluorescence resonance energy transfer (FRET); Dispersion degree; Solid dispersion; Drug carrier; Experimental study; imaging; Fluorescence spectrometry; Lipophilic compound; Nanometer scale; Pyrrolidone(vinyl) polymer; Resonant energy transfer; Measurement method; molecular dispersion
• ISSN: 1022-1336; 1521-3927
• DOI: 10.1002/marc.200600177

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).