Colorimetric Polymer Films for Predicting Lipid Interactions and Percutaneous Adsorption of Pharmaceutical Formulations |
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Authors: | Izek Ben-Shlush Roman Volinsky Marina Katz Yogesh Scindia Racheli Itzhak Hila Tsahor Ohayon Ido Yosha Raz Jelinek |
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Institution: | (1) Department of Chemistry and Ilse Katz Institute for Nanotechnology, Ben Gurion University of the Negev, Beersheba, 84105, Israel;(2) Perrigo Israel Pharmaceutical Ltd., Yeruham, Israel |
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Abstract: | Purpose To develop and demonstrate a rapid and simple colorimetric film assay for evaluating lipid interactions of pharmaceutical
compounds and gel formulations.
Methods The colorimetric assay comprises glass-supported films of phospholipids and polydiacetylene, which undergo visible and quantifiable
blue–red transformations induced by interactions with amphiphilic molecules applied in very small volumes on the film surface.
The color transitions are recorded by scanning of the films, and quantified through a simple image analysis algorithm.
Results We show that pharmaceutical molecules and gel formulations induce blue–red transformations after short incubation with the
lipid/polydiacetylene (PDA) films. Colorimetric dose–response curves exhibit dependence upon the lipid affinity and extent
of membrane binding of the pharmaceutical compounds examined. The colorimetric lipid/PDA film assay was employed for distinguishing
the contributions of individual molecular components within gel formulations.
Conclusions The colorimetric data yield insight into the degree of lipid binding of the molecules tested. The film assay is particularly
advantageous for analysis of semi-solid (gel or lotion) formulations, elucidating the lipid interaction characteristics of
specific molecular components within the mixtures. The new colorimetric film assay constitutes a generic, rapid, and easily
applicable platform for predicting and screening interactions of pharmaceutical compounds and complex formulations with lipid
barriers.
Izek Ben-Shlush and Roman Volinsky contributed equally. |
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Keywords: | gel formulations lipid barriers lipid interactions passive diffusion percutaneous absorption |
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