Colorimetric polymer films for predicting lipid interactions and percutaneous adsorption of pharmaceutical formulations

Izek Ben-Shlush, Roman Volinsky, Marina Katz, Yogesh Scindia, Racheli Itzhak, Hila Tsahor Ohayon, Ido Yosha, Raz Jelinek

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

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.

Original languageEnglish
Pages (from-to)2815-2821
Number of pages7
JournalPharmaceutical Research
Volume25
Issue number12
DOIs
StatePublished - 1 Dec 2008

Keywords

  • Gel formulations
  • Lipid barriers
  • Lipid interactions
  • Passive diffusion
  • Percutaneous absorption

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

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