Auto-fluorescent PAMAM-based dendritic molecules and their potential application in pharmaceutical sciences



El-Betany AMM, Kamoun EA, James C, Jangher A, Aljayyoussi G, Griffiths P, McKeown NB, Gumbleton M.


Int J Pharm. 2020 Apr 15;579:119187. doi: 10.1016/j.ijpharm.2020.119187. Epub 2020 Mar 2.


The epithelial permeation of water-soluble fluorescent PAMAM dendrons based on 7H-benz[de] benzimidazo [2,1-a] isoquinoline-7-one as a fluorescent core across epithelial cell models MDCK I and MDCK II has been quantified. Hydrodynamic radii have been derived from self-diffusion coefficients obtained via pulsed-gradient spin-echo Nuclear Magnetic Resonance (PGSE-NMR). Results indicate that these dendritic molecules are molecularly disperse, non-aggregating, and only slightly larger than their parent homologues. MDCK I permeability studies across epithelial barriers show that these dendritic molecules are biocompatible with the chosen epithelial in-vitro model and can permeate across MDCK cell monolayers. Permeability is demonstrated to be a property of dendritic size and cell barrier restrictiveness indicating that paracellular mechanisms play the predominant role in the transport of these molecules. CI – Copyright © 2020 Elsevier B.V. All rights reserved.

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Link/DOI: 10.1016/j.ijpharm.2020.119187