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Title: Enhanced intestinal permeability of bufalin by a novel bufalin-peptide-dendrimer inclusion through caco-2 cell monolayer
Authors: Chan, CO 
Jing, J
Xiao, W
Tan, Z
Lv, Q
Yang, J
Chen, S 
Issue Date: 2017
Source: Molecules, Dec. 2017, v. 22, no. 12, 2088, p. 1-8
Abstract: Bufalin (BFL) has excellent physiological activities such as defending tumors, improving cardiac function, and so on. However, due to its poor water-solubility and bioavailability, the clinical application of BFL remains limited. In order to improve bioavailability of BFL, in our previous research, a novel peptide-dendrimer (PD) was synthesized and applied to encapsulate BFL. In the present study, we investigate the absorption property and mechanism of BFL in free form and BFL-peptide-dendrimer inclusion (BPDI) delivery system by using the Caco-2 cell monolayer model in vitro. The apparent permeability coefficient (Papp) values of BFL in free or BPDI form were over 1.0 × 10-6 cm/s. Meanwhile, their almost equal bi-directional transport and linear transport percentage with time and concentration course indicated that BFL in both forms was absorbed mainly through passive diffusion. The most important result is that the Papp values of BFL increased about three-fold more BPDI than those of its free form, which indicated the intestinal permeability of BFL could be improved while BFL was encapsulated in BPDI form. Therefore, PD encapsulation may be a potential delivery system to increase the bioavailability of BFL.
Keywords: Apparent permeability coefficient
Bufalin
Bufalin-peptide-dendrimer inclusion
Caco-2 cell monolayer
Intestinal permeability
Peptide-dendrimer
Publisher: Molecular Diversity Preservation International (MDPI)
Journal: Molecules 
ISSN: 1420-3049
DOI: 10.3390/molecules22122088
Rights: © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
The following publication Chan, C.-O.; Jing, J.; Xiao, W.; Tan, Z.; Lv, Q.; Yang, J.; Chen, S. Enhanced Intestinal Permeability of Bufalin by a Novel Bufalin-Peptide-Dendrimer Inclusion through Caco-2 Cell Monolayer. Molecules 2017, 22, 12, 2088,1-8 is available at https://dx.doi.org/10.3390/molecules22122088
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