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Molecules 2017, 22(12), 2088; doi:10.3390/molecules22122088

Enhanced Intestinal Permeability of Bufalin by a Novel Bufalin-Peptide-Dendrimer Inclusion through Caco-2 Cell Monolayer

1
State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen 518057, China
2
School of Pharmacy, University of Queensland, Woolloongabba QLD 4072, Australia
3
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
4
Shenzhen Pharmacists Association, Shenzhen 518024, China
*
Author to whom correspondence should be addressed.
Received: 29 October 2017 / Revised: 17 November 2017 / Accepted: 23 November 2017 / Published: 29 November 2017
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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. View Full-Text
Keywords: bufalin; peptide-dendrimer; bufalin-peptide-dendrimer inclusion; Caco-2 cell monolayer; intestinal permeability; apparent permeability coefficient bufalin; peptide-dendrimer; bufalin-peptide-dendrimer inclusion; Caco-2 cell monolayer; intestinal permeability; apparent permeability coefficient
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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, 2088.

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