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.
Highlights
Toad venom is the dried secretion from the posterior auricular glands or skin glands of Bufobufogargarizans Cantor or Bufomelanostictus Schneider [1]
Bufalin (BFL), (BFL), the the dominant dominant bioactive bioactive component component in in toad toad venom, venom, has has been been demonstrated demonstrated to to Bufalin possess a variety of potential pharmacological effects
bufalin-peptide-dendrimer inclusion (BPDI) could increase the intestinal permeability of BFL across Caco-2 monolayer, peptide dendrimer (PD) may be a potential delivery system of water-insoluble drugs such as BFL
Summary
Toad venom is the dried secretion from the posterior auricular glands or skin glands of Bufobufogargarizans Cantor or Bufomelanostictus Schneider [1]. Due to the highly hydrophobic structure, BFL is a poorly water-soluble drug and with low bioavailability, which limits its application in clinic [5]. Them,a have been developed and applied for delivery of poorly water-soluble drugs [5]. Asymmetric peptide dendrimer (PD) has attracted attention and has been applied for drug due to due its more in terms more attention and hasmore been properly more properly applied fordelivery drug delivery to itsadvantages more advantages in of excellent biocompatibility, low cytotoxicity, and protease-hydrolysis resistance while compared terms of excellent biocompatibility, low cytotoxicity, and protease-hydrolysis resistance while to the low to generation commercial. The poorly highly branched with three-dimensional space and provides many hydrophobic cavities. With respect to the enhancing effects of PD on the bioavailability of small there have been handful reports.
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