Enhancing the Biopharmacological Characteristics of Asperosaponin VI: Unveiling Dynamic Self-Assembly Phase Transitions in the Gastrointestinal Environment

• DOI: 10.2147/ijn.s436372
• Publication Date: 2023-12-06T03:15:05Z
• Authors: Yulin Mo; Yanjun Yang; Jingqi Zeng; Weikun Ma; Yuxin Guan; Jingxi Guo; Xiaochun Wu; Dingkun Liu; Liang Feng; Xiaobin Jia; Bing Yang
• Keywords: dynamic self-assembled structure; Medicine (General); gastrointestinal environment; R5-920; oral bioavailability; International Journal of Nanomedicine; asperosaponin vi; biopharmacological characteristics; Original Research

Purpose: Asperosaponin VI (ASP VI) as an active ingredient of Dipsacus asperoides , which has a wide range biological and pharmacological activity. However, its development application are restricted due to the poor gastrointestinal permeability oral bioavailability. This investigation aims reveal influence self-assembled structure by interaction between ASP endogenous components NaTC and/or DOPC in environment on biopharmaceutical properties, novelty elucidated molecular mechanism for formation nanomicelles. Methods: change phase state fluids is characterized dynamic light scattering (DLS) transmission electron microscope (TEM). UPLC-Q-TOF-MS was used analyze composition exposure nanomicelles vivo. Molecular dynamics simulation (MDS) applied preliminarily elucidate self-assembly environment. Furthermore, theS8 promoting absorption were investigated through vivo pharmacokinetic experiments, parallel artificial membrane assay (PAMPA), quadruple single-pass intestinal perfusion rats, Caco-2 cell monolayer model. Results: We demonstrated that could spontaneously form structures with sodium taurocholate (NaTC) dipalmitoyl phosphatidylcholine (DOPC) during solubilization, promoted increased vivo, thus improving biopharmacological characteristics VI. Moreover, VI-NaTC-DOPC-self-assembled nanostructures VI-NaTC-DOPC-SAN) manifested higher cellular uptake cells evidenced flow cytometry confocal microscopy, this study also revealed driven electrostatic hydrogen bonding interactions. Conclusion: provides evidence transition may play key role insoluble or low ingredients dissolution Chinese medicines. Keywords: VI, structure, environment, characteristics, bioavailability