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Acetylcholine Analog-Modified Albumin Nanoparticles for the Enhanced and Synchronous Brain Delivery of Saponin Components of Panax Notoginseng

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Abstract

Background

Panax notoginseng saponins (PNS) are commonly used first-line drugs for treating cerebral thrombosis and stroke in China. However, the synchronized and targeted delivery of active ingredients in traditional Chinese medicine (TCM) poses a significant challenge for modern TCM formulations.

Methods

Bovine serum albumin (BSA) was modified using 2-methacryloyloxyethyl phosphorylcholine (MPC), an analog of acetylcholine, and subsequently adsorbed the major PNS onto the modified albumin to produce MPC-BSA@PNS nanoparticles (NPs). This novel delivery system facilitated efficient and synchronized transport of PNS across the blood–brain barrier (BBB) through active transport mediated by nicotinic acetylcholine receptors.

Results

In vitro experiments demonstrated that the transport rates of R1, Rg1, Rb1, and Rd across the BBB were relatively synchronous in MPC-BSA@PNS NPs compared to those in the PNS solution. Additionally, animal experiments revealed that the brain-targeting efficiencies of R1 + Rg1 + Rb1 in MPC-BSA@PNS NPs were 2.02 and 7.73 times higher than those in BSA@PNS NPs and the free PNS group, respectively.

Conclusions

This study presents a simple and feasible approach for achieving the targeted delivery of complex active ingredient clusters in TCM.

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Funding

This work was supported by the National Natural Science Foundation of China (81760642; 82060645 and 82260698), the Key Natural Science Foundation of Yunnan Province (202101AT070099), the Yunnan Province Education Department Scientific Research Fund Project (grant NO.2023J0144), the Yunnan Fundamental Research Project (grant NO.202301AU070181).

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  1. Ying Yu and Li Yun Wang contributed equally to this work.

Authors and Affiliations

  1. School of Life Science and Technology, Kunming University of Science and Technology, Kunming, 650500, China

    Ying Yu, Li Yun Wang, Yan Chi Liu, Hao Cui, Cheng Yuan & Cheng Xiao Wang

  2. Key Laboratory of Sustainable Utilization of Panax Notoginseng Resources of Yunnan, Province, Kunming, 650500, China

    Ying Yu, Li Yun Wang, Yan Chi Liu, Hao Cui & Cheng Xiao Wang

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Yu, Y., Wang, L.Y., Liu, Y.C. et al. Acetylcholine Analog-Modified Albumin Nanoparticles for the Enhanced and Synchronous Brain Delivery of Saponin Components of Panax Notoginseng. Pharm Res 41, 513–529 (2024). https://doi.org/10.1007/s11095-024-03670-w

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