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Development and Evaluation of Fucoidan-Based Liposomes: Targeting Smooth Muscle Cells for Atherosclerosis Treatment

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Abstract

Purpose

This study aims to develop effective fucoidan extracted from Undaria pinnatifida seaweed (FCU)-based liposomes for the treatment of atherosclerosis, with a specific focus on human aortic smooth muscle cells (hAoSMCs).

Methods

To develop active liposomes, our research began by investigating the pharmacological activity of FCU towards hAoSMCs before proceeding to the development of FCU-based liposomes using Ox-LDL uptake assessment and ELISA. After confirmation of the pharmaceutical activity of FCU, we designed and formulated two novel types of liposomes: FCU-coated liposomes (FCU-Lip) and sirolimus-loaded FCU-coated liposomes (FCU-Sir-Lip). The developed formulation was then characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). In vitro studies were conducted to evaluate the effects of FCU-Lip and FCU-Sir-Lip targeting SMCs for atherosclerotic treatment, focusing on SMC proliferation, foam cell formation, and the secretion of inflammatory cytokines by hAoSMCs.

Results

The results demonstrated the pharmacological activity of FCU towards hAoSMCs. The formulated FCU-Lip and FCU-Sir-Lip liposomes exhibited sizes of approximately 153.15 nm and 169.13 nm, respectively, with a polydispersity index (PDI) of around 0.15. The zeta potential of both FCU-Lip and FCU-Sir-Lip was approximately -20 mV. FCU-Sir-Lip showed sirolimus encapsulation efficiency of approximately 60%. In vitro studies further revealed the efficacy of FCU-Lip and FCU-Sir-Lip in suppressing hAoSMC proliferation, foam cell formation, and reducing inflammation.

Conclusion

This study demonstrates the therapeutic potential of FCU as an active pharmaceutical ingredient for treating atherosclerosis, specifically targeting hAoSMCs. Furthermore, the observed efficacy of FCU-based liposomes highlights their potential as novel therapeutic agents.

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Data Availability

All data generated or analyzed during this study are included in this article.

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Authors and Affiliations

  1. Cancer Center, Department of Pathology, People’s Hospital of Hangzhou Medical College: Zhejiang Provincial People’s Hospital, 310014, Hangzhou, Zhejiang, China

    Likai Han & Lili Yu

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  1. Likai Han
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  2. Lili Yu
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Correspondence to Lili Yu.

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Han, L., Yu, L. Development and Evaluation of Fucoidan-Based Liposomes: Targeting Smooth Muscle Cells for Atherosclerosis Treatment. J Pharm Innov 18, 2120–2130 (2023). https://doi.org/10.1007/s12247-023-09778-7

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