Evolocumab loaded Bio-Liposomes for efficient atherosclerosis therapy

Author:

Li Zhenxian,Zhu Haimei,Liu Hao,Liu Dayue,Liu Jianhe,Jiang Jiazheng,Zhang Yi,Qin Zhang,Xu Yijia,Peng Yuan,Liu Bin,Long Yun

Abstract

AbstractPCSK9, which is closely related to atherosclerosis, is significantly expressed in vascular smooth muscle cells (VSMCs). Moreover, Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) mediated phenotypic transformation, abnormal proliferation, and migration of VSMCs play key roles in accelerating atherosclerosis. In this study, by utilizing the significant advantages of nano-materials, a biomimetic nanoliposome loading with Evolocumab (Evol), a PCSK9 inhibitor, was designed to alleviate atherosclerosis. In vitro results showed that (Lipo + M)@E NPs up-regulated the levels of α-SMA and Vimentin, while inhibiting the expression of OPN, which finally result in the inhibition of the phenotypic transition, excessive proliferation, and migration of VSMCs. In addition, the long circulation, excellent targeting, and accumulation performance of (Lipo + M)@E NPs significantly decreased the expression of PCSK9 in serum and VSMCs within the plaque of ApoE−/− mice.

Funder

Natural Science Foundation of Hunan Province

Key R&D Projects in Ningxia Hui Autonomous Region

Chinese medicine research Project of Hunan Province

Publisher

Springer Science and Business Media LLC

Subject

Pharmaceutical Science,Applied Microbiology and Biotechnology,Biomedical Engineering,Molecular Medicine,Medicine (miscellaneous),Bioengineering

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