Construction of Renal-targeting Peptide-modified Ginsenoside Rg3 Nanomicelles and Their Regulatory Mechanism on Vascular Calcification and Blood Pressure Abnormalities in Dialysis Patients
LIN Guang-bin
ZHONG Lu-ping
LIN Wen-hong
XIE Hang-zhen
Abstract：Objective: To explore the interventional effects of renal-targeting peptide-modified ginsenoside Rg3 nanomicelle (GRg3@RT-PMs) on hypertension and vascular calcification in patients with long-term renal dialysis, and to elucidate its potential molecular mechanism, providing a new strategy for the precise treatment of dialysis complications. Methods: GRg3@RT-PMs were prepared using chitosan and ginsenoside Rg3 self-assembly technology modified with a renal-targeted peptide (G3-C12). Their particle size, encapsulation efficiency, and in vitro sustained-release characteristics were characterized. A high-phosphate-induced calcification model of human renal tubular epithelial cells (HK-2) was used to evaluate the targeting ability, biocompatibility, and inhibitory effect of GRg3@RT-PMs on calcification marker proteins (BMP-2, Runx2). A total of 18 dialysis patients were enrolled to assess the effects of oral administration of PMs, GRg3, and GRg3@RT-PMs on blood pressure and arterial calcification. Results: GRg3@RT-PMs had a particle size of (125.3±3.2) nm, an encapsulation efficiency of (89.7±2.3)%, and a cumulative release rate of (82.5±3.1)% over >48 h; GRg3@RT-PMs significantly inhibited the expression of BMP-2 and Runx2 in high-phosphate-induced HK-2 cells (P<0.01); In patients, the systolic blood pressure in the GRg3@RT-PMs group trended toward the normal range and was lower than that in the ginsenoside Rg3 and Rg3/β-CD complex groups, while diastolic blood pressure was more stable (P<0.05); The calcification score in the GRg3@RT-PMs group was lower than that in the Rg3 group after administration (P<0.01). Conclusion: GRg3@RT-PMs effectively alleviated dialysis-related vascular calcification and blood pressure abnormalities through the renal-targeted delivery, demonstrating a potential for clinical translation.
Keywords：ginsenoside Rg3(GRg3)renal-targeted deliverynanomicellesvascular calcificationblood pressure regulation
Publication Date：2025-03-31
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：7( 20-26 )