Preparation of PEG-modified isoquercitrin liposomes and anti-chronic kidney disease research

作者：Qinyang Hua, Qilong Wang, Xue Wang, Xia Jiang, Mingjie Gong, Jiaying Li, Tingyuan Li, Xiaowen Wang, Xia Cao, Jiangnan Yu, Elmurat Toreniyazov, Bin Zong, Ximing Xu, Feng Shi, Michael Adu‐Frimpong · 发表于：Journal of Liposome Research · 年份：2025 · DOI：10.1080/08982104.2025.2480782 · 被引用次数：5 · 研究领域：Nanoparticle-Based Drug Delivery、Advanced Drug Delivery Systems、Infant Nutrition and Health

The clinical application of Isoquercitrin (IQ) is limited by its low water solubility and short retention time in the body, despite its diverse pharmacological effects. To address these issues, we prepared polyethylene glycol (PEG)-modified IQ liposomes (IQ-L) using the thin film dispersion method and optimized the formulation through a combination of One Factor at a Time (OFAT) method and response surface experiments. Characterization of the IQ-L that was prepared using the optimal formulation revealed a particle size of 185.48 nm, a polydispersity index of 0.252, a zeta potential of -33.88 mV, and an impressive encapsulation efficiency of 97.84%. In vitro release studies showed a significantly higher cumulative release rate for IQ-L compared to free IQ. Pharmacokinetic evaluations in rats demonstrated a 4.54-fold increase in the area under the concentration-time curve, a 1.63-fold prolongation of the half-life, and a 2.07-fold increase in peak concentration for IQ-L compared to unmodified IQ. Moreover, assessments of renal function in a mouse model indicated promising therapeutic effects. In summary, the PEG-modified liposome system greatly improved the solubility and in vivo retention time of IQ, thus making it a potential clinical agent for the treatment of chronic kidney disease (CKD).