Fluorescence Analysis Method for Determining the Encapsulation Rate of PEGylated Liposomes and Their Pharmacokinetics
10.11969/j.issn.1673-548X.2025.07.010
- VernacularTitle:荧光分析法测定聚乙二醇化脂质体的包封率及其药动学研究
- Author:
Jian-quan PAN
1
;
Xue ZHANG
;
Cheng ZHANG
Author Information
1. 230012 合肥,安徽中医药大学药学院
- Publication Type:Journal Article
- Keywords:
Accelerated blood clearance phenomenon;
PEGylated liposomes;
Fluorescence method
- From:
Journal of Medical Research
2025;54(7):47-53,5
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the feasibility of fluorescence analysis method for determining the encapsulation efficiency(EE)of PEGylated liposomes(PEG-L)and their application in studying the accelerated blood clearance(ABC)phenomenon.Meth-ods DiR-labeled PEGylated liposomes(PEG-DiR-L)were prepared via ethanol injection.Free DiR and total DiR samples were ob-tained using ultrafiltration centrifugation and ultrasonic demulsification,respectively.The EE of PEG-DiR-L was calculated by quantif-ying DiR levels in both samples using a multifunctional microplate reader.Male Sprague-Dawley(SD)rats were divided into two groups:the single injection group[first injected with phosphate-buffered saline(PBS),followed by PEG-DiR-L 7days later]and the repeated injection group(first injected with empty PEG-L,followed by PEG-DiR-L 7days later).Blood samples were collected from the eye canthus of rats,and the plasma concentrations of PEG-DiR-L were measured to construct pharmacokinetic profiles and calculate key pharmacokinetic parameters.Tissue distribution was assessed by ex vivo imaging of heart,liver,spleen,lung,and kidney samples u-sing the IVIS spectroscopy.Results The EE of PEG-DiR-L determined by ultrafiltration centrifugation was 97.68％±0.23％.Com-pared to the single-dose group,the repeated-dose group exhibited significantly accelerated plasma clearance,with reduced AUC(0→t)、AUC(0→∞)、MRT(0→t)、MRT(0→∞)and t1/2z,alongside increased CLz and Vz(P＜0.05).Hepatic accumulation of PEG-DiR-L was markedly enhanced in the repeated-dose group.Conclusion The results of plasma pharmacokinetics and tissue distribution indicated that the ABC phenomenon occurred in the repeated injection group,suggesting that the fluorescence analysis method is able to determine the encapsulation rate of PEG-L and be used to study the ABC phenomenon.
