Research on an effective, accurate, and universally applicable method for dual-loaded liposomes encapsulation efficiency

IF 3.7 3区医学 Q2 CHEMISTRY, MEDICINAL

Journal of pharmaceutical sciences Pub Date : 2025-03-01 DOI:10.1016/j.xphs.2025.01.026

Tong Yuan , Yuqi Zhu , Yaqi Dai , Fulin Bi , Yan Lin , Jin Yang

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引用次数: 0

Abstract

Objective

Dual-loaded liposomes have become increasingly popular in the field of liposomal research. The encapsulation rate of dual-loaded drugs is an important indicator of the quality and efficacy of the dual-loaded liposomes. But it is difficult to determine the encapsulation efficiency of two drugs using a single method when the physicochemical properties of the drugs differ significantly. The aim of this study is to identify a method that is suitable for the different physicochemical properties of drugs and that efficiently and accurately determines the encapsulation efficiency of the two drugs in dual-loaded liposomes.

Methods

This study uses three different types of dual-loaded liposomes that simultaneously encapsulate lipophilic and hydrophilic drugs to examine the separation efficiency, encapsulation rate error, and applicability of various currently available methods for determining the encapsulation efficiency of dual-loaded liposomes. These methods include centrifugation, dialysis, ultrafiltration, microcolumn centrifugation, nanoparticle exclusion chromatography (nPEC), and polyethylene glycol-single-chain variable fragment (PEG-scFv) induced sedimentation.

Results

The results indicate that microcolumn centrifugation, nPEC, and PEG-scFv induced sedimentation methods achieved >90 % separation efficiency for both lipophilic and hydrophilic drugs. Among these, microcolumn centrifugation is cumbersome to operate, and the PEG-scFv induced sedimentation method is only applicable to PEGylated liposomes. In contrast, the nPEC method requires no pre-treatment and is suitable for the separation of all nanoparticles and free drugs.

Conclusions

This study concludes through a comparative analysis that the nPEC method is an effective, accurate, and universally applicable method for assessing the encapsulation efficiency of dual-loaded liposomes.

Abstract Image

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一种有效、准确、普遍适用的双载脂质体包封效率测定方法的研究。

目的：双负载脂质体在脂质体研究领域日益受到关注。双载药物的包封率是衡量双载脂质体质量和疗效的重要指标。但当两种药物的理化性质差异较大时，很难用单一方法测定其包封效率。本研究的目的是寻找一种适合不同药物理化性质的方法，高效准确地测定两种药物在双载脂质体中的包封效率。方法：本研究采用三种不同类型的双载脂质体同时包封亲脂性和亲水性药物，考察目前各种测定双载脂质体包封效率方法的分离效率、包封率误差和适用性。这些方法包括离心、透析、超滤、微柱离心、纳米颗粒排除色谱（nPEC）和聚乙二醇-单链可变片段（PEG-scFv）诱导沉淀。结果：微柱离心、nPEC和PEG-scFv诱导沉降法对亲脂性和亲水性药物的分离效率均在90%以上。其中，微柱离心操作繁琐，PEG-scFv诱导沉降法仅适用于聚乙二醇化脂质体。相比之下，nPEC方法不需要预处理，适用于所有纳米颗粒和游离药物的分离。结论：本研究通过对比分析得出nPEC法是一种有效、准确、普遍适用的双载脂质体包封效率评价方法。

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来源期刊

Journal of pharmaceutical sciences 医学-化学综合

CiteScore

7.30

自引率

13.20%

发文量

367

审稿时长

33 days

期刊介绍： The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.