Efficient Drug Loading Method for Poorly Water-Soluble Drug into Bicelles through Passive Diffusion

模型脂质双层 化学 聚乙二醇 胶束 聚乙二醇化 PEG比率 脂质双层 色谱法 化学工程 生物物理学 有机化学 生物化学 水溶液 脂质双层相行为 财务 工程类 经济 生物
作者
Yuta Arai,Yasunori Iwao,Yoshio Muguruma,Katsuhiko Yamamoto,Yukihiro Ikeda
出处
期刊:Molecular Pharmaceutics [American Chemical Society]
卷期号:20 (11): 5701-5713
标识
DOI:10.1021/acs.molpharmaceut.3c00562
摘要

The bicelle, a type of solid lipid nanoparticle, comprises phospholipids with varying alkyl chain lengths and possesses the ability to solubilize poorly water-soluble drugs. Bicelle preparation is complicated and time-consuming because conventional drug-loading methods in bicelles require multiple rounds of thermal cycling or co-grinding with drugs and lipids. In this study, we proposed a simple drug-loading method for bicelles that utilizes passive diffusion. Drug-unloaded bicelles were placed inside a dialysis device and incubated in a saturated solution of ketoconazole (KTZ), which is a model drug. KTZ was successfully loaded into bare bicelles over time with morphological changes, and the final encapsulated concentration was dependent on the lipid concentration of the bicelles. When polyethylene glycol (PEG) chains of two different lengths (PEG2K and 5K) were incorporated into bicelles, PEG2k and PEG5k bicelles mitigated the morphological changes and improved the encapsulation rate. This mitigation of morphological changes enhanced the encapsulated drug concentration. Specifically, PEG5k bicelles, which exhibited the greatest prevention of morphological changes, had a lower encapsulated concentration after 24 h than that of PEG2k bicelles, indicating that PEGylation with a longer PEG chain length improved the loading capacity but decreased the encapsulation rate owing to the presence of a hydration layer of PEG. Thus, PEG with a certain length is more suitable for passive loading. Moreover, loading factors, such as temperature and vehicles used in the encapsulation process, affected the encapsulation rate of the drug. Taken together, the passive loading method offers high throughput with minimal resources, making it a potentially valuable approach during early drug development phases.
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