Cheng Joan, Kandimalla Karunya K
Department of Pharmaceutics and Brain Barriers Research Center, College of Pharmacy, University of Minnesota, Minneapolis, MN, USA.
Methods Mol Biol. 2025;2965:367-376. doi: 10.1007/978-1-0716-4742-4_18.
First discovered in 1984, bicelles have been traditionally used for the structural characterization of membrane-associated proteins through nuclear magnetic resonance (NMR). However, interest has been growing over the past decade in their application to drug delivery. Discoidal particles, such as bicelles, have demonstrated a higher degree of cellular uptake in both in vitro and in vivo models compared to spherical particles, such as lipid nanoparticles. Favorable electrostatic interactions allow the cationic bicelles to efficiently load nucleic acids, including siRNA, for drug delivery and to readily dock onto the anionic cell surface for internalization via adsorptive endocytosis. In this chapter, we provide a detailed description of the formulation methods, an overview of the techniques that are employed for the characterization of the siRNA-bicelle complexes, and approaches to optimizing their cellular uptake.
双分子层囊泡于1984年首次被发现，传统上用于通过核磁共振（NMR）对膜相关蛋白进行结构表征。然而，在过去十年中，它们在药物递送方面的应用受到的关注越来越多。与脂质纳米颗粒等球形颗粒相比，盘状颗粒（如双分子层囊泡）在体外和体内模型中均表现出更高程度的细胞摄取。有利的静电相互作用使阳离子双分子层囊泡能够有效地负载包括小干扰RNA（siRNA）在内的核酸用于药物递送，并易于停靠在阴离子细胞表面，通过吸附性胞吞作用实现内化。在本章中，我们详细描述了制备方法，概述了用于表征siRNA-双分子层囊泡复合物的技术，以及优化其细胞摄取的方法。
