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A Multiscale Study on the Effect of Sodium Cholate on the Deformation Ability of Elastic Liposomes

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Abstract

Elastic liposoxy1mes (ELs) are biocompatible bilayer vesicular systems commonly used in the transdermal delivery of drugs. Compared with conventional liposomes (CLs), the strong deformation ability conferred by edge activators (EAs) is one of the most critical properties of ELs. However, due to limited research methods, little is known about the effect of EAs on the deformation abilities of vesicles. In this study, taking sodium cholate as an example, a multiscale study was carried to study the effect of EAs on the deformability of ELs, including in vitro diffusion experiment at macroscale, “vesicle-pore” model experiment at the microscale and flat patch model experiment at the molecular scale. As a result, it was found that sodium cholate could decrease the kc of DPPC bilayer, which enabled it to remain morphologically intact during a strong deformation process. Such kind of differences on deformation ability made pogostone ELs (contain sodium cholate) present a better permeation effect compared with that of pogostone CLs. All of these provide a multiscale and thorough understanding of the effect of sodium cholate on the deformation ability of ELs.

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Acknowledgments

The content is solely the responsibility of the authors and does not necessarily represent the official views of the Beijing Natural Science Foundation. All simulations were performed at the National Supercomputer Center in Guangzhou.

Funding

This work was financially supported by the Beijing Natural Science Foundation (7162122).

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Authors and Affiliations

  1. Department of Traditional Chinese Medicine, Beijing University of Chinese Medicine, No. 11 of North 3rd Ring East Road, Chaoyang District, 6, Beijing, 100029, China

    Zhimin Wu, Chang Yang, Liping Chen, Lina Ma, Xiaowen Wu, Xingxing Dai, Yanjiang Qiao & Xinyuan Shi

  2. Key Laboratory of TCM-Information Engineering of State Administration of TCM, No. 11 of 8 North 3rd Ring East Road, Chaoyang District, Beijing, 100029, China

    Zhimin Wu, Lina Ma, Xingxing Dai, Yanjiang Qiao & Xinyuan Shi

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  1. Zhimin Wu
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Correspondence to Yanjiang Qiao or Xinyuan Shi.

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Wu, Z., Yang, C., Chen, L. et al. A Multiscale Study on the Effect of Sodium Cholate on the Deformation Ability of Elastic Liposomes. AAPS PharmSciTech 20, 311 (2019). https://doi.org/10.1208/s12249-019-1485-x

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