Abstract
We describe the dynamics of lipoic acid (LA) alone, incorporated in liposomes and as a part of nanoemulsions. Mass spectrometry shows that LA in water forms aggregates of two or three molecules in the form of a negatively charged ion and a neutral molecule. Phosphatidylcholine (PC)-based nanoforms of LA as liposomes and nanoemulsions with a particle size equal to 145 nm are characterized by a high degree of incorporation of LA into the nanoparticles and long-term stability during storage at room temperature. Dynamic light scattering (DLS) gives the polydispersity index of the nanoforms (> 0.3), characterizing the homogeneity of the obtained nanodispersions. We found that such emulsions can significantly (5 ×) increase the concentration of LA in the aqueous phase (5–7 mg/mL) when compared with an aqueous solution of LA (1 mg/mL) and by 40% when compared with PC liposomes (4 mg/mL). Moreover, the inclusion of LA in liposomes and nanoemulsions from PC did not change the neutral ζ-potential characteristic of PC nanoforms. CryoTEM established that the structural organization of the liposomes practically did not differ from nanoemulsions and both nanoforms contained both multilayer and single-layer vesicles. When studying the release kinetics of LA from phosphatidylcholine nanoforms, we found that at 22 h, 45–55% of LA was released from nanoparticles, but that at the initial stage of the process LA was slowly released from the nanoemulsions and rapidly from the liposomes. Conductance measurements indicate that LA delivered in all the three forms increase membrane permeability, though this result is most marked with the LA in PC liposomes.
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22 September 2021
A Correction to this paper has been published: https://doi.org/10.1007/s00249-021-01571-z
Abbreviations
- PC:
-
Phosphatidylcholine
- LA:
-
Lipoic acid
- PC–LA liposomes:
-
LA-containing PC liposomes
- PC–LA nanoemulsions:
-
LA-containing PC nanoemulsions
- PBS:
-
Phosphate buffered saline
- cryoTEM:
-
Transmission electron cryomicroscopy
- PDI:
-
Polydispersity index
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Acknowledgements
This research was supported by the "Russian Academic Excellence Project 5–100". The authors of this article express their gratitude to Dr. Andrey V. Symon, head of the representative office of Lipoid AG in Moscow.
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All the authors contributed to the study conception and design. Material preparation, data collection and analysis were performed by [VAS], [SOA], [NYL], [OAB], [AVC] and [NSS]. Conceptualization: [EAK]; methodology: [AAA]; writing—original draft preparation: [RAK]; writing—review and editing: [RGV]; supervision: [YS]. The first draft of the manuscript was written by [AAS] and all authors commented on previous versions of the manuscript. All authors read and approved the final manuscript.
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Shchelkonogov, V.A., Alyaseva, S.O., Lotosh, N.Y. et al. Lipoic acid nanoforms based on phosphatidylcholine: production and characteristics. Eur Biophys J 49, 95–103 (2020). https://doi.org/10.1007/s00249-019-01415-x
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DOI: https://doi.org/10.1007/s00249-019-01415-x