Loading of amphipathic weak acids into liposomes in response to transmembrane calcium acetate gradients.
Open accessAbstract
We describe a novel procedure to load amphipathic weak acid molecules into preformed liposomes. Differences in calcium acetate concentrations across the liposomal membrane induce an increase of the internal pH. This pH imbalance serves as an efficient driving force to load and accumulate weak acids (5(6)-carboxyfluorescein and nalidixic acid) inside the lipid vesicles. The mechanism of loading and the relevance of the method in drug delivery systems are discussed.
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A transmembrane calcium acetate gradient is most suitable for loading amphipathic weak acids.
“Overall, from our own experience, we concluded that a transmembrane ammonium sulfate gradient is most suitable for stable encapsulation of amphipathic weak bases [16]–[19], [25], [26], while a transmembrane calcium acetate gradient is most suitable for loading amphipathic weak acids [16], [27], [28].”
From Fabrication Principles and Their Contribution to the Superior In Vivo Therapeutic Efficacy of Nano-Liposomes Remote Loaded with Glucocorticoids (2011) · cites this paper as [28]
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References 22 · Cited by 145
Research works printed but not linked: 2
- Barenholz, Y. and Amselem, S. (1993) in Liposome Technology, 2nd Edn., Vol. I (Gregoriadis, G., ed.), pp. 527-616, CRC Press, Boca Raton.
- Weinstein, J.N., Ralston, E., Leserman, L.D., Klausner, R.D., Drag- sten, P,, Henkart, P. and Blumenthal, R. (1984) in Liposome Tech- nology, Vol. III (Gregoriadis, G., ed.), pp. 183-204, CRC Press, Boca Raton.
- Authors
- Clerc, S., & Barenholz, Y.
- Affiliations
- Hebrew University of Jerusalem (IL)
- Corresponding author
- Clerc, Stéphane
- ORCID
- Barenholz, Yechezkel
- Venue
- Biochimica et Biophysica Acta (BBA) - Biomembranes
- Publisher
- Elsevier BV
- Published
- 1995-12
- Volume
- 1240
- Issue
- 2
- Pages
- 257-265
- ISSN
- 0005-2736 (ISSN-L)
- OpenAlex
- W2025492041
- Cited by
- 145
- References
- 22
- Citations by year
- 2026: 1 · 2025: 7 · 2024: 3 · 2023: 4 · 2022: 9 · 2021: 5 · 2020: 8 · 2019: 9 · 2018: 14 · 2017: 2 · 2016: 11 · 2015: 6 · 2014: 13 · 2013: 7 · 2012: 7
- FWCI
- 1.74
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Biochimica et Biophysica Acta (BBA) - Biomembranes (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Lipid Membrane Structure and Behavior
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- transmembrane pH gradient, internal pH, 5(6)-carboxyfluorescein, nalidixic acid, drug delivery, lipid vesicles
- MeSH terms
- Acetates, Acids, Fluoresceins, Hydrogen-Ion Concentration, Liposomes, Nalidixic Acid, Acetic Acid
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