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Spherical Amorphous Nanoparticles from Birch Bark Triterpenoids: Study of the Conditions for the Formation

https://doi.org/10.32362/2410-6593-2019-14-3-33-41

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Abstract

Triterpenoids from birch bark are valuable biologically active substances. They exhibit important biological properties. However, triterpenoids are insoluble in water due to their hydrophobicity. In order to increase their bioavailability we developed a technique for obtaining spherical amorphous nanoparticles (SANP) by their precipitation with water from a solution in THF. In the form of nanoparticles, triterpenoids show additional useful properties: they can be loaded with hydrophobic substances. SANP were also shown to be effective immunological adjuvants. This article is devoted to the study of conditions that could optimize their production. As a result, it was shown that among the three investigated solvents miscible with water - acetone, dioxane, THF -the latter gives the best results. Lowering temperature decreases the size of SANP. An increased temperature leads to the formation of betulin crystals. When the concentration of triterpenoids in THF is higher than 5 mg/ml, crystals of betulin also begin to form. The results of this study lead to the assumption that the main parameter of the process determining the formation of SANP is the rate of the solvent diffusion into water.

About the Authors

A. N. Bastrich
MIREA - Russian Technological University (M.V. Lomonosov Institute of Fine Chemical Technologies)
Russian Federation

Asya N. Bastrich - Master of Engineering and Technology, M.V. Lomonosov Institute of Fine Chemical Technologies.

86, Vernadskogo pr., Moscow, 119571



A. E. Stepanov
MIREA - Russian Technological University (M.V. Lomonosov Institute of Fine Chemical Technologies)
Russian Federation

Alexander E. Stepanov - D.Sc. (Chemistry), Professor, Professor of the Chair of General Chemical Technology, M.V. Lomonosov Institute of Fine Chemical Technologies.

86, Vernadskogo pr., Moscow, 119571



N. N. Lonina
MIREA - Russian Technological University (M.V. Lomonosov Institute of Fine Chemical Technologies)
Russian Federation

Natalya N. Lonina - Ph.D. (Chemistry), Docent, Associate Professor of the N.A. Preobrazhensky Chair of Chemical Technology of Biologically Active Compounds, Medicinal and Organic Chemistry.

86, Vernadskogo pr., Moscow, 119571


V. I. Popenko
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences
Russian Federation

Vladimir I. Popenko - D.Sc. (Biology), Senior Scientist of the Laboratory of Cellular Basics of Malignant Disease Development.

32, Vavilova st., Moscow, 119991



A. P. Kaplun
MIREA - Russian Technological University (M.V. Lomonosov Institute of Fine Chemical Technologies)
Russian Federation

Alexander P. Kaplun - D.Sc. (Chemistry), Professor, Professor of the Chair of Biotechnology and Industrial Pharmacy, M.V. Lomonosov Institute of Fine Chemical Technologies.

86, Vernadskogo pr., Moscow, 119571


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Supplementary files

1. Fig. 4. The electron micrograph of the dispersion of birch bark dry extract after heating the spherical amorphous nanoparticles within 1h at 100 °C.
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Type Research Instrument
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Bastrich A.N., Stepanov A.E., Lonina N.N., Popenko V.I., Kaplun A.P. Spherical Amorphous Nanoparticles from Birch Bark Triterpenoids: Study of the Conditions for the Formation. Fine Chemical Technologies. 2019;14(3):33-41. (In Russ.) https://doi.org/10.32362/2410-6593-2019-14-3-33-41

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ISSN 2410-6593 (Print)
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