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Article

Bioactive Betulin and PEG Based Polyanhydrides for Use in Drug Delivery Systems

1
Department of Physical Chemistry and Technology of Polymers, Silesian University of Technology, M. Strzody 9, 44-100 Gliwice, Poland
2
Department of Organic Chemistry, Poznan University of Medical Science, Grunwaldzka 6, 60-780 Poznan, Poland
3
Department of Pharmacology, Poznan University of Medical Science, Rokietnicka 5a, 60-806 Poznan, Poland
4
Faculty of Chemical and Process Engineering, Warsaw University of Technology, Warynskiego 1, 00-645 Warsaw, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Catarina Pinto Reis
Int. J. Mol. Sci. 2021, 22(3), 1090; https://doi.org/10.3390/ijms22031090
Received: 31 December 2020 / Revised: 17 January 2021 / Accepted: 19 January 2021 / Published: 22 January 2021
(This article belongs to the Special Issue Therapeutic Polymers for Drug Delivery)
In the course of this study, a series of novel, biodegradable polyanhydrides based on betulin disuccinate and dicarboxylic derivatives of poly(ethylene glycol) were prepared by two-step polycondensation. These copolymers can be used as carriers in drug delivery systems, in the form of microspheres. Betulin and its derivatives exhibit a broad spectrum of biological activity, including cytotoxic activity, which makes them promising substances for use as therapeutic agents. Microspheres that were prepared from betulin based polyanhydrides show promising properties for use in application in drug delivery systems, including inhalation systems. The obtained copolymers release the active substance—betulin disuccinate—as a result of hydrolysis under physiological conditions. The use of a poly(ethylene glycol) derivative as a co-monomer increases the solubility and bioavailability of the obtained compounds. Microspheres with diameters in the range of 0.5–25 µm were prepared by emulsion solvent evaporation method and their physicochemical and aerodynamic properties were analyzed. The morphological characteristics of the microspheres depended on the presence of poly(ethylene glycol) (PEG) segment within the structure of polyanhydrides. The porosity of the particles depended on the amount and molecular weight of the PEG used and also on the speed of homogenization. The most porous particles were obtained from polyanhydrides containing 20% wt. of PEG 600 by using a homogenization speed of 18,000 rpm. View Full-Text
Keywords: betulin; polyanhydrides; biodegradable microspheres; cytostatic activity; drug delivery systems betulin; polyanhydrides; biodegradable microspheres; cytostatic activity; drug delivery systems
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MDPI and ACS Style

Niewolik, D.; Bednarczyk-Cwynar, B.; Ruszkowski, P.; Sosnowski, T.R.; Jaszcz, K. Bioactive Betulin and PEG Based Polyanhydrides for Use in Drug Delivery Systems. Int. J. Mol. Sci. 2021, 22, 1090. https://doi.org/10.3390/ijms22031090

AMA Style

Niewolik D, Bednarczyk-Cwynar B, Ruszkowski P, Sosnowski TR, Jaszcz K. Bioactive Betulin and PEG Based Polyanhydrides for Use in Drug Delivery Systems. International Journal of Molecular Sciences. 2021; 22(3):1090. https://doi.org/10.3390/ijms22031090

Chicago/Turabian Style

Niewolik, Daria, Barbara Bednarczyk-Cwynar, Piotr Ruszkowski, Tomasz R. Sosnowski, and Katarzyna Jaszcz. 2021. "Bioactive Betulin and PEG Based Polyanhydrides for Use in Drug Delivery Systems" International Journal of Molecular Sciences 22, no. 3: 1090. https://doi.org/10.3390/ijms22031090

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