Abstract
This paper describes the preparation and characterization of polymer-drug systems based on polymeric microspheres obtained from poly(betulin disuccinate-co-sebacic acid). The active compound that was coupled to the betulin-based carriers was rifampicin (RIF), an ansamycin drug used in the treatment of tuberculosis. Poly(betulin disuccinate-co-sebacic acid) microspheres were prepared using a solvent evaporation technique from copolymers obtained by polycondensation of betulin disuccinate (DBB) and sebacic acid (SEB). The content of sebacic acid in the copolymers was 20, 40, 60 and 80 wt%, respectively. Small and large rifampicin-loaded microspheres were obtained for each of the copolymers. The initial amount of drug was 10, 30 or 50 wt%, based on the weight of the polymer. Particles obtained in this study were round in shape with diameter in the range of 2–21 μm and of orange to red colour originating from rifampicin. The RIF encapsulation efficacy varied from 7% to 33%. Drug loading varied from 2% to 13% and increased at a higher RIF ratio. The highest degree of drug loading was observed for large particles, in which the initial amount of drug (at the particle preparation stage) was 50 wt%. Microspheres prepared from betulin-based polyanhydrides may have significant applications in drug delivery systems. The concentration of loaded drug was enough to obtain bactericidal effects against reference S. Aureus ATCC 25923 bacteria.
Highlights
Betulin, a pentacyclic triterpene, is a natural compound found in the outer layer of birch bark
A series of polyanhydrides were obtained by melt polycondensation of betulin disuccinate (DBB) and sebacic acid (SA) with the use of acetic anhydride
In the course of this study, new biodegradable polyanhydrides composed of betulin disuccinate and sebacic acid were obtained and used to formulate small and large microspheres using the emulsion solvent evaporation method
Summary
A pentacyclic triterpene, is a natural compound found in the outer layer of birch bark. Polymers derived from natural monomers (e.g., lactic acid, furans or terpenes) have become more desirable because they can replace petroleum-based raw materials [1]. Polymers obtained from renewable raw materials are in demand in many industries, including pharmaceuticals. Just like other natural triterpenes, exhibits a broad spectrum of biological activity [2,3]. The biological activity of betulin is well documented, and has been proven to be effective in both oncological [4] and bacterial [5] lung diseases. Betulin exhibits synergistic effects with other biologically active compounds, such as acyclovir (against herpes simplex viruses) [6], gamma-cyclodextrin derivatives (reduction of the cell proliferation and induced differentiation and cell death in melanoma B164A5 cells) [7] and Pharmaceutics 2022, 14, 579.
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