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

Niewolik, Daria; Bednarczyk–Cwynar, Barbara; Ruszkowski, Piotr; Sosnowski, Tomasz R.; Jaszcz, Katarzyna

doi:10.3390/ijms22031090

Cited by 12 publications

(25 citation statements)

References 44 publications

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“…Betulin is a pentacyclic triterpene. Pentacyclic triterpenoids (including pentacyclic triterpenes such as betulin) are of interest to researchers due to their anti-inflammatory, antimicrobial, antitumor, cytotoxic, and other activities [ 14 , 15 , 18 , 25 , 27 , 28 , 29 , 30 , 36 , 37 , 38 , 39 ], and their possible use as intermediates in the synthesis of new pharmacological substances.…”

Section: Discussionmentioning

confidence: 99%

“…However, betulin and its derivatives have a broad spectrum of biological relevance, thus they have a high potential for application in transdermal systems [ 19 , 20 ]. To date, several formulations containing betulin and its derivatives have been developed [ 21 , 22 , 23 , 24 , 25 ]. However, there are no literature reports describing the penetration of vehicles containing these compounds through the skin.…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives

et al. 2021

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This study investigated the antioxidant activity DPPH, ABTS, and Folin–Ciocalteu methods of betulin (compound 1) and its derivatives (compounds 2–11). Skin permeability and accumulation associated with compounds 1 and 8 were also examined. Identification of the obtained products (compound 2–11) and betulin isolated from plant material was based on the analysis of 1H- NMR and 13C-NMR spectra. The partition coefficient was calculated to determine the lipophilicity of all compounds. In the next stage, the penetration through pig skin and its accumulation in the skin were evaluated of ethanol vehicles containing compound 8 (at a concentration of 0.226 mmol/dm3), which was characterized by the highest antioxidant activity. For comparison, penetration studies of betulin itself were also carried out. Poor solubility and the bioavailability of pure compounds are major constraints in combination therapy. However, we observed that the ethanol vehicle was an enhancer of skin permeation for both the initial betulin and compound 8. The betulin 8 derivative showed increased permeability through biological membranes compared to the parent betulin. The paper presents the transformation of polycyclic compounds to produce novel derivatives with marked antioxidant activities and as valuable intermediates for the pharmaceutical industry. Moreover, the compounds contained in the vehicles, due to their mechanism of action, can have a beneficial effect on the balance between oxidants and antioxidants in the body, minimizing the effects of oxidative stress. The results of this work may contribute to knowledge regarding vehicles with antioxidant potential. The use of vehicles for this type of research is therefore justified.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives

et al. 2021

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“…Polyanhydrides were obtained by polycondensation of betulin disuccinate and sebacic acid (SA) according to the procedure described earlier [ 24 , 25 , 26 ]. Betulin disuccinate and sebacic acid were mixed in defined ratios ( Table 1 ) and refluxed in acetic anhydride (1:10, w / v ) under nitrogen flow for 40 min, forming prepolymers.…”

Section: Methodsmentioning

confidence: 99%

“…CPP-SA has been approved by the FDA for use in medicine in delivering carmustine for the treatment of brain cancer [ 23 ]. In our previous publications, we described the synthesis and characterization of polyanhydrides based on betulin disuccinate and other diacid comonomers that exhibited anticancer activity [ 24 , 25 , 26 ]. These polymers release DBB as a result of hydrolytic degradation in their physiological condition; thus, they can be used as a polymeric prodrug.…”

Section: Introductionmentioning

confidence: 99%

Biodegradable and Bioactive Carriers Based on Poly(betulin disuccinate-co-sebacic Acid) for Rifampicin Delivery

et al. 2022

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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.

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“…In most cases, the optimum in-organic particle filler could be identified by testing which of these produced the highest wear resistance. Another important aspect when investigating new materials is their toxicity to the environment, this includes both the materials themselves and their degradation products [ 16 , 17 ].…”

Section: Introductionmentioning

confidence: 99%

Determination of Mechanical and Tribological Properties of Silicone-Based Composites Filled with Manganese Waste

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Woźniak

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et al. 2021

Materials

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High-tonnage industrial processes generate high amount of waste. This is a growing problem in the whole world. Neutralizing such waste can be time consuming and costly. One of the possibilities of their reuse is to use them as fillers in polymer composites. Introduction of the filler in polymer matrix causes change in its mechanical and tribological properties. In the article, the effect of introducing fillers from post-production waste, and its effect on changing the physical properties of silicone-based composites filled with manganese (II) oxide and waste manganese residue was investigated. The composites were made by gravity casting. Composites with 2.5, 5, 7.5, and 10 wt% of the fillers were examined. The composite materials were subjected to tests such as: density, hardness, resilience, tensile test, abrasion resistance, and ball-on-disc. Microscopic images showed that, the particles of the fillers are uniformly distributed in silicone matrix with the formation of smaller agglomerates. Such agglomerates introduced a discontinuity in the structure of the polymer material, which caused a decrease in the tensile strength and elongation at break for all tested compositions in comparison with the mechanical properties of the silicone used as the matrix. However, it was found that all silicone-based composites filled with manganese (II) oxide and manganese residue showed a reduction in abrasive wear, compared to the reference sample.

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

Cited by 12 publications

References 44 publications

Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives

Enhancement of the Antioxidant and Skin Permeation Properties of Betulin and Its Derivatives

Biodegradable and Bioactive Carriers Based on Poly(betulin disuccinate-co-sebacic Acid) for Rifampicin Delivery

Determination of Mechanical and Tribological Properties of Silicone-Based Composites Filled with Manganese Waste

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