ABSTRACT
Dasatinib (DAS), a potent anticancer drug, has been subjected to formulation enhancements due to challenges such as significant first-pass metabolism, poor absorption, and limited oral bioavailability. To improve its release profile, DAS was embedded in a matrix of the hydrophilic polymer polyvinylpyrrolidone (PVP). Drug amorphization was induced in a planetary ball mill by solvent-free co-grinding, facilitating mechanochemical activation. This process resulted in the formation of amorphous solid dispersions (ASDs). The ASD capsules exhibited a notable enhancement in the release rate of DAS compared to capsules containing the initial drug. Given that anticancer drugs often undergo limited metabolism in the body with unchanged excretion, the ecotoxicological effect of the native form of DAS was investigated as well, considering its potential accumulation in the environment. The highest ecotoxicological effect was observed on the bacteria Vibrio fischeri, while other test organisms (bacteria Pseudomonas putida, microalgae Chlorella sp., and duckweed Lemna minor) exhibited negligible effects. The enhanced drug release not only contributes to improved oral absorption but also has the potential to reduce the proportion of DAS that enters the environment through human excretion. This comprehensive approach highlights the significance of integrating advances in drug development while considering its environmental implications.
ABSTRACT
Research background: Due to numerous health-promoting properties, dandelion has been used in traditional medicine as a herbal remedy, but also as a food product. Dandelion health benefits are ascribed to the presence of different bioactive compounds in its tissues, among which polyphenols play a significant role. However, the low stability of polyphenols is a critical parameter for their successful implementation into products. Thus, their encapsulation using appropriate carrier vehicles is highlighted as an effective technique for their stabilization and protection. The aim of this study is to microencapsulate dandelion leaf extract using spray drying and different carrier materials for the first time. Experimental approach: In spray drying, low inlet temperature of 130 °C was employed to preserve sensitive dandelion polyphenols, while guar gum, gum arabic, inulin, maltodextrin, pectin and alginate were used as carriers. The influence of different carriers and their content on physicochemical, morphological and colour properties, polyphenolic content and encapsulation efficiency of polyphenols in dandelion powders was examined. Specific polyphenols were determined using HPLC-PAD analysis. Their release profiles and antioxidant capacity in simulated gastrointestinal conditions were also evaluated. Results and conclusions: Compared to plain dandelion powder, carrier-containing dandelion powders have favourably increased solubility, enhanced flow and cohesive properties, reduced particle size and prolonged release of polyphenols under simulated gastrointestinal conditions. Powders were characterized by low moisture content (~2-8%) and high solubility (~92-97%). Chicoric acid was the most abundant compound in dandelion powders. Pectin-dandelion powder showed to be the most effective for microencapsulation of polyphenols, especially for chicoric acid entrapment (74.4%). Alginate-dandelion powder enabled the slowest gradual release of polyphenols. Novelty and scientific contribution: Spray drying at 130 °C and the applied carriers proved to be effective for microencapsulation of dandelion extract, where polyphenolic-rich dandelion powders, due to good physicochemical and encapsulation properties, could serve for the enrichment/production of different functional food products. Also, due to the lack of data on dandelion encapsulation, the obtained results could be of great interest for researchers in the encapsulation field, but also for food industry, especially in the field of instant powders.
