Microcapsules based on alginate and guar gum for co-delivery of hydrophobic antitumor bioactives

The main goal was the development of a polysaccharide microcapsule for anticancer application based on guar gum and sodium alginate for the controlled release of hesperidin and betulinic acid by spray drying technique. The microcapsule showed an Encapsulation Efficiency of 98.15 ± 0.34 % for hesperidin and 99.76 ± 0.22 % for betulinic acid. In the release study, the Korsmeyer-Peppas mathematical model was identified as the most adequate to explain the observed release mechanism. In vivo tests were performed in zebrafish model, revealing that the microcapsules did not alter the locomotor activity and were not toxic within 96 h by oral administration, suggesting their biological safety. In vitro cytotoxic activity against HL-60 cells confirmed an IC50 value of 2.52 ± 0.23 μg mL-1 in 72 h. Additionally, a decrease in the cytotoxic activity of betulinic acid against L-929 (non-tumor) cells was evidenced. Therefore, the microcapsules synthesized in this work represent a promising formulation for anticancer applications.