Abstract
Background: Degradable polymeric particles derived from phenolic compounds are promising materials for biomedical applications due to their inherently antioxidant, antimicrobial, and anticancerogenic properties. We revise all the patent regarding to the biomedical and food additive formulations of Rutin (RT) and Quercetin (QC) as phenolic compounds.
Objective: Prepare degradable Poly(Rutin) (p(RT)) and Poly(Quercetin) (p(QC)) particles from natural phenolic compounds, Rutin (RT) and Quercetin (QC).
Method: P(RT), and p(QC) particles were prepared using microemulsion crosslinking method employing phenolic compounds such as RT and QC as monomer and poly(ethylene glycol) diglycidyl ether (PEGGE) as a crosslinker in a single step. The degradability of these particles was investigated at physiological conditions, pH 5.4, 7.4, and 9 at 37.5°C. The antioxidant capacity of RT, QC and their corresponding particles was determined by means of total phenol content and ABTS+ scavenging assay. The blood compatibility of the particles is determined with hemolysis and blood clotting tests, and the cytotoxicity of the particles on L929 fibroblast cell and A549 cancer cells was done by WST-1 tests.
Results: The size of the prepared phenolic particles was in the size range of 0.4 - 4 µm with negative zeta potentials, -20.29±1.7 and -31.31±2.0 mV for p(RT) and p(QC) particles, respectively. The highest amount of degradation was obtained for p(QC) particles in almost a linear profile with relatively longer time degrading kinetics at pH 9, e.g., 197±23 mg/g QC was released up to 130 h. The antioxidant capacities of phenolic compounds were decreased about ten-fold upon the particle formations of the phenolic compound, and the antioxidant capacity of p(QC) particles was found to be better than p(RT) particles with 0.22±0.01 and 0.05±0.001 µmol trolox equivalent g-1, respectively. The blood compatibility test of p(RT) and p(QC) particles revealed that both particles are blood compatible up to 1 mg/mL concentration and possess clotting of blood over 1 mg/mL concentrations. Furthermore, the cytotoxicity tests showed that p(RT) particles are more biocompatible than p(QC) on the fibroblast cell as 91% cell viability versus 50% for p(QC) was observed at 75 µg/mL particle concentrations. Additionally, at this concentration 42.3% of cancer cells were inhibited by p(RT) particles.
Conclusion: Degradable p(RT) and p(QC) particles that are prepared in a single step offer great avenue for biomedical applications as highly antioxidant materials and with good biocompatibility in contact with blood and fibroblast cells, as well as great anticancerogenic capability against the cancer cells.
Keywords: Phenolic particles, antioxidant, anticancer, degradation, controlled drug release, rutin.
20