Hybrid micelles decrease toxicity of anti-tumor medications

A new paper by KFU’s Laboratory of Functional Hybrid Materials appeared in ACS Applied Polymer Materials.

A micelle is a spherical aggregate of many molecules of surface-active substances (surfactants). The hydrophilic (water-soluble) “heads” of all these molecules are located on the outer surface of the particle, and the hydrophobic (insoluble) “tails” are turned inward, towards the center of the micelle. Since the internal environment of the micelles is hydrophobic, any water-insoluble drug can be loaded into it as in a capsule.

“Loading drugs into simple surfactant-based micelles does not lead to good results in all cases. This design often loses stability and stability under the influence of external conditions or components of the biological environment. We figured out how to increase the stability of surfactant micelles by attaching them to the surface of an insoluble polymer. This made it possible to make the design stable in biological fluids. To create a hybrid micelle, we used a polymer of hyperbranched architecture, which simultaneously contains cavities and a large number of peripheral functional groups for encapsulation, specific binding and controlled release of the drug,” says Associate Professor, Lab Head Marianna Kutyreva.

KFU-produced hybrid micelles are 70 to 100 nanometers in size and comprise a hydrophobic polymer nucleus and a hydrophilic outer layer based on Triton X-100 surfactant.

“We loaded our hybrid micelles with doxorubicin, a drug that is most often used in cancer chemotherapy. It was found that the shell of surfactant molecules makes it possible to stabilize polymer-doxorubicin complexes without changing the chemical structure and properties of the carrier polymer, participates in the delivery and release of the dosage form,” continues Kutyreva.

Widely used anti-tumor medications have many serious side effects including general intoxication. Therefore, targeted delivery based on nanosized polymers is a promising path in this regard.

“We have proven that hybrid micelles loaded with doxorubicin are four times more effective against MCF-7 human adenocarcinoma cells compared to traditional medication forms. This new technology allows for decreased dosage and thus decreased toxicity,” concludes the interviewee.

 

Doxorubicin-Loaded Hybrid Micelles Based on Carboxyl-Terminated Hyperbranched Polyester Polyol

https://pubs.acs.org/doi/full/10.1021/acsapm.1c01863

 

Source text: Larisa Busil

Translation: Yury Nurmeev