A team of Sant Pau Research Institute (IR Sant Pau) of Barcelona has designed a strategy in nanomedicine that allows maintaining and improving the antitumor effect of the chemotherapy using “much smaller” amounts of drug.
The strategy, published in an article in ‘Materials Today Bio’, addresses “one of the great challenges of oncology”, which is reduce the toxicity of chemotherapy without losing effectiveness, reports the IR Sant Pau in a statement this Wednesday.
The IR Sant Pau researcher Ugutz Unzueta has pointed out that for years it has been assumed that increasing the amount of drug was the way to improve efficacy, but the results of the study indicate that what is “really decisive” is how and where the drug binds to the nanocarrier.
Targeted nanomedicines
The team has designed protein nanomedicines capable of self-assembling into multivalent nanoparticles and “highly selectively” targeting tumor cells that overexpress the CXCR4 receptor, involved in the progression and dissemination of numerous solid and hematological tumors, and associated with a worse clinical prognosis.
The platform used in the study is based on a protein nanovehicle that, thanks to having multiple copies of a CXCR4 targeting peptide, favors preferential uptake by tumor cells. thus minimizing the accumulation of the treatment in healthy tissues.
Strategic positions in protein
The work has evaluated site-specific conjugation strategies, that is, those that allow fixing a single drug molecule in strategically selected positions of the protein structure.
The results demonstrate that controlling both the number of drug molecules and their exact location has a “positive impact“in the capacity of the nanoconjugate to accumulate in the tumor and, ultimately, in its antitumor efficacy.
“We have proven that placing the drug in a structurally neutral region allows its therapeutic performance to be improved,” Unzueta pointed out.
