The new approach uses peptides to improve antitumor drug formulations

The new approach uses peptides to improve antitumor drug formulations

A team of scientists has developed a groundbreaking approach that uses specially designed peptides to improve drug formulations. This innovative method significantly improves antitumor effectiveness, as shown in leukemia models. The study published in the journalChemwas led by researchers from the CUNY Graduate Center Advanced Science Research Center (CUNY ASRC) and Memorial Sloan Kettering Cancer Center.

Drug delivery systems often face two critical challenges: poor solubility and inefficient delivery within the body. Many medications do not dissolve well, making it difficult for them to reach their intended targets. Additionally, current delivery systems waste a significant portion of the drug while only 5 to 10% of the drug is successfully loaded, resulting in less effective treatments.

Peptide helpers

The research team has developed a novel solution by binding peptides-cabins of amino acids to specific drugs and creating therapeutic nanoparticles. These nanoparticles consist primarily of the drug with a thin peptide coating that improves solubility, improves stability in the body and optimizes delivery to targeted areas. Remarkably, this approach achieves drug exposure of up to 98%, a dramatic improvement over traditional methods.

By using a combination of computer modeling and laboratory testing, new drug/peptide nanoparticles have been identified. They then showed remarkable results in leukemia models. The nanoparticles were more effective at shrinking tumors compared to the drugs alone. In addition, their high efficiency allows for lower drug doses, potentially reducing side effects.

Peptides, which are molecules made from the same building blocks as the proteins in our bodies, are extremely versatile. We thought they might be useful to solve two major problems in many drugs: poor solubility and inefficient delivery. By designing a peptide that binds the drug while improving its solubility, we were able to create very high loading nanoparticles. “

Rein Ulijn, Co-Principal Investigator, Director of the Nanoscience Initiative at Cuny ASRC and Professor of Chemistry at Hunter College

Customizable technology

This innovation has significant potential because peptides can be tailored to improve the effectiveness of various drugs. Given the variety of possible interactions in peptide design, it may be possible to tailor peptides for specific drugs and extend their applicability beyond cancer treatments.

“This breakthrough enables the development of better precision medicines,” said co-principal investigator Daniel Heller, head of the cancer nanomedicine laboratory atMemorial Sloan Kettering Cancer Center's Molecular Pharmacology Program. “Using specially designed peptides, we can build nanomedicines that make existing drugs more effective and less toxic, and even enable the development of drugs that may not work without these nanoparticles.”

Naxhije “Gia” Berisha, a former Ph.D. Student, who carried out much of the experimental work, highlighted the potential of the peptide approach: “We used experimental testing to identify promising peptides and computational modeling to analyze their interactions with therapeutic molecules,” she said. “It is incredible to see how simple variations in peptide sequence could correspond to specific drugs.

Look forward

The research team is now adopting laboratory automation methods to further refine and accelerate the peptide-drug matching process. Their next steps include testing the approach's potential in a broader range of diseases. If successful, this innovation could lead to more effective treatments, reduced side effects and significant cost savings in drug development.

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