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C60 Fullerene Clusters Stabilize the Biologically Inactive Form of Topotecan
Victoria A Buchelnikova1, Eugene A Rogozhin2,3, Anna S Barashkova2
1Sevastopol State University, Sevastopol 299053, Russia.
Chemical Research in Toxicology
|August 18, 2022
Summary
Fullerene clusters did not enhance the antibiotic topotecan's activity as expected. Instead, they stabilized an inactive form of the drug, suggesting potential for selective pH-sensitive drug delivery.
Area of Science:
- Nanotechnology
- Pharmacology
- Biochemistry
Background:
- C60 fullerene clusters are explored as nanoplatforms for drug delivery.
- Biologically active compounds often exhibit altered properties near fullerene clusters in aqueous solutions.
Purpose of the Study:
- To investigate the interaction between fullerene clusters and the antibiotic topotecan (TPT).
- To elucidate the role of C60 fullerene in modulating TPT activity in vitro.
Main Methods:
- UV/vis titration to confirm complexation between TPT and C60 fullerene.
- In vitro cell assays using proliferating and nonproliferating cell lines.
Main Results:
- Complex formation between TPT and C60 fullerene was confirmed.
- Contrary to expectations, C60 fullerene did not enhance TPT activity in proliferating cells.
- Nonproliferating cell assays showed results consistent with complex formation.
Conclusions:
- The study explains the lack of enhanced TPT activity by the stabilization of an inactive carboxylate form of TPT within the fullerene cluster's alkaline shell.
- This interaction neutralizes the drug delivery function of the fullerene.
- Fullerene clusters show potential for the selective delivery of pH-sensitive drug formulations.
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