Researchers developed a new nanostructured lipid carrier system to deliver imatinib to patients with gastrointestinal stromal tumors (GISTs), as published in Nanomaterials.

A small amount of imatinib loaded into the new system will be better than imatinib alone, they said. Imatinib is extensively used for the treatment of GIST. However, the drug can cause side effects such as cardiac, pulmonary, and hepatic toxicity.

Using a nanostructured lipid carrier system to deliver the treatment can allow the deposition of the treatment in a tumor-specific manner. This can provide more effective pharmacokinetics and pharmacodynamics, better internalization and intracellular transport of the drugs, and reduce biodistribution.


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These properties also mean that the harmful effects of the treatment can be kept to a minimum. The team of researchers led by Marival Bermejo, PhD, characterized their system in terms of particle size, polydispersity index, sterility, zeta potential, entrapment efficiency, loading capacity, syringeability, stability, and in vitro release kinetics.

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They reported that the particle size of the carrier system was between 94.76 nm and 98.5 nm, the polydispersity index was between 0.12 and 0.42, the loading capacity was around 96.49%, and the zeta index was between -30.22 mV and -15.18 mV.

The system was stable, thermodynamic, sterile, and syringeable through an 18 gauge needle. The Korsmeyer–Peppas drug release model of the formulation, also known as the “power law,” was 53% at 8 hours. Moreover, it showed more than 90% of cell viability and a 50% inhibition of viability of 23.61 µM.

Finally, it induced apoptosis in cells in culture. The system should now be tested in animal models before it can be tested in clinical trials for the effective delivery of imatinib in patients with cancer, the authors said.

Reference

Gundogdu E, Demir ES, Ekinci M, et al. An innovative formulation based on nanostructured lipid carriers for imatinib delivery: pre-formulation, cellular uptake and cytotoxicity studies. Nanomaterials. 2022;12(2):250. doi:10.3390/nano12020250