Squalenoyl nanomedicines can work as effective prospective therapeutics

Nucleoside analogs like gemcitabine and cytarabine were merely considered to be powerful anti-cancer agents in the past but a recent study shows that they can prove out to be even more valuable with a simple chemical modification for treating varying forms of cancer.

A research team headed by Patrick Couvreur, Ph.D., at the CNRS in Châtenay-Malabry, France, was of the view that this new technique seems to be potential candidate when it comes to working with almost all possible kinds of nucleoside analogs. In addition to that, the technique also has the net effect of increasing the pharmacological behavior of compounds belonging to this class.

From News-Medical.Net:

A research team headed by Patrick Couvreur, Ph.D., at the CNRS in Châtenay-Malabry, France, found that attaching the molecule squalene to any one of several nucleoside analogs triggered a self-assembly process that creates nanoparticles that are stable in biological fluids. Squalene is a naturally occurring, water-insoluble compound involved in synthesizing steroid hormones. Linking this molecule to a water-soluble nucleoside analog causes the resulting conjugates to form a core-shell nanostructure, with the nucleoside analogs creating an outer layer that shields the squalene portion from the surrounding aqueous environment.

Tests using cultured tumor cells showed that a squalene-gemcitabine conjugate was up to eight times more potent as an anticancer agent compared to unmodified gemcitabine. In addition, these in vitro studies showed that the squalene-gemcitabine conjugate was able to kill cells that had developed resistance to gemcitabine. The researchers attribute the improved anticancer activity, in both normal and resistant cells, to the fact that the conjugate is poorly metabolized by the enzymes that normally detoxify nucleoside analogs.

Based on these promising results, the investigators then assessed anticancer activity of squalene-modified gemcitabine in both mouse and rat models of human leukemia. In each case, 40 percent of the animals treated with the squalene-gemcitabine conjugate survived for at least 100 days after treatment. In contrast, control animals that received a placebo or unmodified gemcitabine all died from cancer within 60 days.

In other words, it was said that squalene-gemcitabine conjugate was potent by as much as eight times when compared to unmodified gemcitabine for treating varying forms of cancer.