Researchers from Penn State College of Medicine have published results in the journal Molecular Cancer Therapeutics, titled “Nanolipolee-007, a Novel Nanoparticle-Based Drug Containing Leelamine for the Treatment of Melanoma”, showing the development of a nanoparticle capable of delivering a melanoma-fighting drug directly to cancer cells.
“The drug is packaged into a lipid ball significantly smaller than the width of a hair to make it soluble in the blood stream and prevent negative side effects. The drug-containing nanoparticle ball then travels in the bloodstream to the tumor, where it accumulates and the drug is released in the tumor to kill the cancer cells,” study author Gavin Robertson, professor of pharmacology, pathology, dermatology, and surgery and director of the Penn State Hershey Melanoma Center, said in a University press release.
Malignant melanoma is a difficult cancer to treat, in part because this type of malignancy has the ability of rapidly developing resistance to drugs that target single proteins.
In order to overcome this problem, researchers need to identify pharmacologic agents that can target multiple key pathways involved in melanoma development.
Leelamine, a substance derived from pine bark, has been shown to possess anti-cancer properties, and function in a way that simultaneously targets different pathways of cancer cells. Mechanistically, it inhibits cholesterol movement and shuts down the necessary signals for cancer cell survival, turning off essential pathways for cancer development, such as PI3K, MAPK and STAT3.
However, it also has a poor bioavailability in animals and can cause irreparable damage and ultimately become lethal when administered intravenously.
To overcome this problem, the research team developed a nanoliposomal-based delivery system, the Nanolipolee-007, which can be injected intreavenously and stably load 60% of the compound. Furthermore, the vehicle can accumulate in tumors due to its reduced size, and release the drug in situ, specifically killing the malignant cells.
“This nanoparticle moves leelamine one step closer to the clinic,”Dr. Robertson said. “We now have a drug that has the potential to be given to humans that could not be done before.”
Researchers used in vivo mice models to show that leelamine delivered with Nanolipolee-007 intravenously, inhibited tumor development with no detectable side effects.
Penn State has already patented these results and has licensed them to Melanovus Oncology, partly owned by Penn State and Dr. Robertson, for future FDA-required tests that will enable it to be tested in humans.