Self-microemulsifying lipid delivers anticancer drug
doi:10.1038/nindia.2015.66 Published online 18 May 2015
Researchers have synthesized nanosized, self-microemulsifying lipids that can deliver etoposide, a widely used anticancer drug that targets skin cancer cells1. These lipids reduce the drug’s toxicity and thus are a potentially safe therapeutic option for cancer patients.
Most anticancer drugs kill cancer cells by entering their nuclei or the intracellular fluid surrounding the nuclei. But this process is often disrupted by vesicles that trap and degrade anticancer drugs.
To prevent such degradation, the researchers synthesized self-microemulsifying lipids by using a monoguanidine heterolipid and a surfactant. They then probed the stability of the etoposide-loaded formulations by subjecting them to various stress conditions and extreme temperatures. The scientists found that they retained their ability to form clear microemulsions and that their globule size, zeta potential and drug content did not vary significantly even after six months of storage.
To explore the therapeutic potential of the formulations, the researchers treated cultured skin cancer cells and tumour-bearing mice with the drug-loaded formulations. All the drug-based formulations inhibited cancer cell growth by altering their morphological features. The lipids also increased the bioavailability of the drug inside the cancer cells. The researchers attribute this increased bioavailability to hydrogen bonds that the lipids form with the ions and molecules on the cancer cell membranes.
1. Shete, H. et al. Mono-guanidine heterolipid based SMEDDS: A promising tool for cytosolic delivery of antineoplastics. Biomaterials 57,116–132 (2015)