Cancer is the second leading cause of deaths worldwide. Using microRNAs as therapeutics and their nanoparticle-mediated delivery is one new and innovative approach to overcome the current need for clinical improvements. MicroRNA-7 (miR-7) is a 'tumour suppressor' which results in reduced cell viability and tumour growth. This research explored PGMA-PEI nanoparticles as delivery agents for mlR-7, and small molecules as modulators of endogenous miR-7 expression. This project resulted in the development of a screening platform which successfully identified several small molecule regulators of miR-7, which were found to upregulate miR-7 in human colon and liver cancer cells.