Development of gemcitabine-loaded lipobeads using the Quality by Design approach

Lipobeads (LB) are drug delivery systems entrapping a nanogel core in a lipidic layer, which have been designed to overcome the low entrapment of hydrophilic drugs in liposomes. This study describes the development of gemcitabine-loaded lipobeads (LB-GEM) using the Quality by Design (QbD) approach. Two experimental designs (screening and optimization) were carried out to improve the formulation and characteristics of the nanocarriers. The cytotoxicity of the optimal LB-GEM formulation was compared in vitro with free GEM and empty LB on lung cancer and normal cell lines. The obtained results suggested that LB-GEM induced an increased cytotoxicity compared to free GEM in A549 lung cancer cells but did not affect the viability of normal foreskin fibroblasts. Also, the empty LB evaluated at concentrations equivalent to the LB-GEM formulation did not exhibit cytotoxic effects, proving the safety of the nanocarrier. Overall, these findings suggest that LB-GEM provide a novel strategy to improve the chemotherapeutic efficacy against tumors.