Co-encapsulation of phytol modulates colloidal properties and methotrexate release from polylactic nanoparticles as potential strategy for improving chemotherapy efficacy
Methotrexate. Phytol. Nanoparticle co-delivery. Antiproliferative activity. HeLa cancer cells.
Despite advances in oncology treatments, the lack of drug specificity for neoplastic
tissue remains a significant challenge, contributing to the high incidence of adverse
effects. Phytol, a bioactive secondary metabolite of chlorophyll, shows promising
anticancer activity, while methotrexate (MTX) is widely used as a
chemotherapeutic agent for the treatment of malignant tumors. Nanoparticles have
been explored as drug delivery vehicles, enabling site-specific release and
overcoming limitations imposed by biological barriers. This study aimed to
characterize co-encapsulated nanoparticles containing phytol and methotrexate,
functionalized with polyethyleneimine (PEI), to assess a potential increase in
antiproliferative activity in cancer cells, particularly in HeLa cells. Physicochemical
characterization revealed nanoparticles with an average size of 250 nm, a
polydispersity index (PdI) below 0.2, spherical morphology, encapsulation
efficiency over 90%, and stability throughout the evaluation period. The formulation
also showed good cytocompatibility with L929 cells at a PLA concentration of 5
µg/mL. In terms of biological efficacy, the functionalized nanoparticles
demonstrated significant antiproliferative effects in HeLa cells, reducing cell
viability by 63% in the MTT assay after 24 hours of exposure. Additionally, further
tests, including zeta potential, pH, and infrared absorption spectroscopy (FTIR
ATR), confirmed the stability of the formulations. The results suggest that the
functionalized nanoparticle platform for co-encapsulation of phytol and MTX holds
great potential for in vitro biological activity studies and may be promising for future
applications in cancer treatment.