In vitro evaluation of folate-modified PLGA nanoparticles containing paclitaxel for ovarian cancer therapy

Highlights: • Folate-modified PLGA nanoparticles containing paclitaxel (PN-PCX-FA) were produced for promoting active targeting. • PN-PCX-FA and unmodified nanoparticles containing paclitaxel (PN-PCX) showed low MPD and PDI with negative ZP. • PN-PCX-FA and PN-PCX were able to reduce cell viability using SKOV-3 cell line. • PN-PCX-FA showed higher reduction of cell viability in low paclitaxel concentration. • PN-PCX-FA demonstrated a 3.6-fold higher cellular uptake than PN-PCX. -- Abstract: Ovarian cancer is the most lethal gynecological cancer of female reproductive system. In order to improve the survival rate, some modifications on nanoparticles surfaces have been investigated to promote active targeting of drugs into tumor microenvironment. The aim of this study was the development and characterization of folate-modified (PN-PCX-FA) and unmodified PLGA nanoparticles (PN-PCX) containing paclitaxel for ovarian cancer treatment. Nanocarriers were produced using nanoprecipitation technique and characterized by mean particle diameter (MPD), polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (EE), DSC, FTIR, in vitro cytotoxicity and cellular uptake. PN-PCX and PN-PCX-FA showed MPD < 150 nm and PDI < 0.2 with high EE (about 90%). Cytotoxicity assays in SKOV-3 cells demonstrated the ability of both formulations to cause cellular damage. PCX encapsulated in PN-PCX-FA at 1 nM showed higher cytotoxicity than PN-PCX. Folate-modified nanoparticles showed a 3.6-fold higher cellular uptake than unmodified nanoparticles. PN-PCX-FA is a promising system to improve safety and efficacy of ovarian cancer treatment. Further in vivo studies are necessary to prove PN-PCX-FA potential.