Active targeted nanoparticles: Preparation, physicochemical characterization and in vitro cytotoxicity effect

Sh Heidarian, K Derakhshandeh, H Adibi, L Hosseinzadeh


In this study, the folate decorated biodegradable poly (lactide-co-glycolide) (PLGA) nanoparticles were developed for tumor targeting of anticancer agents. Due to the overexpression of the folate receptor on tumor surface, the folate has been efficiently employed as a targeting moiety for various anticancer agents to avoid their non-specific attacks on normal tissues and also to increase their cellular uptake within target cells. Folate conjugate PLGA was synthesized successfully and its chemical structure was evaluated by FTIR, DSC and 1HNMR spectroscopy. PLGA-folate nanoparticles (PLGA-Fol NPs) were prepared by nanoprecipitation method, adopting PLGA as a drug carrier, folic acid as a targeting ligand and 9-nitrocampthotecin as a model anticancer drug. The average size and encapsulation efficiency of the prepared PLGA-Fol NPs were found to be around 115  12 nm and 57%, respectively. In vitro release profile indicated that nearly 85% of the drug was released in 50 h. The in vitro intracellular uptakes of PLGA-Fol NPs showed greater cytotoxicity on cancer cell lines compared to non-folate mediated carriers.

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