(M1130-01-06) Formulation and In Vitro Anticancer Activity of Folate Receptor Targeted PLGA Nanoparticles Loaded with Apigenin

Purpose: Breast cancer is the most common cancer among females in the world. Different strategies have been used for treatment of cancer, including chemotherapy which increases the survival rate but comprises of a wide range of side effects. This problem can be overcome by delivering anticancer agents as active and/or passive targeted nano-formulations. Apigenin, a flavonoid group of natural molecule has significant anticancer property, but its application is restricted due to low bioavailability. In the present investigation we examined the folate receptor-targeted and PEGylated poly(lactide-co-glycolide) nanoparticles (PLGA-PEG-FA NPs) containing apigenin for targeted delivery to breast cancer cells, MCF-7.

Methods: The PLGA-based NPs loaded with apigenin were prepared by nanoprecipiotation method. The NPs were characterized for physicochemical properties and evaluated for anticancer activity in MCF-7 cells by MTT assay.

Results: Apigenin loaded PLGA-PEG and PLGA-PEG-FA NPs were small in size, have negative zeta potential, showed sustained release of apigenin and produced significantly higher anticancer activity than the pure drug in breast cancer cells. The half maximal inhibitory concentration (IC₅₀) value of apigenin, apigenin-loaded PLGA, PLGA-PEG and PLGA-PEG-FA NPs was 50.2, 49.4, 18.1 and 13.3 µM, respectively. Apigenin-loaded PLGA-PEG and PLGA-PEG-FA NPs showed 2.79-, and 3.77-fold higher cytotoxicity than the pure drug.

Conclusion: Folate-conjugated PLGA nanoparticles could be developed for potential target-specific delivery of apigenin in the treatment of breast cancer. However, in vivo studies are required to establish the anticancer potential of this fabricated nano-formulation.

References: 1. Saxena V, Naguib Y, Hussain MD. Folate receptor targeted 17-allylamino-17-demethoxygeldanamycin (17-AAG) loaded polymeric nanoparticles for breast cancer. Colloids Surf B Biointerfaces 2012; 94: 274-280.
2. El-Hammadi MM, Delgado AV, Melguizo C, Prados JC, Arias JL. Folic acid-decorated and PEGylated PLGA nanoparticles for improving the antitumour activity of 5-fluorouracil, Int J Pharm. 2017; 516: 61-70.

Acknowledgements: This work was supported by the University Grants Commission, New Delhi, India (F.NO.5-63/2016[IC]) as Raman Fellowship for Postdoctoral Research in USA to AP.