Damrongrak K.Kloysawat K.Bunsupa S.Sakchasri K.Wongrakpanich A.Taresco V.Cuzzucoli Crucitti V.Garnett M.C.Suksiriworapong J.Mahidol University2023-06-182023-06-182022-04-25International Journal of Pharmaceutics Vol.618 (2022)03785173https://repository.li.mahidol.ac.th/handle/20.500.14594/86870The study demonstrated the fabrication of new poly(glycerol adipate) (PGA) nanoparticles decorated with folic acid (FOL-PGA) and triphenylphosphonium (TPP-PGA) and the potential on the delivery of acetogenin-enriched Annona muricata Linn leaf extract to ovarian cancer cells. FOL-PGA and TPP-PGA were successfully synthesized and used to fabricate FOL-decorated nanoparticles (FOL-NPs) and FOL-/TPP- decorated nanoparticles (FOL/TPP-NPs) by blending two polymers at a mass ratio of 1:1. All nanoparticles had small size of around 100 nm, narrow size distribution and high negative surface charge about −30 mV. The stable FOL/TPP-NPs showed highest drug loading of 14.9 ± 1.9% at 1:5 ratio of extract to polymer and reached to 35.8 ± 2.1% at higher ratio. Both nanoparticles released the extract in a biphasic sustained release manner over 5 days. The toxicity of the extract to SKOV3 cells was potentiated by FOL-NPs and FOL/TPP-NPs by 2.0 – 2.6 fold through induction of cell apoptosis. FOL/TPP-NPs showed lower IC50 and higher cellular uptake as compared to FOL-NPs. FOL-NPs exhibited folate receptor-mediated endocytosis. FOL/TPP-NPs provided more advantages than FOL-NPs in terms of stability in physiological fluid, uptake efficiency and targeting ability to mitochondria and showed a promising potential PGA platform for targeted delivery of herbal cytotoxic extracts.Pharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.ijpharm.2022.1216362-s2.0-851260571801873347635259439