title: Oleanolic Acid Loaded PEGylated PLA and PLGA Nanoparticles with Enhanced Cytotoxic Activity against Cancer Cells.
abstract: Oleanolic acid (OA) is a natural triterpenoid with anticancer properties, but its hydrophobic nature and poor aqueous solubility pose challenges in pharmaceutical formulation development. The present study aimed at developing OA-loaded mPEG-PLGA or mPEG-PLA nanoparticles (NPs) to improve the delivery of OA. The NPs were prepared by nanoprecipitation, and their physicochemical properties were characterized. The OA encapsulation efficiency of the NPs was between 40 and 75%. The size of the OA-loaded NPs was around 200-250 nm, which fell within the range required for tumor targeting by means of the enhanced permeability and retention (EPR) effect, and the negatively charged NPs remained physically stable for over 20 weeks with no aggregation observed. The OA-loaded NPs produced significant cytotoxic effects through apoptosis in cancer cell lines. Overall, the OA-loaded mPEG-PLGA NPs and mPEG-PLA NPs shared similar physicochemical properties. The former, especially the OA-loaded mPEG-P(D,L)LGA NPs, were more cytotoxic to cancer cells and therefore were more efficient for OA delivery.
authors.forename: Dede K W
authors.initials: DK
authors.lastname: Man
authors.affiliation: ‡Department of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza Rinascimento, 6, 61029 Urbino, Pesaro and Urbino, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Casettari
authors.affiliation: §School of Pharmacy, University of Camerino, via Sant'Agostino 1, 62032 Camerino, Macerata, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Cespi
authors.affiliation: §School of Pharmacy, University of Camerino, via Sant'Agostino 1, 62032 Camerino, Macerata, Italy.
authors.forename: Giulia
authors.initials: G
authors.lastname: Bonacucina
authors.affiliation: §School of Pharmacy, University of Camerino, via Sant'Agostino 1, 62032 Camerino, Macerata, Italy.
authors.forename: Giovanni Filippo
authors.initials: GF
authors.lastname: Palmieri
authors.affiliation: ∥School of Chinese Medicine, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Pokfulam, Hong Kong.
authors.forename: Stephen C W
authors.initials: SC
authors.lastname: Sze
authors.forename: George P H
authors.initials: GP
authors.lastname: Leung
authors.forename: Jenny K W
authors.initials: JK
authors.lastname: Lam
authors.forename: Philip C L
authors.initials: PC
authors.lastname: Kwok
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D002460:Cell Line; D004337:Drug Carriers; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms; D009828:Oleanolic Acid / Q000737:chemistry* / Q000494:pharmacology; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D009828:Oleanolic Acid
keywords: PEGylation; PLA; PLGA; cytotoxicity; nanoparticles; oleanolic acid