In Vitro Cytotoxicity of Oleanolic/Ursolic Acids-Loaded in PLGA Nanoparticles in Different Cell Lines

Abstract

Oleanolic (OA) and ursolic (UA) acids are recognized triterpenoids with anti-cancer properties, showing cell-specific activity that can be enhanced when loaded into polymeric nanoparticles. The cytotoxic activity of OA and UA was assessed by Alamar Blue assay in three different cell lines, i.e., HepG2 (Human hepatoma cell line), Caco-2 (Human epithelial colorectal adenocarcinoma cell line) and Y-79 (Human retinoblastoma cell line). The natural and synthetic mixtures of these compounds were tested as free and loaded in polymeric nanoparticles in a concentration range from 2 to 32 µmol/L. The highest tested concentrations of the free triterpene mixtures produced statistically significant cell viability reduction in HepG2 and Caco-2 cells, compared to the control (untreated cells). When loaded in the developed PLGA nanoparticles, no differences were recorded for the tested concentrations in the same cell lines. However, in the Y-79 cell line, a decrease on cell viability was observed when testing the lowest concentration of both free triterpene mixtures, and after their loading into PLGA nanoparticles.

Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity

“…Results (Figure 4) demonstrate that both blank NLC and NLC loading sucupira oil are considered non-toxic. Indeed, cellular viability was greater than 95% and 90%, for blank and loaded-NLC, respectively, for all concentrations and time-points, which translates a high biocompatibility in vitro of the developed particles [62,68,70]. The selected surfactant d-α-tocopheryl polyethylene glycol succinate, or vitamin E TPGS, has been approved by the Food and Drug Administration as a safe ingredient and is commonly used in pharmaceutical dosage forms [71].…”

“…The human intestinal Caco-2 cell line, a cell line derived from a colorectal adenocarcinoma, has a epithelial like-morphology and is commonly used as in vitro model for cytotoxicity screening of formulations intended for oral administration. In this work, the cell viability results, was tested in two time-points and using empty (blank) and loaded NLC, as recommended by Silva et al [68,69]. Results (Figure 4) demonstrate that both blank NLC and NLC loading sucupira oil are considered non-toxic.…”

Soft Cationic Nanoparticles for Drug Delivery: Production and Cytotoxicity of Solid Lipid Nanoparticles (SLNs)

“…Test solutions were prepared just prior to cell application, by dispersing the required volume of particles in FBS-free culture media to achieve the desired final concentration. Test solutions (100 µL/well; in quadruplicates) were added to the cells, after removing the growing culture media, and cells were exposed for 24 h or 48 h to test solutions before the cell viability assessment using the Alamar Blue (Invitrogen; Alfagene, Lisbon, Portugal), as previously reported [27,28]. Briefly, 24 h or 48 h after cell exposure, the incubating test solutions were removed and replaced by Alamar Blue solution (10% (v/v) in FBS-free culture media; 100 µL/well).…”

Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods

“…Polymeric nanoparticles can be obtained from natural, semi-synthetic or synthetic polymers (e.g., chitosan [37][38][39], polylactic acid (PLA), poly(lactic-co-glycolic acid) (PLGA) [40][41][42][43]), which will then govern the way the drugs are encapsulated inside the matrix (dissolved or dispersed) or attached onto the nanoparticle' surface (chemically bound or adsorbed), and how the drug is released [44]. Polymeric nanoparticles can be produced with a variety of sizes and shapes, with high drug payload for both hydrophilic and lipophilic molecules, can be surface-modified to increase the plasma half-life (e.g., PEGylation [45,46]) to have site-specific targeted delivery [47], and release the drug in a controlled fashion [48][49][50].…”