RT Journal Article
T1 Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid.
A1 Aguilera-Garrido, Aixa
A1 Arranz, Elena
A1 Galvez-Ruiz, Maria Jose
A1 Marchal, Juan Antonio
A1 Galisteo-Gonzalez, Francisco
A1 Giblin, Linda
K1 Solid lipid nanoparticle
K1 bioaccessibility
K1 digestion
K1 intestinal permeability
K1 maslinic acid
AB Maslinic acid (MA) is a plant-derived, low water-soluble compound with antitumor activity. We have formulated MA in the form of solid lipid nanoparticles (SLNs) with three different shell compositions: Poloxamer 407 (PMA), dicarboxylic acid-Poloxamer 407 (PCMA), and HA-coated PCMA (PCMA-HA). These SLNs improved the solubility of MA up to 7.5 mg/mL, are stable in a wide range of pH, and increase the bioaccessibility of MA after in vitro gastrointestinal (GI) digestion. Gastrointestinal digested SLNs afforded MA delivery across in vitro gut barrier models (21 days old Caco-2 and mucus-producing Caco-2/HT29-MTX co-cultures). The cellular fraction of Caco-2/HT29-MTX co-cultures retained more MA from GI digested PCMA-HA than the Caco-2 monolayers. The concentration of MA reached in the basolateral chamber inhibited growth of pancreatic cancer cells, BxPC3. Finally, confocal microscopy images provided evidence that Nile Red incorporated in MA SLNs was capable of crossing Caco-2 monolayers to be taken up by basolaterally located BxPC3 cells. We have demonstrated that SLNs can be used as nanocarriers of hydrophobic antitumor compounds and that these SLNs are suitable for oral consumption and delivery of the bioactive across the gut barrier.
PB Taylor & Francis Inc.
YR 2022
FD 2022-05-30
LK http://hdl.handle.net/10668/19677
UL http://hdl.handle.net/10668/19677
LA en
NO Aguilera-Garrido A, Arranz E, Gálvez-Ruiz MJ, Marchal JA, Galisteo-González F, Giblin L. Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid. Drug Deliv. 2022 Dec;29(1):1971-1982.
NO This work has been supported by the Ministerio de Ciencia e Innovacion (MCIN/AEI/10.13039/501100011033/FEDER) under Grants [RTI2018-101309-B-C21] and [RTI2018-101309-B-C22]; the European MolecularBiology Organization (EMBO-short term fellowships) under Grant 8475;the Enterprise Ireland (Career-FIT) and the European Union’s Horizon2020 research and innovation program under the Marie SkłodowskaCurie Grant Agreement No. 713654 (Project MF2018-0151 Food-BIBS);Science Foundation Ireland (SFI) and the Department of Agriculture,Food and Marine on behalf of the Government of Ireland under GrantNumber [16/RC/3835]. This work has also been supported by theEuropean Commission; European Regional Development Funds of theJunta de Andaluc ıa; Spanish Ministry of Science and Innovation.
DS RISalud
RD Apr 6, 2025