Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid
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AuthorAguilera Garrido, Aixa María; Gálvez Ruiz, María José; Marchal Corrales, Juan Antonio; Galisteo González, Francisco
Taylor & Francis
Solid lipid nanoparticleMaslinic acidDigestionBioaccessibilityIntestinal permeability
Aixa Aguilera-Garrido... [et al.] (2022) Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid, Drug Delivery, 29:1, 1971-1982, DOI: [10.1080/10717544.2022.2086937]
SponsorshipMinisterio de Ciencia e Innovacion (MCIN/AEI/FEDER) RTI2018-101309-B-C21 RTI2018-101309-B-C22; European Molecular Biology Organization (EMBO-short term fellowships) 8475; Enterprise Ireland (Career-FIT); European Commission 713654; MF2018-0151 Food-BIBS; Science Foundation Ireland; Department of Agriculture, Food and Marine on behalf of the Government of Ireland 16/RC/3835; European Commission European Commission Joint Research Centre European Regional Development Funds of the Junta de Andalucia; Spanish Government
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 7.5mg/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.