Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid Aguilera Garrido, Aixa María Gálvez Ruiz, María José Marchal Corrales, Juan Antonio Galisteo González, Francisco Solid lipid nanoparticle Maslinic acid Digestion Bioaccessibility Intestinal permeability 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. 2022-07-11T08:04:51Z 2022-07-11T08:04:51Z 2022-06-28 info:eu-repo/semantics/article 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] http://hdl.handle.net/10481/75921 10.1080/10717544.2022.2086937 eng info:eu-repo/grantAgreement/EC/H2020/713654 http://creativecommons.org/licenses/by/4.0/ info:eu-repo/semantics/openAccess Atribución 4.0 Internacional Taylor & Francis