4.7 Article

Solid lipid nanoparticles to improve bioaccessibility and permeability of orally administered maslinic acid

期刊

DRUG DELIVERY
卷 29, 期 1, 页码 1971-1982

出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2022.2086937

关键词

Solid lipid nanoparticle; maslinic acid; digestion; bioaccessibility; intestinal permeability

资金

  1. Ministerio de Ciencia e Innovacion (MCIN/AEI/FEDER) [RTI2018-101309-B-C21, RTI2018-101309-B-C22]
  2. European Molecular Biology Organization (EMBO-short term fellowships) [8475]
  3. Enterprise Ireland (Career-FIT)
  4. European Union [713654, MF2018-0151 Food-BIBS]
  5. Science Foundation Ireland (SFI)
  6. Department of Agriculture, Food and Marine on behalf of the Government of Ireland [16/RC/3835]
  7. European Commission
  8. European Regional Development Funds of the Junta de Andalucia
  9. Spanish Ministry of Science and Innovation

向作者/读者索取更多资源

Maslinic acid (MA), a low water-soluble compound derived from plants, has been formulated into solid lipid nanoparticles (SLNs) to improve its solubility and bioaccessibility for effective antitumor activity. SLNs can serve as nanocarriers for hydrophobic antitumor compounds and have demonstrated stability and suitability for oral consumption.
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.

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