Preparation and characterization of lutein loaded folate conjugated polymeric nanoparticles

J Microencapsul. 2020 Nov;37(7):502-516. doi: 10.1080/02652048.2020.1809724. Epub 2020 Aug 26.

Abstract

Aim: To prepare and characterise lutein-loaded polylactide-co-glycolide-polyethylene glycol-folate (PLGA-PEG-FOLATE) nanoparticles and evaluate enhanced uptake in SK-N-BE(2) cells.

Methods: Nanoparticles were prepared using O/W emulsion solvent evaporation and characterised using DLS, SEM, DSC, FTIR and in-vitro release. Lutein-uptake in SK-N-BE(2) cells was determined using flow-cytometry, confocal-microscopy and HPLC. Control was lutein PLGA nanoparticles.

Results: The size of lutein-loaded PLGA and PLGA-PEG-FOLATE nanoparticles were 189.6 ± 18.79 nm and 188.0 ± 4.06 nm, respectively. Lutein entrapment was ∼61%(w/w) and ∼73%(w/w) for PLGA and PLGA-PEG-FOLATE nanoparticles, respectively. DSC and FTIR confirmed encapsulation of lutein into nanoparticles. Cellular uptake studies showed ∼1.6 and ∼2-fold enhanced uptake of lutein from PLGA-PEG-FOLATE nanoparticles compared to PLGA nanoparticles and lutein, respectively. Cumulative release of lutein was higher in PLGA nanoparticles (100% (w/w) within 24 h) compared to PLGA-PEG-FOLATE nanoparticles (∼80% (w/w) in 48 h).

Conclusion: Lutein-loaded PLGA-PEG-FOLATE nanoparticles could be a potential treatment for hypoxic ischaemic encephalopathy.

Keywords: Lutein; PLGA; PLGA-PEG-FOLATE; folate decorated nanoparticles; hypoxic ischaemic encephalopathy; perinatal asphyxia; targeted delivery.

MeSH terms

  • Cell Line, Tumor
  • Drug Carriers / chemistry*
  • Drug Delivery Systems
  • Folic Acid / analogs & derivatives*
  • Folic Acid / chemistry
  • Humans
  • Hypoxia-Ischemia, Brain / drug therapy
  • Lutein / administration & dosage*
  • Lutein / pharmacokinetics
  • Polyesters / chemistry*
  • Polyethylene Glycols / chemistry*

Substances

  • Drug Carriers
  • Polyesters
  • poly(ethylene glycol)-folate
  • polyethylene glycol-poly(lactide-co-glycolide)
  • Polyethylene Glycols
  • Folic Acid
  • Lutein