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Drug Delivery and Translational Research

, Volume 9, Issue 1, pp 178–191 | Cite as

Poly (d, l-lactide-co-glycolide)-phospholipid nanocarrier for efficient delivery of macular pigment lutein: absorption pharmacokinetics in mice and antiproliferative effect in Hep G2 cells

  • Arunkumar Ranganathan
  • Yuki Manabe
  • Tatsuya Sugawara
  • Takashi Hirata
  • Naveen Shivanna
  • Vallikannan BaskaranEmail author
Original Article
  • 118 Downloads

Abstract

Lutein has various biological activities, its application in food and pharma industries are limited due to poor aqueous solubility, stability, and bioavailability. To achieve various benefits, lutein-poly (lactic-co-glycolic acid) (PLGA)-phospholipid (PL) nanocapsules were prepared. Lutein-PLGA NCs (+PL) were synthesized, characterized and its bioavailability was studied in vitro and in vivo. The cellular uptake and anti-proliferative activity were analyzed in Hep G2 cells. The mean size and zeta value of lutein-PLGA NCs (+PL) were 140 ± 6 nm and − 44 mV. The amorphous nature of lutein in PLGA NCs (+PL) was confirmed by XRD and DSC. In vitro lutein release kinetics showed an initial burst followed by sustainable release up to 86%. In vitro bioavailability showed 62.7% higher lutein bioaccessibility than lutein in free form. The AUC of lutein after single oral dose of lutein-PLGA NCs (+PL) revealed 3.91-fold (plasma), 2.89-fold (liver), and 3.12-fold (eyes) higher absorption than the control (mixed micelles). The IC50 of lutein-PLGA NCs (+PL) in Hep G2 cells at 72 h was 4.5 μM as opposed to 23.4 μM for lutein in free form. Thus, results reveal that PL added to PLGA NCs helps in enhancing the solubility which in turn resulted in its better bioavailability and bioefficacy.

Keywords

Biomaterials Bioavailability Carotenoids Hep G2 Lutein Nanocapsules PLGA Phospholipids Stability 

Notes

Acknowledgments

R. Arunkumar acknowledges Indian Council of Medical Research (ICMR), Govt. of India for awarding Senior Research Fellowship.

Funding information

This research project was financially supported by the Department of Science and Technology (DST), Govt. of India (DST, INT/JSPS/P-122/11)

Compliance with ethical standards

Ethical standards

Manuscripts submitted for publication must contain a declaration that the experiments comply with the current laws of the country in which they were performed.

Animal studies

All institutional and national guidelines for the care and use of laboratory animals were followed.

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

13346_2018_590_MOESM1_ESM.docx (1.8 mb)
ESM 1 (DOCX 1835 kb)

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Copyright information

© Controlled Release Society 2018

Authors and Affiliations

  • Arunkumar Ranganathan
    • 1
    • 2
  • Yuki Manabe
    • 3
  • Tatsuya Sugawara
    • 3
  • Takashi Hirata
    • 4
  • Naveen Shivanna
    • 5
  • Vallikannan Baskaran
    • 1
    Email author
  1. 1.Department of BiochemistryCSIR-Central Food Technological Research InstituteMysoreIndia
  2. 2.John. A. Moran Eye CenterUniversity of UtahSalt Lake CityUSA
  3. 3.Department of Applied Bioscience, Graduate School of AgricultureKyoto UniversityKyotoJapan
  4. 4.Department of RehabilitationShijonawategakuen UniversityOsakaJapan
  5. 5.Department of Applied MicrobiologyDRDO- Defence Food Technological Research InstituteMysoreIndia

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