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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

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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.

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Acknowledgments

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

Funding

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

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Authors and Affiliations

  1. Department of Biochemistry, CSIR-Central Food Technological Research Institute, Mysore, Karnataka, 570020, India

    Arunkumar Ranganathan & Vallikannan Baskaran

  2. John. A. Moran Eye Center, University of Utah, Salt Lake City, 84132, USA

    Arunkumar Ranganathan

  3. Department of Applied Bioscience, Graduate School of Agriculture, Kyoto University, Kyoto, 6068502, Japan

    Yuki Manabe & Tatsuya Sugawara

  4. Department of Rehabilitation, Shijonawategakuen University, Osaka, 5740011, Japan

    Takashi Hirata

  5. Department of Applied Microbiology, DRDO- Defence Food Technological Research Institute, Mysore, Karnataka, 570011, India

    Naveen Shivanna

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  1. Arunkumar Ranganathan
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  2. Yuki Manabe
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  3. Tatsuya Sugawara
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  4. Takashi Hirata
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Correspondence to Vallikannan Baskaran.

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Ranganathan, A., Manabe, Y., Sugawara, T. et al. 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. Drug Deliv. and Transl. Res. 9, 178–191 (2019). https://doi.org/10.1007/s13346-018-0590-9

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  • DOI: https://doi.org/10.1007/s13346-018-0590-9

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