In Vitro Cytotoxicity and Bioavailability of Ginsenoside-Modified Nanostructured Lipid Carrier Containing Curcumin.

Abstract:

:Our aim was to investigate the cellular uptake, in vitro cytotoxicity and bioavailability of ginsenoside-modified nanostructured lipid carrier loaded with curcumin (G-NLC). The formulation was prepared by melt emulsification technique, in which water was added to the melted lipids and homogenized to give a uniform suspension of NLC (without ginsenoside) and G-NLC. Cellular uptake of curcumin in two colon cancer cell lines (HCT116 and HT29) was increased when administered using both NLC and G-NLC compared to control (curcumin dissolved into DMSO) as measured by fluorescence microscopy. Ginsenoside modification resulted in 2.0-fold and 1.4-fold increases in fluorescence intensity in HCT116 and HT29 cell lines, respectively, compared to plain NLC. In vitro cytotoxicity (assessed by MTT assay) had a dose-dependent relationship with curcumin concentration for both NLC and G-NLC. Although G-NLC was taken up more readily in HCT116 cells, ginsenoside modification did not produce a significant increase in cytotoxic effect; a significant increase was observed in HT29 cells. Oral administration of G-NLC in ten colon cancer patients produced an appreciable plasma level of unbound curcumin (2.9 ng/mL). In conclusion, introduction of ginsenoside into NLC enhanced the cellular uptake and cytotoxicity of curcumin as well as its oral bioavailability, and this strategy can be used to improve clinical outcomes in the treatment of colon cancer with similar genotype to HT29.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Vijayakumar A,Baskaran R,Baek JH,Sundaramoorthy P,Yoo BK

doi

10.1208/s12249-019-1295-1

subject

Has Abstract

pub_date

2019-01-23 00:00:00

pages

88

issue

2

issn

1530-9932

pii

10.1208/s12249-019-1295-1

journal_volume

20

pub_type

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