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1.
Mater Sci Eng C Mater Biol Appl ; 91: 785-795, 2018 Oct 01.
Article in English | MEDLINE | ID: mdl-30033314

ABSTRACT

Fucoxanthin (FUCO), a marine carotenoid is photo-, and thermo-labile and poorly bioavailable due to its lipophilicity. Hence, we developed a chitosan (CS) + glycolipid (GL) nanogels (NGs) to increase cellular uptake and anticancer efficacy of FUCO (10 µM) in human colon cells (Caco-2). Effect of FUCO loaded in NGs with/with no GL was studied in comparison with micellar FUCO. Results showed that the cell viability was lower (p < 0.05) in NGs + GL (50.5%) compared to NGs (-GL) (66.5%) and the mixed micelles (72.5%) groups over 48 h exposure. An enhanced reactive oxygen species (ROS) generation was evident in NGs + GL (379.2%) group compared to NGs (-GL) and mixed micelles groups. Further, induction of apoptosis with an increased chromatin condensation and DNA fragmentation as evidenced in DAPI staining and DNA ladder assay were higher in NGs + GL group than other groups. Down-regulation of Bcl-2 (6.6 folds) was higher in NGs + GL group compared to NGs (-GL) (1.94 fold) and mixed micelles (1.19 fold) groups. Higher Bax up-regulation in NGs + GL compared to other groups supports the Bcl-2 down regulation. Mitochondrial membrane polarisation (ΔΨm) was higher in NGs + GL group (2.46 fold) compared to NGs (-GL) (1.91 fold) and mixed micelles (1.26 fold) groups. The cellular FUCO uptake illustrated a positive correlation between its level (pmol/106 cells) in NGs + GL (758.3) and enhanced caspase-3 activity (25.8 folds). This could be the reason for an increased apoptotic activity in NGs + GL group than other groups. Results demonstrate that delivery of FUCO in NGs + GL carrier aids cellular uptake and chemotherapeutic potential of FUCO. Results further demonstrate, for the first time, higher anti-cancer activity of FUCO loaded in NGs + GL and the effect was through ROS generation via a caspase dependent mechanism in Caco-2 cells.


Subject(s)
Apoptosis/drug effects , Chitosan/chemistry , Colonic Neoplasms/pathology , Drug Carriers/chemistry , Drug Delivery Systems , Glycolipids/chemistry , Nanoparticles/chemistry , Xanthophylls/pharmacology , Caco-2 Cells , Carotenoids/chemistry , Carotenoids/pharmacology , Caspases/metabolism , Cell Survival/drug effects , DNA Fragmentation/drug effects , Endocytosis/drug effects , Enzyme Activation/drug effects , Humans , Kinetics , Membrane Potential, Mitochondrial/drug effects , Muramidase/metabolism , Nanogels , Polyethylene Glycols , Polyethyleneimine , Reactive Oxygen Species/metabolism , Xanthophylls/chemistry , bcl-2-Associated X Protein/metabolism
2.
J Biomater Appl ; 30(4): 420-34, 2015 Oct.
Article in English | MEDLINE | ID: mdl-26084499

ABSTRACT

Fucoxanthin (FUCO) is a light- and heat-sensitive marine xanthophyll carotenoid, present in brown algae that render physiological properties as anti-oxidants. In this study, nanoencapsulation is an approach adopted to improve bioavailability of FUCO by using ionic-gelation method with polymeric chitosan (CS) dispersed in glycolipid (GL), as a carrier. Further, the aim was to investigate adverse effect of acute and sub-acute toxicity of chitosan nanogels (CS-NGs) loaded with FUCO+GL in rats. In the acute toxicity study, FUCO was fed to rats at doses of 0.1, 1, 10 and 100 mg/kg body weight (BW). In the sub-acute toxicity study, FUCO was fed at doses of 1 and 10 mg/kg BW for 28 days. In both the studies, no mortality and abnormalities in gross morphology were observed. Acute toxicity study revealed that the LD50 of FUCO in CS-NGs is higher than 100 mg/kg BW. No postprandial plasma levels of FUCO were detected. However, fucoxanthinol (FUOH), a hydrolytic metabolite of FUCO was detected in a dose dependent manner (P < 0.01). Compared to the control group(s), no dose-related toxic effects of CS-NGs with FUCO + GL were found in haematological, histopathological, plasma biochemical indices, etc. The no-observed-adverse-effect level (NOAEL) for CS-NGs with FUCO + GL in rats was 10 mg/kg/day. To conclude, no apparent adverse effect of CS-NGs with FUCO + GL demonstrating CS could be a promising polymer matrix for safe delivery of FUCO. This is the first study to demonstrate the safety assessment of CS-NGs with FUCO + GL.


Subject(s)
Anti-Obesity Agents/administration & dosage , Chitosan/chemistry , Drug Carriers/chemistry , Glycolipids/chemistry , Xanthophylls/administration & dosage , Animals , Anti-Obesity Agents/chemistry , Anti-Obesity Agents/toxicity , Female , Gels/chemistry , Rats, Wistar , Seaweed/chemistry , Xanthophylls/chemistry , Xanthophylls/toxicity
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