Ocular delivery of cyanidin-3-glycoside in liposomes and its prevention of selenite-induced oxidative stress

Abstract

Context: Cataracts have become the leading cause of blindness around the world, which is mainly mediated by oxidative stress.

Objective: N-trimethyl chitosan (TMC)-coated liposomes of cyanidin-3-glycoside (C3G) (C3G-TCL) were prepared to attenuate oxidative stress induced by selenite sodium in rats.

Materials and methods: C3G-TCL were prepared by reverse-phase evaporation method and then coated with self-synthesized TMC. The physicochemical properties were determined. A gamma-scintigraphy study was employed to evaluate the precorneal elimination of the radioactive preparations. The transcorneal visualization for fluorescence-labeled samples was determined by confocal laser scanning microscopy (CLSM). The in vivo anti-oxidative study using C3G-TCL was carried out in rats with selenite-induced cataracts by topical administration.

Results: The sphere-like morphological characterization of the vesicles was confirmed by TEM, with a size of 158.3 ± 2.8 nm and a zeta potential of 31.7 mV. The encapsulation efficiency was (53.7 ± 0.2) % as measured by ultrafiltration. C3G-TCL showed a 3.3-fold increment in precorneal residence time when compared with that of the ^99mTc-solution. A TMC coating enhanced the transepithelial transport of liposomes to a depth of 40-μm in the cornea. Moreover, C3G-TCL could significantly elevate the activity of superoxide dismutase and catalase in lens and also show a considerable reversal of reduced glutathione activity. The lipid peroxidation in lens was strongly prevented when compared with that of groups treated with uncoated C3G-loaded liposomes.

Discussion and conclusion: The coating material TMC for liposomes helps improve the anti-oxidative effect of C3G in vivo through prolonged residence time on the cornea and improved permeability in the corneal epithelium.

• Cyanidin-3-glycoside
• N-trimethyl chitosan
• oxidative stress
• precorneal residence time
• transcorneal permeability

Acknowledgements

The authors thank Andrew Satterlee for editing the manuscript.

Declaration of interest

The authors report no declarations of interest. The authors thank the National Natural Science Fund of China (No. 81202927), the Natural Science Fund of Jiangxi Province (20151BAB215040), the Research program of Traditional Chinese Medicine of Jiangxi Provincial Health Department (2012A160 and 2014A018), the Youth Foundation of Jiangxi Provincial Education Department (GJJ12535) and the Open fund of collaborative innovation center of Jiangxi University of Traditional Chinese Medicine (JXXT201403013) for financial support.