Jing Zhang1, Xinli Liang1, Xiang Li2, Zhiyu Guan3, Zhenggen Liao1, Yun Luo1, Yunxia Luo1. 1. a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China . 2. b National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China , and. 3. c School of Pharmacy, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China.
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 (99m)Tc-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.
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 (99m)Tc-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.