title: Ocular delivery of cyanidin-3-glycoside in liposomes and its prevention of selenite-induced oxidative stress.
abstract: BACKGROUND
  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.
  
  
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China .
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.affiliation: a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China .
authors.forename: Xinli
authors.initials: X
authors.lastname: Liang
authors.affiliation: b National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China , and.
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.affiliation: c School of Pharmacy, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China.
authors.forename: Zhiyu
authors.initials: Z
authors.lastname: Guan
authors.affiliation: a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China .
authors.forename: Zhenggen
authors.initials: Z
authors.lastname: Liao
authors.affiliation: a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China .
authors.forename: Yun
authors.initials: Y
authors.lastname: Luo
authors.affiliation: a Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine , Nanchang , Jiangxi , P.R. China .
authors.forename: Yunxia
authors.initials: Y
authors.lastname: Luo
mesh_terms: D000818:Animals; D000872:Anthocyanins / Q000008:administration & dosage* / Q000378:metabolism; D003315:Cornea / Q000187:drug effects* / Q000378:metabolism; D004337:Drug Carriers / Q000008:administration & dosage / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D006027:Glycosides / Q000008:administration & dosage* / Q000378:metabolism; D008081:Liposomes; D018384:Oxidative Stress / Q000187:drug effects* / Q000502:physiology; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D020887:Selenious Acid / Q000037:antagonists & inhibitors / Q000633:toxicity*
chemical_list: D000872:Anthocyanins; D004337:Drug Carriers; D006027:Glycosides; D008081:Liposomes; C000597824:cyanidin-3-glycoside; D020887:Selenious Acid
keywords: Cyanidin-3-glycoside; N-trimethyl chitosan; oxidative stress; precorneal residence time; transcorneal permeability