title: Targeting delivery of Radix Ophiopogonis polysaccharide to ischemic/reperfused rat myocardium by long-circulating macromolecular and liposomal carriers.
abstract: Drug delivery to ischemic myocardium is an enormous challenge. This work aimed to characterize cardiac delivery behaviors of mono-polyethylene glycosylated (PEGylated) conjugates and long-circulating liposomes (L-Lps) with Radix Ophiopogonis polysaccharide (ROP) as drug. The results showed that compared to native ROP, 32-, 52-, and 45-fold increases in blood half-life were achieved by 20-kDa PEG mono-modified ROP (P(20k)-R), 40-kDa PEG mono-modified ROP (P(40k)-R), and ROP-loaded L-Lp, respectively. With comparable blood pharmacokinetics, ROP-loaded L-Lp showed both significantly higher targeting efficacy and drug exposure in infarcted myocardium than P(40k)-R. With regard to P(20k)-R, both its targeting efficacy and its level in infarcted myocardium at 3 hours postdose were comparable to P(40k)-R, but its level in blood and myocardium reduced obviously faster. As a whole, the results indicate that both loading in L-Lps and mono-PEGylation are effective in targeting drug to ischemic myocardium, but the former appears to induce stronger effects.
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China ; Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: LiNa
authors.initials: L
authors.lastname: Wang
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: ChunXia
authors.initials: C
authors.lastname: Yao
authors.affiliation: Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: Fei
authors.initials: F
authors.lastname: Wu
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China ; Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lin
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: Lan
authors.initials: L
authors.lastname: Shen
authors.affiliation: Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Feng
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D008081:Liposomes / Q000737:chemistry*; D046911:Macromolecular Substances / Q000737:chemistry; D008297:Male; D009203:Myocardial Infarction / Q000188:drug therapy*; D031441:Ophiopogon / Q000737:chemistry*; D018517:Plant Roots / Q000187:drug effects; D011134:Polysaccharides / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D046911:Macromolecular Substances; D011134:Polysaccharides
keywords: PEGylation; Radix Ophiopogonis polysaccharide; fluorescent imaging; liposome; myocardial targeting