Galactosylated Chitosan Coated Liposomes of Ledipasvir for Liver Targeting: Chemical Synthesis,Statistical Optimization,In-vitro and In-vivo evaluation期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

按检索

Galactosylated Chitosan Coated Liposomes of Ledipasvir for Liver Targeting: Chemical Synthesis,Statistical Optimization,In-vitro and In-vivo evaluation

Authors:	Ahmed M Fatouh Ahmed H Elshafeey Ahmed Abdelbary

Institution:	Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Abstract:	Ledipasvir is a novel antiviral agent used in the treatment of hepatitis C. We aim in our study to increase its delivery to hepatocytes and prolong its retention within liver. Several formulae of ledipasvir loaded liposomes were prepared and the best formula regarding particle size, zeta potential, polydispersity index and entrapment efficiency was selected. On the other hand, galactosylated chitosan was synthesized in a chemical reaction. Then the best liposomes formula was coated with the galactosylated chitosan. Having galactose residues on their surface, the coated liposomes can bind to the asialoglycoprotein receptors on the targeted hepatocytes enhancing ledipasvir uptake into them. The galactosylated chitosan coated liposomes had particle size of 218.2 nm ± 7.21, zeta potential of 27.15 mV ± 1.76, polydispersity index of 0.278 ± 0.055 and entrapment efficiency % of 54.63% ± 0.05 respectively. The pharmacokinetic study revealed a significant increase in the liver peak concentration (C_max) and the area under liver concentration versus time curve AUC_(0–72 h) and significant prolongation in the liver terminal half life (t½) and mean residence time (MRT) in comparison to the oral dispersion of ledipasvir with values of 11,400 ng/g, 88,855 ng1h/g, 32.00 h and 18.11 h respectively.

Keywords:	Liposomes Targeted drug delivery Pharmacokinetics ASGPRs"} {"#name":"keyword" "$":{"id":"kwrd0030"} "$$":[{"#name":"text" "_":"asialoglycoprotein receptors AUC"} {"#name":"keyword" "$":{"id":"kwrd0040"} "$$":[{"#name":"text" "_":"area under curve CHL"} {"#name":"keyword" "$":{"id":"kwrd0050"} "$$":[{"#name":"text" "_":"cholesterol maximum concentration DAA"} {"#name":"keyword" "$":{"id":"kwrd0070"} "$$":[{"#name":"text" "_":"direct acting agents EDC"} {"#name":"keyword" "$":{"id":"kwrd0080"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"N"} {"#name":"__text__" "_":"-(3- dimethylaminopropyl) -"} {"#name":"italic" "_":"N"} {"#name":"__text__" "_":"-ethylcarbodiimide hydrochloride EE"} {"#name":"keyword" "$":{"id":"kwrd0090"} "$$":[{"#name":"text" "_":"entrapment efficiency FTIR"} {"#name":"keyword" "$":{"id":"kwrd0100"} "$$":[{"#name":"text" "_":"Fourier transform infrared Gal"} {"#name":"keyword" "$":{"id":"kwrd0110"} "$$":[{"#name":"text" "_":"galactose GC"} {"#name":"keyword" "$":{"id":"kwrd0120"} "$$":[{"#name":"text" "_":"galactosylated chitosan HCV"} {"#name":"keyword" "$":{"id":"kwrd0130"} "$$":[{"#name":"text" "_":"hepatitis C virus HNMR"} {"#name":"keyword" "$":{"id":"kwrd0140"} "$$":[{"#name":"text" "_":"proton nuclear magnetic resonance LA"} {"#name":"keyword" "$":{"id":"kwrd0150"} "$$":[{"#name":"text" "_":"lactobionic acid LC"} {"#name":"keyword" "$":{"id":"kwrd0160"} "$$":[{"#name":"text" "_":"lecithin LDV"} {"#name":"keyword" "$":{"id":"kwrd0170"} "$$":[{"#name":"text" "_":"ledipasvir MRT"} {"#name":"keyword" "$":{"id":"kwrd0180"} "$$":[{"#name":"text" "_":"mean residence time NHS"} {"#name":"keyword" "$":{"id":"kwrd0190"} "$$":[{"#name":"text" "$$":[{"#name":"italic" "_":"N"} {"#name":"__text__" "_":"-hydroxysuccinimide PDI"} {"#name":"keyword" "$":{"id":"kwrd0200"} "$$":[{"#name":"text" "_":"polydispersity index PS"} {"#name":"keyword" "$":{"id":"kwrd0210"} "$$":[{"#name":"text" "_":"particles size Re"} {"#name":"keyword" "$":{"id":"kwrd0220"} "$$":[{"#name":"text" "_":"relative uptake rate SAA"} {"#name":"keyword" "$":{"id":"kwrd0230"} "$$":[{"#name":"text" "_":"surface active agent TEMED"} {"#name":"keyword" "$":{"id":"kwrd0240"} "$$":[{"#name":"text" "_":"N N N′ N″- tetramethylethylenediamine TEM"} {"#name":"keyword" "$":{"id":"kwrd0250"} "$$":[{"#name":"text" "_":"transmission electron microscopy time to reach maximum conc half life ZP"} {"#name":"keyword" "$":{"id":"kwrd0280"} "$$":[{"#name":"text" "_":"zeta potential
本文献已被 ScienceDirect 等数据库收录！

设为首页 | 免责声明 | 关于勤云 | 加入收藏