title: Surface charge effect on mucoadhesion of chitosan based nanogels for local anti-colorectal cancer drug delivery.
abstract: To develop more effective anticancer mucoadhesive drug delivery system for the treatment of colorectal cancer, chitosan based nanogels (NGs) were prepared by electrostatic interaction between chitosan (CS) and carboxymethyl-chitosan (CMCS). By respectively using tripolyphosphate (TPP) and CaCl2 as ionic crosslinker, two well-characterized doxorubicin hydrochloride (DOX) loaded NGs with opposite zeta potential (DOX:CS/CMCS/TPP NGs, -32.6±1.1 mV and DOX:CS/CMCS/Ca2+ NGs, +31.8±0.9 mV) were obtained. Compared with DOX:CS/CMCS/TPP NGs, DOX:CS/CMCS/Ca2+ NGs were taken up to a greater extent by colorectal cancer cells, resulting in greater reduction in percentage of cell viability. Owing to high binding capability to mucin and inhibited paracellular transport by colon, DOX:CS/CMCS/Ca2+ NGs exhibited improved mucoadhesion and limited permeability. This is beneficial to prolong the contact time of formulation onto intestinal mucosa and improved local drug concentration. The results provided evidence DOX:CS/CMCS/Ca2+ NGs to be exciting and promising for the treatment of colorectal cancer.
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China. Electronic address: fengchao@ouc.edu.cn.
authors.forename: Chao
authors.initials: C
authors.lastname: Feng
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China.
authors.forename: Ming
authors.initials: M
authors.lastname: Kong
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China.
authors.forename: Ya
authors.initials: Y
authors.lastname: Liu
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China.
authors.forename: Xiao Jie
authors.initials: XJ
authors.lastname: Cheng
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.affiliation: Graduate School of Biotechnology, Korea University, 1,5-Ka, Anam-Dong, Sungbuk-Ku, Seoul 136-701, South Korea.
authors.forename: Hyun Jin
authors.initials: HJ
authors.lastname: Park
authors.affiliation: College of Marine Life Science, Ocean University of China, Qingdao 266003, PR China. Electronic address: xgchen@ouc.edu.cn.
authors.forename: Xi Guang
authors.initials: XG
authors.lastname: Chen
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000494:pharmacology*; D001692:Biological Transport; D018938:Caco-2 Cells; D002122:Calcium Chloride / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000031:analogs & derivatives* / Q000737:chemistry*; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers; D004339:Drug Compounding; D065546:Drug Liberation; D005782:Gels; D006801:Humans; D007700:Kinetics; D009077:Mucins / Q000737:chemistry; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry; D055672:Static Electricity; D013499:Surface Properties
chemical_list: D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D005782:Gels; D009077:Mucins; D011122:Polyphosphates; C514968:carboxymethyl-chitosan; D004317:Doxorubicin; D048271:Chitosan; D002122:Calcium Chloride; C005692:triphosphoric acid
keywords: Cellular uptake; Chitosan; Colorectal cancer; Mucoadhesion; Nanogels