title: Novel self-assembled pH-responsive biomimetic nanocarriers for drug delivery.
abstract: Novel pH-responsive biodegradable biomimetic nanocarriers were prepared by the self-assembly of N-acetyl-l-histidine-phosphorylcholine-chitosan conjugate (NAcHis-PCCs), which was synthesized via Atherton-Todd reaction to couple biomembrane-like phosphorylcholine (PC) groups, and N,N'-carbonyldiimidazole (CDI) coupling reaction to link pH-responsive N-acetyl-l-histidine (NAcHis) moieties to chitosan. In vitro biological assay revealed that NAcHis-PCCs nanoparticles had excellent biocompatibility to avoid adverse biological response mainly owing to their biomimetic PC shell, and DLS results confirmed their pH-responsive behavior in acidic aqueous solution (pH≤6.0). Quercetin (QUE), an anti-inflammatory, antioxidant and potential anti-tumor hydrophobic drug, was effectively loaded in NAcHis-PCCs nanocarriers and showed a pH-triggered release behavior with the enhanced QUE release at acidic pH5.5 compared to neutral pH7.4. The results indicated that pH-responsive biomimetic NAcHis-PCCs nanocarriers might have great potential for site-specific delivery to pathological acidic microenvironment avoiding unfavorable biological response.
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Minming
authors.initials: M
authors.lastname: Wu
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Zhaoyu
authors.initials: Z
authors.lastname: Cao
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Yunfei
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China. Electronic address: tzengronga@jnu.edu.cn.
authors.forename: Rong
authors.initials: R
authors.lastname: Zeng
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Mei
authors.initials: M
authors.lastname: Tu
authors.affiliation: Department of Materials Science and Engineering, College of Science and Engineering, Jinan University, Guangzhou 510632, PR China.
authors.forename: Jianhao
authors.initials: J
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D040761:Biomimetic Materials / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D048271:Chitosan / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D006639:Histidine / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010767:Phosphorylcholine / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D010767:Phosphorylcholine; D006639:Histidine; D048271:Chitosan; C023495:N-acetylhistidine
keywords: Biomimetic; Chitosan; Controlled release; Nanocarriers; pH-responsive