title: Surface Distribution and Biophysicochemical Properties of Polymeric Micelles Bearing Gemini Cationic and Hydrophilic Groups.
abstract: Polymeric micelles containing cationic gemini quaternary ammonium (GQA) groups have shown enhanced cellular uptake and efficient drug delivery, while the incorporation of poly(ethylene glycol) (PEG) corona can potentially reduce the absorption of cationic carriers by opsonic proteins and subsequent uptake by mononuclear phagocytic system (MPS). To understand the interactions of GQA and PEG groups and their effects on the biophysicochemical characteristics of nanocarriers, a series of polyurethane micelles containing GQA and different molecular weights of PEG were prepared and carefully characterized. It was found that the GQA and PEG groups are unevenly distributed on the micellar surface to form two kinds of hydrophilic domains. As a result, the particle surface with some defects cannot be completely shielded by the PEG corona. Despite this, the longer PEG chains with a brush conformation provide superior stabilization and steric repulsion against the absorption of proteins and, thus, can reduce the cytotoxicity, protein absorption, and MPS uptake of micelles to some extent. This study provides a new understanding on the interactions between PEG chains and cationic groups and a guideline for the design and fabrication of safe and effective drug delivery systems.
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Zhicheng
authors.initials: Z
authors.lastname: Pan
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Danxuan
authors.initials: D
authors.lastname: Fang
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Nijia
authors.initials: N
authors.lastname: Song
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Yuanqing
authors.initials: Y
authors.lastname: Song
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Mingming
authors.initials: M
authors.lastname: Ding
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Jiehua
authors.initials: J
authors.lastname: Li
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Luo
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Hong
authors.identifier: http://orcid.org/0000-0003-0695-1619
authors.initials: H
authors.lastname: Tan
authors.affiliation: College of Polymer Science and Engineering, State Key Laboratory of Polymer Materials Engineering, Sichuan University , Chengdu, Sichuan 610065, China.
authors.forename: Qiang
authors.identifier: http://orcid.org/0000-0002-2346-1171
authors.initials: Q
authors.lastname: Fu
mesh_terms: D001669:Biochemical Phenomena; D055598:Chemical Phenomena; D004337:Drug Carriers; D016503:Drug Delivery Systems; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D010316:Particle Size; D011092:Polyethylene Glycols; D013499:Surface Properties
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011092:Polyethylene Glycols
keywords: Gemini cation; PEG; cellular uptake; phagocytosis; polyurethane micelles; surface distribution