title: Multifunctional biocompatible and biodegradable folic acid conjugated poly(ε-caprolactone)-polypeptide copolymer vesicles with excellent antibacterial activities.
abstract: Cancer patients after chemotherapy may also suffer bacterial attack due to badly decreased immunity. Although with high bacterial efficacy, conventional antibiotics are prone to inducement of drug resistance and may be not suitable for some cancer patients. In contrast, antibacterial peptides are highly effective in inhibiting bacteria without inducing resistance in pathogens. Presented in this article is a novel kind of highly effective antibacterial peptide-based biocompatible and biodegradable block copolymer vesicle. The copolymer is poly(ε-caprolactone)-block-poly[phenylalanine-stat-lysine-stat-(lysine-folic acid)] [PCL19-b-poly[Phe12-stat-Lys9-stat-(Lys-FA)6]], which can self-assemble into vesicles in aqueous solution. The biocompatible and biodegradable PCL forms the vesicle membrane, whereas the poly[Phe12-stat-Lys9-stat-(Lys-FA)6] block constitutes the vesicle coronas. Compared to the individual polymer chains, the vesicles showed enhanced antibacterial activities against both Gram-positive and Gram-negative bacteria (16 μg mL(-1)) due to the locally concentrated antibacterial poly[Phe12-stat-Lys9-stat-(Lys-FA)6] coronas, which may avoid the inducement of antibiotic-resistant bacteria and side effects of multidrug interactions. Furthermore, folic acid is introduced into the vesicle coronas for potential further applications such as cancer-targeted drug delivery. Moreover, the amino groups can be further functionalized when necessary. This low cytotoxic, biocompatible, biodegradable, and antibacterial vesicle (without antibiotic resistance) may benefit patients after tumor surgery because it is highly anti-inflammatory, and it is possible to deliver the anticancer drug to tumor cells simultaneously.
authors.affiliation: School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, China.
authors.forename: Mingzhi
authors.initials: M
authors.lastname: Wang
authors.affiliation: School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, China.
authors.forename: Chuncai
authors.initials: C
authors.lastname: Zhou
authors.affiliation: School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.affiliation: School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, China.
authors.forename: Yufen
authors.initials: Y
authors.lastname: Xiao
authors.affiliation: School of Materials Science and Engineering, Key Laboratory of Advanced Civil Engineering Materials of Ministry of Education, Tongji University, 4800 Caoan Road, Shanghai 201804, China.
authors.forename: Jianzhong
authors.initials: J
authors.lastname: Du
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D023181:Antimicrobial Cationic Peptides / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001672:Biocompatible Materials; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000494:pharmacology; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000494:pharmacology; D065546:Drug Liberation; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development; D005492:Folic Acid / Q000737:chemistry*; D022781:Hepatocytes / Q000187:drug effects / Q000473:pathology; D006801:Humans; D007700:Kinetics; D011091:Polyesters / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D013499:Surface Properties
chemical_list: D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D023181:Antimicrobial Cationic Peptides; D000970:Antineoplastic Agents; D001672:Biocompatible Materials; D004337:Drug Carriers; D011091:Polyesters; C016240:polycaprolactone; D004317:Doxorubicin; D005492:Folic Acid