title: Nanoparticles based on phenylalanine ethyl ester-alginate conjugate as vitamin B2 delivery system.
abstract: Phenylalanine ethyl ester (PAE)-alginate (Alg) conjugate (PAE-Alg, PEA) was synthesized and formation of an amide bond between PAE and Alg was confirmed by Fourier transformed-infrared and (1)H nuclear magnetic resonance spectroscopy. The degree of PAE substitution was 3.5-4.7 (PAE group per hundred sugar residues of Alg) which was determined by elemental analysis. The critical aggregation concentration values determined for PEA conjugates PEA1, PEA2, and PEA3 were 0.20, 0.12, and 0.10 mg/ml, respectively. The particle size of PEA nanoparticles (PEA-NPs) decreased from 425 nm to 226 nm with the increasing degree of PAE substitution. Vitamin B2 (VB2), as a model nutrient, was encapsulated into the nanoparticles. The drug-loading content increased with increasing degree of PAE substitution. The maximum VB2 loading capacity and loading efficiency of PEA3 nanoparticles were 3.53 ± 0.03% and 91.48 ± 0.80%, respectively. The in vitro release behavior of VB2 from the PEA-NPs showed a biphasic release profile with an initial burst release of about 40-50% of VB2 in the first 10 h followed by a steady and continuous release phase for the following 50 h in PBS, pH 7.4. The human colorectal carcinoma cell line was used to investigate the cytotoxicity of PEA-NPs. Our results showed that various concentrations of nanoparticles did not cause significant cytotoxicity against cell lines at normal concentrations.
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Pei
authors.initials: P
authors.lastname: Zhang
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Shi-Rui
authors.initials: SR
authors.lastname: Zhao
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Jun-Xia
authors.initials: JX
authors.lastname: Li
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Liang
authors.initials: L
authors.lastname: Hong
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Mazhar A
authors.initials: MA
authors.lastname: Raja
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China.
authors.forename: Le-Jun
authors.initials: LJ
authors.lastname: Yu
authors.affiliation: College of Marine Life Sciences, Ocean University of China, Qingdao, PR China liucg@ouc.edu.cn.
authors.forename: Chen-Guang
authors.initials: CG
authors.lastname: Liu
mesh_terms: D000464:Alginates / Q000737:chemistry* / Q000633:toxicity; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity; D004058:Diffusion; D016503:Drug Delivery Systems / Q000379:methods* / Q000592:standards; D020723:Glucuronic Acid / Q000737:chemistry / Q000633:toxicity; D006603:Hexuronic Acids / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D007700:Kinetics; D008422:Materials Testing; D053769:Nanocapsules / Q000737:chemistry* / Q000633:toxicity / Q000648:ultrastructure; D058726:Nanoconjugates / Q000008:administration & dosage* / Q000737:chemistry / Q000633:toxicity / Q000648:ultrastructure; D010316:Particle Size; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000633:toxicity; D012256:Riboflavin / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000464:Alginates; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; C505757:L-phenylalanine ethylester; D053769:Nanocapsules; D058726:Nanoconjugates; D010649:Phenylalanine; D020723:Glucuronic Acid; D012256:Riboflavin
keywords: Alginate; cytotoxicity; nanoparticles; phenylalanine ethyl ester; sustained release; vitamin B2