access icon free Synthesis of biotin-targeted chitosan/poly (methyl vinyl ether-alt-maleic acid) copolymeric micelles for delivery of doxorubicin

© The Institution of Engineering and Technology
Received 24/11/2016, Accepted 26/05/2017, Revised 30/04/2017, Published 16/06/2017

Biotinylated chitosan/poly(methyl vinyl ether-alt-maleic acid) (PMVEMA) copolymer was synthesised by an amide reaction in two steps. Structural characterisation was performed using 1HNMR and Fourier transform infra-red (FTIR) spectra. Critical micelle concentration (CMC) of the copolymer was determined by pyrene as a fluorescent probe. Doxorubicin (DOX) was loaded in the micelles by the direct dissolution method. The effects of different variables including type of copolymer, copolymer concentration, stirring rate and stirring time were studied on the physicochemical properties of the micelles including: particle size, zeta potential, release efficiency and loading efficiency of nanoparticles using an irregular factorial design. The in vitro cytotoxicity of DOX-loaded biotin-targeted micelles was studied in HepG2 cells which over express biotin receptors by 3, 5-[dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide assay. The successful synthesis of the biotinylated copolymer of chitosan/PMVEMA was confirmed by FTIR and 1HNMR. The optimised micelles showed the CMC of 33 μg/ml, particle size of 247 ± 2 nm, zeta potential of +9.46 mV, polydispersity index of 0.22, drug-loading efficiency of 71% and release efficiency of 84.5 ± 1.6%. The synthesised copolymer was not cytotoxic. The cytotoxicity of DOX-loaded in targeted micelles on HepG2 cell line was about 2.2-fold compared with free drug.

Inspec keywords: drugs; drug delivery systems; polymer blends; toxicology; dissolving; electrokinetic effects; Fourier transform infrared spectra; biomedical materials; fluorescence; particle size; spectrochemical analysis; cellular biophysics

Other keywords: structural characterisation; DOX-loaded biotin-targeted micelles; direct dissolution method; doxorubicin delivery; voltage 9.46 mV; drug-loading efficiency; physicochemical properties; amide reaction; in vitro cytotoxicity; HepG2 cell line; irregular factorial design; polydispersity index; zeta potential; 1HNMR spectra; biotin-targeted chitosan-poly (methyl vinyl ether-alt-maleic acid) copolymeric micelles; particle size; fluorescent probe; 3, 5-[dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide assay; nanoparticles; pyrene; Fourier transform infrared spectra

Subjects: Electromagnetic radiation spectrometry (chemical analysis); Biomedical materials; Electrochemistry and electrophoresis; Cellular biophysics; Patient care and treatment

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