Preparation and Antitumor Effect of N-Trimethylchitosan/Fucoidan Ion-Complex Submicron Particles

Abstract

The aim of this study was to develop a delivery system to enable the promotion of the antitumor potential of fucoidan (FUC). FUC/N-trimethylchitosan (TMC) ion-complex submicron particles (FUC/TMC-SMP) were produced by ionic complexation, and their particle characteristics were investigated. Antitumor effect was examined in vivo using sarcoma 180-bearing mice by oral administration, and body weight loss was checked as an index of toxic side effects. FUC/TMC-SMP could be obtained by the complexation of negatively charged fucoidan with positively charged N-trimethylchitosan under aqueous conditions. The mean particle size was 325 nm and mean FUC content was 47 % (w/w). Oral administration was conducted using two treatment schedules, that is, pre-and post-tumor inoculation. As to pre-treatment, oral administration was performed from 13 days before inoculation to 1 day before inoculation every other day. For post-treatment, preparation samples were administered orally from 1 day after inoculation to 13 days after inoculation every other day. FUC/TMC-SMP were more effective than FUC solution and suppressed tumor growth significantly in both treatment schedules. FUC/TMC-SMP are suggested to be a useful oral delivery system enhancing the antitumor potential of FUC.

Preparation and Evaluation of Enteric-Coated Chitosan Derivative-Based Microparticles Loaded with Salmon Calcitonin as an Oral Delivery System

“…The ratio of the N -trimethyl group in TMC was examined based on the proton nuclear magnetic resonance (NMR) spectra which were obtained using D 2 O and 1% ( v/v ) CD 3 COOD in D 2 O as solvents. As the details of the signal assignment had been reported before [ 32 ], the proton signal found at a 0.9 ppm low magnetic field against the HDO proton signal was assigned as the protons of N + (CH 3 ) 3 , which was based on the report by Sieval et al [ 22 ]. The substitution degree was calculated by comparing the integrated intensity of the N -trimethyl proton signal (3.7–3.8 ppm) with that of the C1 proton signal (4.8–6 ppm).…”

“…The chemical structure of TMC obtained was examined by 1 H-NMR spectroscopy, in which a JNM-LA500 (JEOL, Tokyo, Japan) was used as an NMR spectrometer and measurements were performed at 80 °C using D 2 O and 1% CD 3 COOD in D 2 O as solvents. The degree of N -trimethylation was calculated based on 1 H-NMR spectra; the substitution degree was obtained from the ratio of the integrated intensity of N -trimethyl group protons (3.7–3.8 ppm) to that of the C1 proton (4.8–6 ppm) of the glucosamine unit of Ch [ 22 , 32 ].…”

Characterization of Methotrexate Loaded Fucoidan/Chitosan Nanoparticles

“…Usually, SEM-analyzed nanoparticles are aggregated by several dozen smaller particles, irregular in form and differ in mean dimension. Other particles such as FUC / TMC / TPP-MP incorporate easily simpli ied content due to the strong interaction of the positive charge of TMC and the negative charge of TPP and FUC (Hayashi et al, 2011). SEM is also used to analyse the surface morphology, pore distribution and pore size in studies related to bone tissue engineering.…”