Application of pH-Responsive Fucoidan/Chitosan Nanoparticles to Improve Oral Quercetin Delivery

Abstract

Polymeric nanoparticles based on fucoidan and chitosan were developed to deliver quercetin as a novel functional food. Through the polyelectrolyte self-assembly method, fucoidan/chitosan (F/C) nanoparticles were obtained with three different weight ratios (1/1, 3/1, and 5/1). The content of quercetin in the fucoidan/chitosan nanoparticles was in the range 110 ± 3 to 335 ± 4 mg·mL−1, with the increase of weight ratio of fucoidan to chitosan in the nanoparticle. Physicochemically stable nanoparticles were obtained with a particle size within the 300–400 nm range and surface potential higher than +30 mV for the 1F/1C ratio nanoparticle and around −30 mV for the 3F/1C and 5F/1C ratios nanoparticles. The 1F/1C ratio nanoparticle became larger and more unstable as the pH increased from 2.5 to 7.4, while the 3F/1C and 5F/1C nanoparticles retained their initial characteristics. This result indicates that the latter nanoparticles were stable along the gastrointestinal tract. The quercetin-loaded fucoidan/chitosan nanoparticles showed strong antioxidant activity and controlled release under simulated gastrointestinal environments (in particular for the 3F/1C and 5F/1C ratios), preventing quercetin degradation and increasing its oral bioavailability.

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

“…Zhang et al [94] aimed to improve the oral absorption of baicalin, which has low solubility and poor permeability, by using a micellar formulation comprised of the carriers Pluronic P123 copolymer and sodium taurocholate. Sustained release profile of baicalin-loaded mixed micelles, in in vitro drug release experiment, held in several pH conditions, showed 14% drug released after 2 h in gastric conditions and 54% release within 48 h in intestinal conditions, compared to 34% and 79% release [105], nanoparticles [106][107][108][109][110], phytosome [111], nanoliposome [112], mixed micelles [113,114], SNEDDS [115,116], nanocarrier [117,118], nanoemulsion [119], nanosuspension [ Mixed micelles [129,130], nanoparticles [131,132], solid dispersion [133,134] , SNEDDS [135] , SMEDDS [136], lipid carrier [137], copolymeric micelles [138], exosomes [139] Naringenin DENV, HCV SNEDDS [140], solid dispersion [141], nanoparticles [142,143] , liposome [144], nanosuspension [145,146] In vitro uptake studies, carried out with a caco-2 cell line, determined the absorption of baicalin within the mixed micelles and verified their internalization ability. Baicalin-loaded ST-P123-MMs formulation achieved high oral bioavailability (Fig.…”

Marine Polysaccharides in Pharmaceutical Applications: Fucoidan and Chitosan as Key Players in the Drug Delivery Match Field

“…However, the pH-responsive profile of fucoidan-chitosan nanoparticles prevents degradation under acidic conditions of the gastrointestinal tract and allows drug absorption in the intestine. Hence, fucoidan-chitosan nanoparticles have been widely explored for oral delivery of active pharmaceutical ingredients [110,111,113,118,[123][124][125][126][127][128][129], also taking advantage of chitosan's property of increased contact with the mucus layer and consequently longer resistance times at the absorption site [129]. The biological properties of fucoidan described in Section 3.1.1 were explored by some authors to obtain synergic effects with a drug, for example, ciprofloxacin [117] or gemcitabine [126].…”

“…Moreover, the benefits of fucoidan-chitosan nanoparticles in polyphenols delivery by improving aqueous solubility and, consequently, oral bioavailability, led also to the development of nanostructures for the delivery of berberine, red ginseng, and quercetin [113,127,131]. Generally, these nanoparticles demonstrated their ability to control polyphenols release, retain biological activity, and prevent degradation.…”

“…Kim et al explored the bioactivity of fucoidan for improving the antithrombotic activity of red ginseng and demonstrated significant effects in vivo of the anticoagulation activity of fucoidan and significantly lower thrombus formation than free red ginseng [131]. A rationale based on different weight ratios of fucoidan and chitosan was applied to obtain pH-responsive nanoparticles to improve the oral bioavailability of quercetin [127]. Fucoidan-chitosan nanoparticles with higher amounts (3/1 and 5/1) of fucoidan from Fucus vesiculosus (M W 50-190 kDa, pKa 1.0-2.5) were resistant to the gastrointestinal pH environments and retained quercetin antioxidant activity.…”

Bioengineered ciprofloxacin loaded chitosan nanoparticles for the treatment of Bovine Mastitis

“…Antibiotics loaded nanocarriers offer great advantages over conventional therapy such as targeted delivery on disease site and controlled release of drug which help to maintain optimal concentration of drug at affected site [23]. The present studies show CPX encapsulated into a chitosan based nanocarrier able to release drug at physiological and acidic pH in controlled manner, which can overcome limitations of antibiotics treatments of mastitis in dairy animals[24].…”