Poly(n-butylcyanoacrylate) nanoparticles for oral delivery of quercetin: preparation, characterization, and pharmacokinetics and biodistribution studies in Wistar rats

Abstract

Background Quercetin (QT) is a potential bioflavonol and antioxidant with poor bioavailability and very low distribution in the brain. A new oral delivery system comprising of poly(n-butylcyanoacrylate) nanoparticles (PBCA NPs) was introduced to improve the oral bioavailability of QT and to increase its distribution in the brain. Physicochemical characteristics, in vitro release, stability in simulated gastric fluid and intestinal fluids, and pharmacokinetics and biodistribution studies of QT-PBCA NPs coated with polysorbate-80 (P-80) were investigated. Objective This study aimed to investigate the physicochemical characteristics, in vitro release, stability in simulated gastric fluid and intestinal fluids, and pharmacokinetics and biodistribution studies of QT-PBCA NPs coated with polysorbate-80 (P-80). Results The results showed that QT-PBCA NPs and QT-PBCA NPs coated with P-80 (QT-PBCA+P-80) had mean particle sizes of 161.1±0.44 nm and 166.6±0.33 nm respectively, and appeared spherical in shape under transmission electron microscopy. The mean entrapment efficiency was 79.86%±0.45% for QT-PBCA NPs and 74.58%±1.44% for QT-PBCA+P-80. The in vitro release of QT-PBCA NPs and QT-PBCA+P-80 showed an initial burst release followed by a sustained release when compared to free QT. The relative bioavailability of QT-PBCA NPs and QT-PBCA+P-80 enhanced QT bioavailability by 2.38- and 4.93-fold respectively, when compared to free QT. The biodistribution study in rats showed that a higher concentration of QT was detected in the brain after the NPs were coated with P-80. Conclusion This study indicates that PBCA NPs coated with P-80 can be potential drug carriers for poorly water-soluble drugs. These NPs were observed to improve the drugs’ oral bioavailability and enhance their transport to the brain.

Retracted Article: Organometallic Ag nanostructures prepared usingHypericum perforatumextract are highly effective against multidrug-resistant bacteria

“…46,47 NS carrying quercetin used in drug delivery have also displayed a typical diffraction peak at 27 when observed by XRD. 48 During the crystal growth of Ag, some higher-energy Ag ions were rapidly and individually captured by phytoreductants, which resulted in the creation of smaller organometallic clusters embedded between the crystal planes of OM-Ag-NS. The diffraction peaks also indicate the high degree of reactivity and affinity of the phytochelating agents (such as avonoids and phenolic acid derivatives) in H. perforatum extract.…”

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.…”

Using superparamagnetic iron oxide nanoparticles to enhance bioavailability of quercetin in the intact rat brain

“…Quercetin (3,3′,4′,5,7-pentahydroxyflavone, (QT)) is an active biological flavonoid found in large quantities in edible fruits, vegetables and medicinal plants such as onions, cabbage, and apples [ 17 – 19 ]. Quercetin has antiinflammatory [ 20 ], antioxidant [ 21 ], anti-cancer [ 22 ], anti-viral [ 23 ], and anti-ischemic effects [ 24 , 25 ].…”

“…Neuronal protection of QT has been reported in both in vitro and in vivo investigations [ 27 – 31 ]. Therefore, QT has a potential therapeutic for various neuronal injuries and neurodegenerative diseases [ 19 ]. However, the solubility of QT in water is low and it has a short biological half-life.…”