Quercetin‐encapsulated magnetoliposomes: Fabrication, optimization, characterization, and antioxidant studies

Abstract

Quercetin (QU) faces challenges in its therapeutic efficacy due to its hydrophobic nature and limited oral bioavailability. Using a Box–Behnken design (BBD) approach, we developed QU‐loaded magnetoliposomes (QMLs) to address these limitations. By encapsulating QU within iron oxide nanoparticles (IONPs) and liposomes (LPs), we enhanced its hydrophilicity and improved its potential for drug delivery. Through systematic adjustments of phosal, polyvinyl alcohol, and magnetic/IONPs, we optimized the particle size, zeta potential, and iron content of the QMLs. The formulations underwent comprehensive structural characterization using techniques, such as Fourier transform infrared spectroscopy, X‐Ray diffraction, differential scanning calorimetry–thermogravimetric analysis, and energy‐dispersive X‐ray analysis, whereas their morphology was examined through field emission scanning electron microscopy. Furthermore, we evaluated the in vitro drug release of the QMLs and antioxidant activity of QU, QU‐loaded LPs, and QMLs using DPPH, 2,2′‐azino‐bis(3‐ethylbenzthiazoline‐6‐sulfonic acid), and H2O2 scavenging assays, enabling us to compare their antioxidant potential and the efficiency of QU encapsulation within the magneto LPs.Practical Application: This research holds significant practical implications, particularly in targeted drug delivery using magnetic liposomes. The developed system shows promise in enhancing cancer therapy, providing localized treatment for inflammation‐related conditions, delivering drugs to the brain to address neurological disorders, promoting wound healing, and incorporating quercetin into skincare products for its antioxidant and antiaging benefits.

Intranasal Delivery of Carvedilol- and Quercetin-Encapsulated Cationic Nanoliposomes for Cardiovascular Targeting: Formulation and In Vitro and Ex Vivo Studies

“…Peaks at 962 and 840 (sharp) and 717 and 635 cm –1 are indicative of aromatic hydrocarbon out-of-plane C–H bending with % transmittance of 81.19, 76.99, 85, and 84.61%. Kar et al reported similar peaks regarding IR spectra of QC at 3392 and 1372 cm –1 for −OH stretching and bending, 1564 cm –1 for aromatic ring, 1094 and 1009 cm –1 for C–O stretching vibrations, 1162 cm –1 for C–CO–C stretching, and 1658 cm –1 for ketone and CO bands bending . Similar outcomes for the QC IR spectra were also reported by Rajamohan et al, with characteristics peaks at 1379 cm –1 for −OH phenolic bending, 1666 cm –1 for −CO stretching, 1610, 1560, and 1510 cm –1 for CC aromatic stretching, 933, 820, 679, and 600 cm –1 for C–H bending in aromatic hydrocarbon (out-of-plane), 1263 cm –1 for C–O stretching in aryl ether ring, and 1165 cm –1 for C–CO–C stretching and bending in ketone .…”

“…It shows a total weight loss of 99.787% (0.938 mg) from 28 to 492 °C. Such a distinct endothermic peak of pure QC was also reported by Kar et al at 321 °C implying the crystalline nature of drug QC. A moisture peak above 100 °C, that is, greater than its boiling temperature, indicates strong hydrogen bonding between the water and QC crystals.…”

“…Kar et al reported similar peaks regarding IR spectra of QC at 3392 and 1372 cm −1 for −OH stretching and bending, 1564 cm −1 for aromatic ring, 1094 and 1009 cm −1 for C−O stretching vibrations, 1162 cm −1 for C−CO−C stretching, and 1658 cm −1 for ketone and C�O bands bending. 23 Similar outcomes for the QC IR spectra were also reported by Rajamohan et al, with characteristics peaks at 1379 cm −1 for −OH phenolic bending, 1666 cm −1 for −C�O stretching, 1610, 1560, and 1510 cm −1 for C�C aromatic stretching, 933, 820, 679, and 600 cm −1 for C−H bending in aromatic hydrocarbon (out-of-plane), 1263 cm −1 for C−O stretching in aryl ether ring, and 1165 cm −1 for C−CO−C stretching and bending in ketone. 56 The IR peaks of blank NLPs (without any loaded drug) exhibit distinctive peaks at 3383 cm −1 , which are indicative of −OH or �CH or N−H wide peaks with a transmittance of 92.27%.…”

“…Figure a–I illustrate the surface characteristics of the drug and formulation. Figure a–c reveals the crystalline nature or the presence of crystalline particles of pure QC, which corresponds with the outcome reported by ref with similar structural features. The FESEM micrographs of the developed CVD/QC-loaded cationic NLPs (Figure d–f) show spherical structures of nanoliposomes at different resolutions.…”

“…Quercetin (QC) [2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-1-benzopyran-4-one], a potential polyphenolic compound (flavonol), is widely available in apples, onions, citrus fruits, blueberries, red wine, broccoli, and tea. QC exhibits various pharmacological activities including the following: antioxidant, anti-inflammatory, cardio-protective, antihypertensive, antiviral, anticancer, antileishmanial activity, and neurodegenerative. − QC is also a hydrophobic drug with very low oral bioavailability (less than 17% in rats and about 1% in humans); therefore, to enhance the solubility and bioavailability, it is essential to develop a stable nanocarrier system incorporating QC . Hence, it is essential to develop a novel nanocarrier system for the delivery of CVD and QC to improve their bioavailability, stability, intracellular uptake, and therapeutic efficacy synergistically with enhanced circulation time and reduced undesirable side effects.…”