Intensification of quercetin nanobubble formulation and performance by multi-factor optimization and interaction analysis
Creators: name: A.V., Hema Kumar
name: Kantlam, Chamakuri
Publisher: name: Taylor & Francis
Year: 2024
Subjects: Biophysics
Biochemistry
Space Science
Medicine
Pharmacology
Biotechnology
Chemical Sciences not elsewhere classified
Biological Sciences not elsewhere classified

description: The natural flavonoid Quercetin (QT) showed a potential for various health benefits, but its pharmaceutical applications are hindered by low solubility, permeability, and limited bioavailability. This research aimed to synthesize, develop and optimize polylactic acid co-glycolic acid (PLGA) nanobubbles using solvent evaporation method as a sustained delivery system for QT, thus improving stability and bioavailability. Through a four-factor, three-level Box Behnken Design, 29 experimental runs were carried out to optimize QT-PLGA nanobubbles. An optimized formulation consisted of 50 mg QT, 250 mg PLGA, and 1.89% <i>w/v</i> PVA. The nanobubbles displayed a particle size of 139.5 ± 6.24 nm, polydispersity index of 0.296 ± 0.19, and zeta potential of −23.0 ± 3.44 mV, with an entrapment efficiency of 59.24 ± 3.08%. Analysis through Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction confirmed no drug-polymer interaction, while scanning electron microscopy revealed a uniform spherical nanoparticle. <i>In vitro</i> studies exhibited an excellent drug release, and stability studies showed no significant changes after one month. <i>In vivo</i> studies in rats demonstrated increased <i>C</i><sub>max</sub> (3.03) and <i>AUC</i><sub>0–t</sub> (5.84), indicating an improved sustained release and absorption. These findings underscored a potential of QT-loaded PLGA nanobubbles to enhance the drug kinetics and bioavailability, offering possibilities for targeted drug delivery and improved therapeutic outcomes. Quercetin is one of the most effective flavonoids with many therapeutic applications but undergoes first-pass metabolism when ingested orally.It faces obstacles when used widely in pharmaceuticals due to its limited solubility in water, inadequate permeability, and vulnerability to instability in physiological fluids.These degradation processes can result in the loss of quercetin potency and effectiveness over time. Encapsulation or suitable formulation strategies can be employed to enhance the drug stability and shelf-life.The utilization of nanobubbles offers a ground breaking strategy to improve the pharmaceutical products through prolonged release and precise drug targeting. The implementation of nanobubbles substantially enhanced the bioavailability of quercetin. Quercetin is one of the most effective flavonoids with many therapeutic applications but undergoes first-pass metabolism when ingested orally. It faces obstacles when used widely in pharmaceuticals due to its limited solubility in water, inadequate permeability, and vulnerability to instability in physiological fluids. These degradation processes can result in the loss of quercetin potency and effectiveness over time. Encapsulation or suitable formulation strategies can be employed to enhance the drug stability and shelf-life. The utilization of nanobubbles offers a ground breaking strategy to improve the pharmaceutical products through prolonged release and precise drug targeting. The implementation of nanobubbles substantially enhanced the bioavailability of quercetin.