Formulation and Optimization of Quercetin Loaded Nanosponges Topical Gel: Ex Vivo, Pharmacodynamic and Pharmacokinetic Studies

Abstract

Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug.
 Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies.
 Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation.
 Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

β-Cyclodextrin-Based Nanosponges Inclusion Compounds Associated with Gold Nanorods for Potential NIR-II Drug Delivery

“…Figure 10 depicts the thermograms of MPH, CUR, NSs, NSs–MPH, and NSs–CUR. NSs exhibit an endothermic peak at 350 °C, representing the melting point of the crosslinked polymer, as reported previously [ 43 , 58 , 59 ]. DSC thermogram of MPH shows a sharp endothermic peak at around 203 °C, corresponding to the melting point of the free drug [ 60 ].…”

Loxoprofen Nanosponges: Formulation, Characterization and Ex-Vivo Study

“…Accurately weighed 10 mg of the formulation was added to 60 ml distilled water and stirred using a magnetic stirrer (Magnetic Stirrer Hot Plate: Prolabo: France) at 1000 rpm for 15 min then filtered. The absorbance of the filtrate was measured spectrophotometrically at the predetermined λmax and the concentration was calculated using the constructed calibration curve [16].…”

β-Cyclodextrin Nanosponges Inclusion Compounds Associated with Silver Nanoparticles to Increase the Antimicrobial Activity of Quercetin

“…Quercetin (3,3 ,4 ,5.7-pentahydroxyflavone) is a flavonoid compound widely present in plants, exhibiting antioxidant and antibacterial properties. Despite its broad biological properties, quercetin (QRC) use in pharmaceutics is minimal due to its low aqueous solubility and photodegradation [16][17][18]. Regarding these disadvantages, NSs can form inclusion compounds through host-guest interactions with different molecules [19][20][21].…”