<p>This study aimed to develop luteolin-loaded mPEG-PCL polymeric micelles for improved neuroprotective delivery. A 3<sup>2</sup> factorial design yielded nine formulations, with F9 (15 mg/mL polymer, 1:20 drug-to-polymer ration) being optimal. F9 exhibited a particle size of 78.4±2.7 nm, zeta potential of −25.0±1.0 mV, drug loading of 12.3±0.6% and encapsulation efficiency of 85.1±2.8%. Sustained in vitro drug release reached 84.56±0.71% at 48 h, following anomalous transport kinetics (<i>R</i><sup>2</sup>=0.98). In an LPS-induced neuroinflammation rat model, F9 reduced TNF-α and IL-6 levels to 38.25±4.82 and 38.91±4.47 pg/mL respectively, and MDA to 1.58±0.28 nmol/mg protein. Cognitive improvement was evident via Morris Water Maze test with escape latency of 20.98±2.27 s. Pharmacokinetically, F9 achieved Cmax of 150.21±15.87 ng/mL, <i>T</i><sub>1/2</sub> of 8.47±1.08 h and AUC of 353.56±41.67 µg<sup>.</sup>h/mL. These results endorse the potential of F9 micelles for managing neuroinflammation and neurodegeneration.</p> Graphical Abstract <p></p>

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RETRACTED ARTICLE: Luteolin-Encapsulated Polymeric Micelles for Anti-inflammatory and Neuroprotective Applications: An In Vivo Study

  • Ruchi Tiwari,
  • Gaurav Tiwari,
  • Bhupesh Chander Semwal,
  • S. Amudha,
  • Shankar Lal Soni,
  • Shashi Ravi Suman Rudrangi,
  • Hanish Singh Jayasingh Chellammal,
  • Pankaj Sharma

摘要

This study aimed to develop luteolin-loaded mPEG-PCL polymeric micelles for improved neuroprotective delivery. A 32 factorial design yielded nine formulations, with F9 (15 mg/mL polymer, 1:20 drug-to-polymer ration) being optimal. F9 exhibited a particle size of 78.4±2.7 nm, zeta potential of −25.0±1.0 mV, drug loading of 12.3±0.6% and encapsulation efficiency of 85.1±2.8%. Sustained in vitro drug release reached 84.56±0.71% at 48 h, following anomalous transport kinetics (R2=0.98). In an LPS-induced neuroinflammation rat model, F9 reduced TNF-α and IL-6 levels to 38.25±4.82 and 38.91±4.47 pg/mL respectively, and MDA to 1.58±0.28 nmol/mg protein. Cognitive improvement was evident via Morris Water Maze test with escape latency of 20.98±2.27 s. Pharmacokinetically, F9 achieved Cmax of 150.21±15.87 ng/mL, T1/2 of 8.47±1.08 h and AUC of 353.56±41.67 µg.h/mL. These results endorse the potential of F9 micelles for managing neuroinflammation and neurodegeneration.

Graphical Abstract